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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]

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]

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]

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]

2,3-Dihydro-1,3,4-thiadiazoles, 2,3-dihydro-1,3,4-selenadiazoles, and triazolino[4,3-a]pyrimidines containing benzoxazole or benzothiazole moieties were prepared from the reaction of each of ethyl 3-aza-3-(benzoxazol-2-ylamino)-2-chloroprop-2-enoate and ethyl 3-aza-3-(benzothiazolo-2-ylamino)-2-chloroprop-2-enoate 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. Some of the newly synthesized compounds were screened toward certain cancer tumors. 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]

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]

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]

2,3-dihydro-1,3,4-thiadiazoles, triazolino[4, 3- a ] pyrimidines , andpyrazolo [3, 4- d ]pyridazines were synthesized in good yields from reactions of hydrazonoyl halides with alkyl carbodithioates, pyrimidine-2-thione, and substituted prop-2-ene-1-one, respectively. All structures of the newly synthesized compounds were elucidated by elemental analysis, spectral data, and an alternative synthesis method. Some of the new compounds were tested towards bacteria and fungi. [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]

Hydrazonoyl halides 4a-h have been caused to react with each of alkyl carbodithioates ( 3 , 13-17 ) a , b in the presence of triethylamine to give 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]

Hydrazonoyl halides have been caused to react with each of ethyl 4-(2 H -benzo[3,4- d ]1,3-dioxolen-5-yl)-6-methyl-2-methylthio-3,4-dihydropyrimidin-5-carboxylate, potassium thiocyanate (or thiourea), potassium selenocyanate, and alkyl carbodithioate in the presence of triethylamine to give 4,3-dihydro-1,2,4-triazolino[4,3- a ]pyrimidine, 1,3,4-thiadiazoline, 1,2,4-selenadiazoline, and unsymmetrical azine derivatives 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]

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]