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Alkyl phenylcarbamodithioates were reacted with hydrazonoyl bromide 1a, b in ethanol containing a catalytic amount of triethylamine solution to afford and 1,3,4-thiadiazole derevatives 5a, b, respectively. In the same manner, alkyl hydrazinecarbodithioate (6–10)a, b were reacted with the appropriate hydrazonoyl bromide (1a, b) in ethanol containing a catalytic amount of triethylamine solution to afford 1,3,4-thiadiazole derivatives (13–17), respectively. Moreover, hydrazonoyl bromide 1a or 1b was reacted with 5-phenyl-1,3,4-oxadiazole-2-thione 22A in refluxing chloroform containing triethylamine to give 1,3,4-thiadiazole derivatives 21a and b, respectively. Elemental analysis, spectral data, and an alternative synthetic route were used to confirm the structures of all the newly synthesized heterocyclic compounds. AutoDock was used to screen possible drugs. To screen potential medications, AutoDock was utilized. The antiviral medications chloroquine, hydroxychloroquine, and Lopinavir, as well as their synthesized components, were all tested. Confirmation comes from molecular docking and computational investigations. The results of a detailed exploration of the structural characterization of 5b and 13b using quantum chemistry methods calculated using the DFT (B3LYP) method with a 6-31 + g (d, p) basis set are presented in the computational study. The goal of this study was to investigate the molecular dynamics and structural characteristics that regulate chemical behavior, as well as to compare theoretical predictions with experimental results. [ABSTRACT FROM AUTHOR]

Based on the pharmaceutical importance of the coumarin scaffold, we decided here to synthesize and evaluate the biological activity of some new coumarins. The new coumarin derivatives were synthesized starting from 3-(2-bromoacetyl)-2H-chromen-2-one (1) and their structures were clarified by fully spectral data. Ten of the new synthesized compounds were investigated for their anticancer activity against 60 human cancer cell lines by NCI USA. All the tested compounds showed good to mild activity against the tested cancer cell lines. Compounds 5, 7, and 8 were the most active against Renal Cancer UO-31 cancer cell line with growth inhibition percentage of 38.74%, 45.09%, and 34.65%, respectively. Where, compound 12 demonstrated strong to moderate activity toward Leukemia K-562, Renal Cancer UO-31and Breast Cancer T-47D cancer cell lines with growth inhibition percentage of 27.00%, 31.59%, and 32.98%, respectively. [ABSTRACT FROM AUTHOR]

2,3-Dihydro-2-oxo-4-phenyl-6-(thien-2-yl)pyridine-3-carbonitrile (4) was synthesized via reaction of four compounds (benzaldehyde, 2-acetylthiophene, ethyl cyanoacetate and ammonium acetate) in one step reaction. 2-((Hydrazinocarbonyl)methyloxy)-4-phenyl-6-(2-thienyl)pyridine-3-carbonitrile was obtained by reaction of 5 with hydrazine hydrate. Schiff's bases, pyrazole derivatives, urea derivatives, and carbamates were also synthesized. Based on the spectral facts and elemental analysis, structures of the newly synthesized compounds were elucidated. Also, the new compounds were evaluated for their antibacterial and antitumor activities. [ABSTRACT FROM AUTHOR]

Reaction of ethyl 2-(2-((methylthio)carbonothioyl)hydrazono)propanoate (2) and ethyl 2-(2-carbamothioyl-hydrazono)propanoate (3) with hydrazonoyl halides 4a-e afforded the corresponding thiadiazoles 5a-e. Also, treatment of compound 2 with α-ketohydrazonoyl halides 12a-f in absolute ethanol and in the presence of triethylamine gave the corresponding thiadiazoles 13a-f; while reaction of ethyl 2-(2-carbamothioyl-hydrazono)propanoate (3) with α-ketohydrazonoyl halide 12 gave thiazole derivatives 15. Also, the reaction of compound 3 with hydrazonoyl chloride 12f afforded thiazolone derivative 18. Antimicrobial studies are performed using two-gram positive bacteria and two-gram negative bacteria. Data revealed that thiazole derivative 17a achieved the lowest MIC values (high efficient derivative) against the sensitive bacterial strain S. aureus with MIC value 160 µg/ml. [ABSTRACT FROM AUTHOR]

Sodium salt of 3‐hydroxy‐1‐(1‐aryl‐5‐methylpyrazolyl)propenone derivatives was used as a precursor for synthesis of various fused azolopyrimidine ring systems as pyrazolopyrimidines, triazolopyrimidines, and pyrimidobenzimidazoles following many procedures. The identity of the prepared compounds was elucidated by their spectral data and elemental analyses. The in vitro antimicrobial activity of 13 new compounds was evaluated, and many derivatives showed good to moderate activity. [ABSTRACT FROM AUTHOR]

A literature survey revealed that a great deal of interest has been focused on the synthesis of functionalized pyrazole derivatives due to their synthetic and biological potentialities. The pharmacological activities that have been found for some pyrazole derivatives include selective enzyme inhibition, antiviral, estrogen receptor agonist, anti‐inflammatory, anticancer, antiobesity, and antitumor properties. Other activities such as potential inhibitors of HIV‐1, pesticides, fungicides, and antihypertensive agents were reported for other pyrazole derivatives. This review summarizes the synthetic methods and reactions of 3‐acetyl‐pyrazoles, 4‐acetyl‐pyrazoles, and 3,4‐di‐acetyl‐pyrazoles. Most reaction types have been successfully applied and used in the production of biologically active compounds. The aim of this review is to focus mainly on the utility of acetylpyrazole derivatives in the synthesis of heterocyclic compounds during the period 1990–2018. [ABSTRACT FROM AUTHOR]

Sodium 1‐aryl‐3‐(3‐(ethoxycarbonyl)‐5‐methyl‐1H‐pyrazol‐4‐yl)‐3‐oxoprop‐1‐en‐1‐olate was used as precursor for the preparation of some novel derivatives of various fused azolotriazine ring systems via coupling reactions with hetaryldiazonium salts. Hydrazinolysis of the latter products yielded the corresponding pyrazolopyridazine derivatives. The structures of the products were established by their spectral data and elemental analyses. The antibacterial and antifungal activities of some of the new products were also evaluated. [ABSTRACT FROM AUTHOR]

A new series of 1,3‐thiazole‐benzofuran derivatives was synthesized via heterocyclization of 2‐(1‐(6‐alkoxy‐4,7‐dimethoxybenzofuran‐5‐yl)ethylidene)‐2‐methyl‐2l4‐diazane‐1‐carbothioamides with hydrazonoyl halides. Also, 1‐(4,7‐dimethoxybenzofuran‐5‐yl)‐3‐phenylprop‐2‐en‐1‐one derivatives were used for synthesis of another series of 1,3‐thiazole‐pyrazole‐benzofuran. The structure of the newly synthesized products was elucidated via elemental analysis, spectral data, and alternative routes whenever possible. Seven new compounds were evaluated for their anticancer activity against the human breast carcinoma (MCF‐7) cell lines compared with doxorubicin drug. The results revealed that some new compounds showed promising anticancer activity. [ABSTRACT FROM AUTHOR]

Two series of novel 1,3,4-thiadiazole-benzofuran and 1,3,4-thiadiazole-furochromene derivatives were synthesized through heterocyclization of alkyl 2-(1-(6-hydroxy-4,7-dimethoxybenzofuran-5-yl)ethylidene)hydrazine-1-carbodithioate 3a-f and 2-(1-(5-methoxy-8-methyl-2,6-dioxo-2,6-dihydropyrano[3,2-g]chromen-3-yl)ethylidene)hydrazinecarbothioamide 9a,b with various hydrazonoyl halides, respectively. The structure of the newly synthesized products was elucidated through elemental analysis, spectral data and alternative routes whenever possible. Ten new compounds were evaluated for their anticancer activity against the human breast carcinoma (MCF-7) cell lines in comparison with reference doxorubicin using MTT assay. The results showed that some new compounds have promising anticancer activity. [ABSTRACT FROM AUTHOR]

In the rapidly expanding era of cancer target therapy, regulators of apoptosis are emerging as attractive therapeutic targets. X-linked inhibitor of apoptosis (XIAP) is of specific interest owing to its characteristic overexpression in a wide variety of neoplasms, with a resultant survival advantage for tumor cells and treatment resistance. In this study, we examined three pyrazolo [3,4- d ] pyridazine derivatives (PPDs) through molecular modeling and studied their modes of interaction with XIAP-BIR3 domain. PPD-1, which possessed the highest binding affinity with XIAP, was tested on A549 (lung cancer cell line); HCT-116 (colorectal carcinoma cell line); HEPG2 (liver carcinoma cell line), HFB4 (normal human skin melanocyte cell line) and WI-38 (human embryonic lung fibroblasts). In comparison to cisplatin as a positive control, PPD-1 yielded remarkable cytotoxicity on all cancer cell lines, with the highest anti-tumor activity on A549 and a favorable therapeutic ratio. Flow cytometry studies concluded that PPD-1 treatment induces Sub G1 and G2/M cell cycle arrest and apoptosis. The percentage of apoptotic cells in PPD-1 treated A549 cells was considerably higher than that in untreated cells (10.06% vs 0.57%, respectively). To further investigate the mechanism of induction of apoptosis by PPD-1, Real time-PCR was used to quantify the expression levels of key apoptotic regulators. Significant overexpression of the effector capsase-3 , pro-apoptotic bax and tumor suppressor gene p53 were noted as compared to untreated cells (7.19 folds, 7.28 folds, and 5.08 folds, respectively). Moreover, PPD-1 inhibited the expression of the anti-apoptotic bcl-2 gene to 0.22 folds. These findings demonstrate that PPD-1 treatment disrupts the Bcl-2/BAX balance in lung cancer cell lines, leading to apoptosis induction possibly through intrinsic mitochondria-dependent pathway. These novel insights elucidate the mechanism of PPD-1 cytotoxicity in lung cancer cell lines and offer a promising therapeutic approach that needs further study. [ABSTRACT FROM AUTHOR]

Due to its high potency and selectivity, anticancer agents consisting of combined molecules have gained great interests. The current study introduces newly synthesized progesterone derivatives of promising anticancer effect. Moreover, the pro-apoptotic and anti-angiogenic effects of these compounds were studied extensively. Several thiazole, pyridine, pyrazole, thiazolopyridine and pyrazolopyridine progesterone derivatives were synthesized. The structure of the novel progesterone derivatives was elucidated and confirmed using the analytical and spectral data. This novel derivatives were tested for their cytotoxic effect against human breast cancer cells (MCF-7) using neutral red uptake assay. Tested compounds showed anticancer activity against MCF-7 cancer cell line in the descending order of 7 > 2 > 3 > 8 > 6 > 9 > 4 . The expression levels of Bcl-2, survivin, CCND1, CDC2, P53 and P21, VEGF, Hif-1α, MMP-2, MMP-9, Ang-1, Ang-2, and FGF-1 genes were investigated using QRT-PCR (Quantitative real time-polymerase chain reaction). The study clarified that compounds 2 , 3 , 4 , 6 , 7 , 8 and 9 showed significant pro-apoptotic effect through the down regulation of Bcl-2., besides, survivin and CCND1 expression levels were down regulated by compounds 3 , 4 , 6 , 7 , 8 , 9 . However, Compound 4 may exert this pro-apoptotic effect through the up-regulation of P53 gene expression. On the other hand, the anti-angiogenic effect of these newly synthesized derivatives was due to their down regulation of VEGF, Ang-2, MMP-9 and FGF-1; and the up-regulation of HIF-1α and ang-1. This study recommended promising pro-apoptotic and anti-angiogenic anticancer agents acting through the regulation of key regulators of apoptosis, cell cycle genes, and pro-angiogenic genes. [ABSTRACT FROM AUTHOR]

Three novel series of nitroso derivatives (11 – 15 ), isoxazolopyrazoles ( 17a – c ) and isoxazolo[3,4- d ]pyridazines (18a – c ) were prepared from the hydroxyimoyl chloride 10 . In vitro COX1⧹2 inhibition activities were evaluated, both of 17b and 18a proved a promising inhibitory activity with IC 50 = 1.12, 0.78 μM in sequent . Carrageenan induced Paw edema, ulcer liability, nitric oxide (NO ) release and histopathological study were determined. Most of the prepared compounds showed excellent activities. Reactions of 2-aminopyridine and enaminone with hydroxyimoyl chloride 10 were investigated and proved by 2D NMR. Molecular docking for most active compounds was operated giving a hint for compound–receptor interactions . [ABSTRACT FROM AUTHOR]

A series of new 5-(heteroaryldiazenyl)thiazole incorporating pyrazole moiety have been synthesized through coupling of the thiazole with the appropriate heteroaryldiazonium salts. The newly synthesized compounds were characterized by elemental analysis, spectroscopic (IR, 1H NMR, and Mass) data, and alternative synthesis whenever possible. [ABSTRACT FROM AUTHOR]

2-(5-Methyl-1-phenyl-1H-pyrazol-4-yl)-2-oxo-N′-phenylaceto-hydrazonoyl bromide was synthesized and used as precursor for synthesis of some new 1,3,4-thiadiazoles, pyrrolo[3,4-c]pyrazoles, and 1,2,4-triazolo[4,3-a]pyrimidines. The mechanisms that account for formation of products were discussed. Also, the structures of all the newly synthesized products were confirmed based on elemental analysis, spectral data and by alternative methods. [ABSTRACT FROM AUTHOR]

2-(2-(1-(1 H-Indol-3-yl)ethylidene)-hydrazinyl)-4-substituted 5-(aryldiazenyl)thiazoles and 5-((1-(1 H-indol-3-yl)ethylidene)hydrazono)-2-substituted-4-phenyl-4,5-dihydro-1,3,4-thiadiazoles were synthesized via reaction of hydrazonoyl halides and 2-(1-(1 H-indol-3-yl)ethylidene)hydrazine-1-carbothioamide and alkyl 2-(1-(1 H-indol-3-yl)ethylidene)hydrazine-1-carbodithioate in ethanolic triethylamine. Structures of the newly synthesis were elucidated on the basis of elemental analysis, spectral data, and alternative synthetic route whenever possible. [ABSTRACT FROM AUTHOR]

Pyrazolo[3,4- d]pyridazines, isoxazolo[3,4- d]pyridazines, azolo[1,5- a]pyrimidines, azolo[5,1- c]triazines, pyrazoles, and benzo[ b][l,4]diazepine were synthesized from the appropriate hydrazonoyl halides, hydroximoyl halides, heterocyclic amines, diazotized heterocyclic amines, arenediazonium chlorides, and o-phenylenediamines with appropriate of sodium 3-(5-bromobenzofuran-2-yl)-3-oxoprop-1-en-1-olate or 1-(5-bromobenzofuran-2-yl)-3-(dimethylamino)prop-2-en-1-one. The newly synthesized compounds were elucidated by elemental analyses, spectral data, and alternative synthesis whenever possible. [ABSTRACT FROM AUTHOR]

A novel series of 1,3,4-thiadiazoles, 5-arylazothiazoles and hexahydropyrimido-[4,5-d] [1,2,4]triazolo[4,3-a]pyrimidines were synthesized via reaction of hydrazonoyl halides with each of alkyl carbothioates, carbothioamides and 7-thioxo-5,6,7,8-tetrahydropyrimido-[4,5-d]pyrimidine- 2,4(1H,3H)-diones in the presence of triethylamine. The structures of the newly synthesized compounds were established based on their spectral data, elemental analyses and alternative synthetic routes whenever possible. Also, the newly synthesized compounds were screened for their antimicrobial activity against various microorganisms. [ABSTRACT FROM AUTHOR]

2-(3-(1H-Indol-3-yl)-5-(p-tolyl)-4,5-dihydro-1H-pyrazol-1-yl)-4-substituted-5-(substituted diazenyl)thiazoles and 2-(1H-indol-3-yl)-9-substituted-4,7-disubstituted pyrido[3,2-e][1,2,4]triazolo [4,3-a]pyrimidin-5(7H)-ones were synthesized via reaction of hydrazonoyl halides with each of 3-(1H-indol-2-yl)-5-(p-tolyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide and 7-(1H-indol-3-yl)-2- thioxo-5-substituted-2,3-dihydropyrido[2,3-d]pyrimidin-4(1H)-ones, respectively. Also, hydrazonoyl halides were reacted with N’-(1-(1H-indol-3-yl)ethylidene)-2-cyanoacetohydrazide to afford 1,3,4-thiadiazole derivatives. Structures of the new synthesis were elucidated on the basis of elemental analysis, spectral data, and alternative synthetic routes whenever possible. Fifteen of the new compounds have been evaluated for their antitumor activity against the MCF-7 human breast carcinoma cell line. The results indicated that many of the tested compounds showed moderate to high anticancer activity when compared with doxorubicin as a reference drug. [ABSTRACT FROM AUTHOR]

1,3,4-Thiadiazoles, pyrazolo[1,5- a]pyrimidines, pyrazolo[5,1- c]triazine, and thieno[3,2- d]pyrimidines were synthesized from 1-(5-bromobenzofuran-2-yl)ethanone. The structures of the newly synthesized compounds were elucidated by elemental analysis, spectral data, chemical transformation, and alternative synthesis route whenever possible. [ABSTRACT FROM AUTHOR]

Synthesis of pyrazolo[1,5- a]pyrimidines, [1,2,4]triazolo[1,5- a]pyrimidine, 8,10-dimethyl-2-(5-methyl-1-phenyl-4,5-dihydro-1 H-1,2,3-triazol-4-yl)pyrido[2′,3′:3,4]-pyrazolo[1,5- a]pyrimidine, benzo[4,5]imidazo[1,2- a]pyrimidine via heterocyclic amines, and sodium 3-hydroxy-1-(5-methyl-1-phenyl-1 H-1,2,3-triazole-4-yl)prop-2-en-1-one were carried out. Also, synthesis of isoxazoles, and pyrazoles from sodium 3-hydroxy-1-(5-methyl-1-phenyl-1 H-1,2,3-triazole-4-yl)prop-2-en-1-one and hydroxymoyl chlorides and hydrazonoyl halides, respectively, were made. Analogously, (1,2,3-triazol-4-yl)thieno[2,3- b]pyridine derivatives were obtained from sodium 3-hydroxy-1-(5-methyl-1-phenyl-1 H-1,2,3- triazole-4-yl)prop-2-en-1-one and cyanothioacetamide followed by its reacting with active methylene compounds. In addition to full characterization of all synthesized compounds, they were tested to evaluate their antimicrobial activities, and some compounds showed competitive activities to those of tetracycline, the typical antibacterial drug, and clotrimazole, the typical antifungal drug. [ABSTRACT FROM AUTHOR]

Starting from N -aryl 2-aroylhydrazono-propanehydrazonoyl chlorides, a series of new functionalized 1,3,4-thiadiazoles were prepared. The structures of the compounds prepared were confirmed by both elemental and spectral analyses as well as by alternate synthesis. The mechanisms of the studied reactions are outlined. The antimicrobial activities of the compounds prepared were screened and the results showed that most of such compounds exhibit considerable activities. [ABSTRACT FROM AUTHOR]

Condensation of sodium 3-oxo-3-(1-phenyl-1H-pyrazol-4-yl)prop-1-en-1-olate (2) with several heterocyclic amines, cyanoacetamide, cyanothioacetamide, and 2-cyanoacetohydrazide gives pyrazolo[1,5-a]pyrimidines (5a-d), pyrido[2',3':3,4]pyrazolo[1,5- a]pyrimidine (9), benzo[4,5]imidazo[1,2-a]pyrimidine (10), [1,2,4]triazolo[1,5-a]pyrimidine (11), and pyridine derivatives (12-14). Also, thieno[2,3-b]pyridines (15-18) were synthesized via pyridinethione (13) with α-halo ketones and α-halo ester. Structures of the newly synthesized compounds were elucidated by elemental analysis, spectral data, alternative synthetic routes, and chemical transformation whenever possible. [ABSTRACT FROM AUTHOR]

2,3-Dihydro-1,3,4-thiadiazoles, 2,3-dihydro-1,3,4-selenadiazoles, and triazolino[4,3- a]pyrimidines containing benzofuran moiety were prepared from the reaction of 2-(2-phenylhydrazono)-1-(5-bromobenzofuran-2-yl)-2-chloroethanone with each of potassium thiocyanate, potassium selenocyanate, alkyl carbodithioate, and pyrmidine-2-thione derivatives. All the newly synthesized compounds were confirmed by elemental analysis, spectral data, and alternative route synthesis whenever possible. [ABSTRACT FROM AUTHOR]

Naphtho[2,1- b]furan-2-yl)(8-phenylpyrazolo[5,1- c][1,2,4]triazin-3-yl)methanone, ([1,2,4]triazolo[3,4- c][1,2,4]triazin-6-yl)(naphtho[2,1- b]furan-2-yl)methanone, benzo[4,5]imidazo[2,1- c][1,2,4]triazin-3-yl-naphtho[2,1- b]furan-2-yl-methanone, 5-(naphtho[2,1- b]furan-2-yl)pyrazolo[1,5- a]pyrimidine, 7-(naphtho[2,1-b]furan-2-yl)-[1,2,4]triazolo[4,3-a]pyrimidine, 2-naphtho[2,1- b]furan-2-yl-benzo[4,5]imidazo[1,2- a]pyrimidine, pyridine, and pyrazole derivatives are synthesized from sodium salt of 5-hydroxy-1-naphtho[2,1- b]furan-2-ylpropenone and various reagents. The newly synthesized compounds were elucidated by elemental analysis, spectral data, chemical transformation, and alternative synthetic route whenever possible. J. Heterocyclic Chem., (2012). [ABSTRACT FROM AUTHOR]

Abstract: Pyrrolo[3,4-c]pyrazole-4,6(1H,5H)-dione, pyrano[2,3-c]pyrazole-5-carbonitrile, pyrano[2,3-d]4-imidazolines, pyrido[2,1-b]benzimidazole, pyrido[2,1-b][1,3]benzoxazole, pyrido[2,1-b][1,3]benzothiazole and pyrido[2,1-b]quinazoline were synthesised from antipyrine derivatives with appropriate reagents such as maleimides, malononitrile, ethyl cyanoacetate, benzimidazole-2-acetonitrile, benzothiazole-2-acetonitrile, benzoxazol-2-acetonitrile, benzoylacetonitrile and other reagents. The newly synthesised compounds were established by elemental analysis, spectral data, and alternative synthetic routes whenever possible. [Copyright &y& Elsevier]

1-(2-(4,5-Dihydro-3-(4-methyl-2-phenylthiazol-5-yl)-5-phenylpyrazol-1-yl)-4-substituted thiazol-5-yl)-2-phenyldiazene were synthesized from hydrazonoyl halides and 3-(4-methyl-2-phenyl-1,3-thiazol-5-yl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide in ethanolic triethylamine. Also, pyrazolo[5,1-a]pyrimidines, 2,3,6-trisubstituted pyridines, and pyrazolo[3,4-d]pyridazines were obtained from sodium salt of 3-hydroxy-1-(4-methyl-2-phenylthiazol-5-yl)prop-2-en-1-one and different heterocyclic amines. All structures of the newly synthesized compounds were elucidated by elemental analysis, spectral data, and alternative synthetic route whenever possible. The newly synthesized compounds were tested towards different microorganisms. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. [ABSTRACT FROM AUTHOR]

3-Arylazo-2-(4-methyl-2-phenylthiazol-5-yl)imidazo[1,2-a]pyrimidine, 2-(4-methyl-2-phenyl-1,3-thiazol-5-yl)-3-phenylazoimidazo[1,2-a]pyridine, 3-arylazo-2-(4-methyl-2-phenylthiazol-5-yl)-6-phenyl-5Himidazo[1,2-b]pyrazole, 6-(4-methyl-2-phenyl-thiazol-5-yl)-5-phenylazo3-phenyl-imidazo[2,1-b]thiazole, 3-(4-methyl-2-phenylthiazol-5-yl)-2-phenylhydrazino-(1H)-quinoxaline, 3-(4-methyl-2-phenylthiazol-5-yl)- 2-phenylazoquinoxaline, 3-(4-methyl-2-phenylthiazol-5-yl)-2-phenylhydrazinobenzo-[1,4] thiazine, 3-(4-methyl-2-phenyl-thiazol-5-yl)-2-phenylhydrazinobenzo[1,4]oxazine, and 3-(4-methyl-2-phenylthiazol-5-yl)-2-phenylazo-1H-pyrido[2,3-b]pyrazine derivatives were synthesized via reaction of 2-(4-methyl-2-phenyl-1,3-thiazol-5-yl)-2-oxo-N-arylethanehydrazonoyl bromide with each of 2-aminopyrimidine, 2-aminopyridine, 3-aminopyrazoles, 2-amino-4-phenylthiazole, o-phenylenediamine, o-aminothiophenol, o-aminophenol, or 2, 3-diaminopyridine, respectively. All structures of the newly synthesized compounds were elucidated by elemental analysis, spectral data, and alternative synthetic route whenever possible. The entire newly synthesized compounds are tested toward different microorganisms. [ABSTRACT FROM AUTHOR]

Thieno[2,3-b]pyridines were synthesized from 6-benzofuran-2-yl-4-phenyl-2-sulfanylpyridine-3-carbonitrile and each of chloro acetone, ethyl chloroacetate, ω -bromoacetophenone, and chloroacetonitrile. These compounds were conveniently converted into novel pyrido[4',5':4,5]thieno[3,2-d]pyrimidines. Also, 2,3-dihydro-1,3,4-thiadiazole was synthesized from hydrazonoyl halides and 2-benzofuran-2-yl-3-(phenylamino)-3-thioxopropanenitrile. The structures of the products have been elucidated by elemental analyses, spectral data studies, and alternative syntheses whenever possible. The newly synthesized compounds were tested towards microorganisms. [ABSTRACT FROM AUTHOR]

2-[1,2-Diaza-3-(2,3-dimethyl-5-oxo-1-phenyl(3-pyrazolin-4-yl))prop-2-enylidene]-3-phenyl-5-substituted 1,3,4-thiadiazolines and 2-{[4-(2,3-dimethyl-5-oxo-1-phenyl(3-pyrazolin-4-yl))(1,3-thiazol-2-yl)]cyanomethylene}-3-phenyl-5-substitu- ted 1,3,4-thiadiazolines were synthesized from hydrazonoyl halides and 4-{-2-aza-2-[(methylthiothioxomethyl)amino]vinyl}-2,3-dimethyl-1-phenyl-3-pyrazoin-5-one and 2-[4-(2,3-dimethyl-5-oxo-1-phenyl-3-pyrazolin-4-yl)-1,3-thiazol-2-yl]ethane-nitrile, respectively. All synthesize compounds were elucidated by elemental analysis, spectra, and alternative synthesis routes, whenever possible. [ABSTRACT FROM AUTHOR]

1,3,4-Thiadiazolines containing a chromone moiety and 5-{1-[4-substituted-5-phenyldiazenyl)(1,3-thiazol-2-yl]-5-phenyl-2-pyrazolin-3-yl)}-4-methoxybenzo[b]-furan-6-ol were synthetic from hydrazonoyl halide and alkyl carbodithioates and 5-[1-aminothiomethoxy)-5-phenyl-2-pyrazolin-3-yl)]-4-methoxybenzo[b]furan-6-ol, respectively. All structures of the newly synthesized compounds were elucidated by elemental analysis, spectral data, and alternative synthesis methods whenever possible. [ABSTRACT FROM AUTHOR]

2,3-Dihydro-1,3,4-thiadiazole, triazolino[4,3-a]pyrimidine and pyrimido[1,2-b][1,2,4,5]tetrazin-6-one containing benzofuran Moiety were synthesized from C-benzofuran-2-yl-N-phenylhydrazonoyl bromides, and the appropriate alkyl arylidenehydrazinecabodithioates and pyrimidine-2-thione and N-aminopyrimidine-2-thione, respectively. All structures of the newly synthesized compounds were elucidated by elemental analysis, spectral data, and alternative synthetic methods whenever possible. Newly compounds are capable of high inhibiting the growth of bacteria (gram positive and gram negative). [ABSTRACT FROM AUTHOR]

2,3-Dihydro-1,3,4-thiadiazoles and triazolino[4,3-a]pyrimidines containing benzofuran moiety were prepared from reaction of 1-bromo-2-(5-chlorobenzofuranyl) ethanedione-1-phenylhydrazone with each of potassium thiocyanate, alkyl carbodithioates and pyrmidine-2-thiones. All newly synthesized were confirmed by elemental analysis, spectral data, and alternative route synthesis whenever possible. [ABSTRACT FROM AUTHOR]

2-(5-imino-4-aryl-4,5-dihydro-[1,3,4]-thiadiazole-2-(carbonyl)benzo[f]chro-men-2-one, 2-(2-amino-5-arylazothiazol-4-yl)benzo[f]chromen-3-one and ethyl 6-methyl-3-oxo-benzo [f]chromen-2-yl)-1,4-dihydro-[1,2,4]triazolo[4,3-a]pyrimidine-5-carboxy- late were synthesized from hydrazonoyl bromides. Structures of the newly synthesized compounds were established by elemental analysis, spectral data and alternative synthesis route whenever possible. [ABSTRACT FROM AUTHOR]

6-(2-Naphtyl)-1-phenyl-4-3,5-disubstituted 4,3a-triazolino[4,3-a]pyrimidines, [2(1-(2-naphthyl)-5-substitued (1-pyrazolin-3-yl)-4-phenyl(thiazol-5-yl)phenyldiazine and 1-(2-aza-2-[4-phenyldiazenyl)-(1,3-thiazol-2-yl)]amino}vinyl)-naphthalene-2-ol were synthesized via reactions of hydrazonoyl halides with 4-(2-naphthyl)-6-substituted 3,4-dihydropyrimidine-2-thione, Amino(3-(2-naphthyl)-5-substituted pyrazolin-2-ylmethane-1-thione, and 2-hydroxynaphthalenecarbaldehyde-thiosemicarbazone. All structures of the newly synthesized compounds were elucidated by elemental analysis, spectral data, and alternative synthesis methods whenever possible. Some of the new compounds were tested towards bacteria. In general, all tested compounds were capable of highly inhibiting the growth of gram positive of bacteria and gram negative. [ABSTRACT FROM AUTHOR]

[5-Substituted 2-(3-phenyl-5-substituted 2-pyrazolinyl)(1,3-thiazol-4-yl)] phenyldiazene and 2,3-dihydro-1,3,4-thiadiazoles were synthesized via reactions of hydrazonoyl halides with 5-substituted-3-phenyl-4,5-dihydropyrazole-1-carboximidothionic acid and {[2-2-}aza-2-((methylthioxomethyl)-amino]-vinyl}phenyl)-1-azavinyl]amino}methylthiomethane-1-thione, respectively. All structures of the newly synthesized compounds were elucidated by elemental analysis, spectral data, X-ray single crystal, and alternative synthesis methods whenever possible. Some of the new compounds were tested towards bacteria. In general, all tested compounds were capable of a high inhibiting the growth of gram positive and gram negative. [ABSTRACT FROM AUTHOR]

[5-Substituted 2-(3-phenyl-5-substituted 2-pyrazolinyl)(1,3-thiazol-4-yl)]phenyldiazenes, triazolo[3,4-a]pyrimidines, and 2,3-dihydro-1,3,4-thiadiazoles were synthesized with good yields from reactions of hydrazonoyl halides with 5-substituted-3-phenyl-4,5-dihydropyrazole-1-carboximidothionic acid, pyrimidine-2-thione, methyl carbodithioate, respectively. All structures of the newly synthesized compounds were elucidated by elemental analysis, spectral data, and alternative synthesis methods. Newly developed compounds are capable of inhibiting the growth of bacteria (gram positive and gram negative) greatly. [ABSTRACT FROM AUTHOR]

1-amino-4-methyl-4H-3-thia-4,5a,10-triazacyclopenta-[ a ]fluoren-5-one and 6-methyl-6H-,9H-thia-4b,6,9,11,12-pentaazaindeno[1,2- a ]-fluorene-5,8-dione derivatives were prepared from 2-methyl-1-oxo-3-thioxo-2,4,9 b -trihydropyrimidino[1,6- a ] benzimidazole-4-carbonitrile. Also, 2,3-dihydro-1,3,4-thidazoles were synthesized via a reaction of hydrazonoyl chlorides with 3-(methylamino)-2-substituted 3-thioxopropanenitrile. Structures of newly synthesized compounds were elucidated on the basis of elemental analyses, spectral data, and alternative methods synthesis whenever possible. [ABSTRACT FROM AUTHOR]

Triazoles, thiadiazoles, and triazolo[4, 3-a]pyrimidines were synthesized via reaction of hydrazonoyl halides with each of 3-methyl-4-(methylthiothioxomethyl)-2-pyrazolin-5-one, 3-methyl-4-[methylthio(phenylamino)methyl]-2-pyrazolin-5-one, and pyrimidine-2-thiones. Structures of the newly synthesized compounds were elucidated on the basis of elemental analysis, spectral data, and alternative-methods synthesis whenever possible. [ABSTRACT FROM AUTHOR]

Thiazolylacetonitrile was used in the synthesis of coumarin, pyrazolo[4,3]pyrimidines, 1,3,4-thiadiazolines, aminothiophenes, and thiazoles in a good yields. Also, pyrazolo[4,5- d ]triazolino[4,5- a ]pyrimidines, pyrazolo[4,5- d ]thiazolino[3,2-a]pyrimidines, and pyrazolo[4,5-d]tetrazolino[1,5-a]pyrimidines were synthesized from pyrazolo[4,5-d]pyrimidine. Structures of the newly synthesized were elucidated by elemental analysis, spectral data, and alternative synthesis routes whenever possible. Some synthesized compounds were tested for their antimicrobial activity. [ABSTRACT FROM AUTHOR]

Coumarin, thiazole, and 2,3-dihydro-1,3,4-thiadiazole derivatives were synthesized from 2-(4-naphtho[1,2- d ]furan-2-yl-1,3-thiazol-2-yl)ethanenitrile and different reagents. Structures of the new compounds were elucidated on the basis of elemental analysis, spectral data, and alternative methods of synthesis whenever possible. [ABSTRACT FROM AUTHOR]

2,3-Dihydro-1,3,4-thiadiazoles, 2,3-dihydro-1,3,4.selenadiazoles, unsymmetrical azines and triazolino[4,3-a]pyrimidines were prepared from reaction of (2Z)-3-aza-2-bromo-1-naptho[1,2-d]furan-2-yl-3-(phenylamino)prop-2-en-1- one (6) with each of potassium thiocyanate, potassium selenocyanate, alkyl carbodithioate, ethyl 6-methyl-2-methylthio-4-substituted 3,4-dihydropyrimidine-5-carboxylate or (ethyl 4-methyl-6-substituted 2-thione-1,3,6-trihydropyrimidine-5-carboxylate). All compounds were elucidated on the basis of elemental analysis, spectral data. and alternative synthesis method whenever possible. [ABSTRACT FROM AUTHOR]

C-acyl-N-phenyllhydrazonoyl halides1a–ghave been caused to react with 3-(aminomethylthiomethyl)-2H-chromen-2-one in the presence of triethylamine to give triazoles. Also, C-acyl-N-pyrazolylhydrazonoyl chlorides13a,breact with alkyl carbodithioates (14or15)a–mafforded 2,3-dihydro-1,3,4-thiadiazoles in good yields. Structures of the new compounds were elucidated on the basis of elemental analyses, spectral data, and alternative methods of synthesis whenever possible. [ABSTRACT FROM AUTHOR]

1,3,4-Thiadiazolines, 1,3,4-selenadiazolines and triazolino[4,3-a]pyrimidines have been synthesized from 3-aza-[2,4-dimethyl(1,3-thiazol-5-yl) -2-bromo-3-substituted-amino]prop-2-en-1-ones with potassium thiocyanate, potassium selenocyanate, alkyl carbodithioates and 6-methyl-2-methylthio-4-substituted 3,4-dihydropyrimidine-5-carboxylates. Structures of the newly synthesized compounds have been established by elemental analysis, spectral data and alternative synthesis whenever possible. Some of products have been tested towards bacteria. [ABSTRACT FROM AUTHOR]

1,2,4-Triazolo[4,3-a]pyrimidines, thiadiazolines and selenadiazolines synthesized via reactions of hydrazonoyl halides with each of ethyl 4 - (3, 4- dimethoxyphenyl) -6-methyl -2-methylthio-3,4-dihydropyrimidine -5-carboxylate (or ethyl 6-(3,4-dimethylphenyl)-4-methyl-2-thio -1,3,6-trihydropyrimidine-5-carboxylate), ethyl 4-(2,3-dimethoxyphenyl) -6-methyl-2-methylthio-3,4-dihydropyrimidine-5-carboxylate, potassium thiocyanate, potassium selenocyanate, and carbodithioates respectively. [ABSTRACT FROM AUTHOR]

Some new 2,3-dihydro-1,3,4-thiadiazoles containing pyrazol-3-yl, indolin-2-one-2-yl and indan-1,3-dione-2-yl moieties in a good yields obtained from the reaction of hydrazonoyl halides with thiocarbamate and carbodithioate in ethanolic triethylamine respectively. In contrast, pyrazolylthiourea reacts with hydrazonoyl halides under the same condition afford corresponding hydrazonoyl sulfide derivatives. [ABSTRACT FROM AUTHOR]

Background: Pyrazolines show different biological activities. In recent years, interest in the chemistry of hydrazonoyl halides has been renewed. 1,3,4-Thiadiazoles are one of the most common heterocyclic pharmacophores with a wide range of biological activities. Results: Ethyl 2-(5-(furan-2-yl)-3-(p-tolyl)-4,5-dihydro-1H-pyrazol-1-yl)-4-methyl-thiazole-5-carboxylate, 2-(5-(furan-2-yl)-3-(p-tolyl)-4,5-dihydro-1H-pyrazol-1-yl)thiazol-4(5H)-one, and 1-(2-(5-(furan-2-yl)-3-(p-tolyl)-4,5-dihydro-1H-pyrazol-1-yl)-4-methylthiazol-5-yl)ethan-1-one were synthesized from the reaction of 5-(furan-2-yl)-3-(p-tolyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide with different halogenated compounds. Thiazole, 1,3,4-thiadiazole and pyrano[2,3-d]thiazole derivatives were also synthesized. The structures of the newly synthesized compounds were elucidated based on elemental analysis, spectral data, and alternative synthetic routes whenever possible. Additionally, the newly synthesized compounds were screened for antimicrobial activity against various microorganisms. Conclusions: A new series of novel functionalized 1,3,4-thiadiazoles, 1,3-thiazoles, and pyrazoline-containing moieties were synthesized using hydrazonoyl halides as precursors and evaluated for their in vitro antibacterial, and antifungal activities. The antimicrobial results of the examined compounds revealed promising results and some derivatives have activities similar to the references used. [ABSTRACT FROM AUTHOR]

Nanoparticles supply an environmentally friendly procedure for the synthesis of pyrano[2,3-d]pyrimidines by the one-pot three-component condensation reaction of thiobarbituric acid and malononitrile with pyrrol-2-carboxaldehyde. The catalyst could be easily recovered using an external magnet and reused for six cycles with almost consistent activity. A facile synthesis of a new series of cyclic and acyclic nucleosides of pyrano[2,3-d]pyrimidines derivatives was performed. The synthesis of poly heterocyclic compounds starting from pyrano[2,3-d]pyrimidines derivatives was achieved. Structures of the newly synthesized compounds were confirmed on the bases of elemental analyses and spectral data (IR, 1H NMR, 13C NMR, and mass spectra). Compound 6 exhibited the most potent biological activity. [ABSTRACT FROM AUTHOR]

The title compounds are prepared from brominated benzofuran (I) using standard procedures. [ABSTRACT FROM AUTHOR]

Some of the title compounds exhibit competitive antibacterial and antifungal activity. [ABSTRACT FROM AUTHOR]