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1,5-Diaryl-1H-1,2,4-triazole-3-carboxamide derivatives were designed, synthesized, and evaluated for its anticonvulsant activity using maximal electroshock (MES) and chemoshock (scPTZ and Strychnine) animal screen methods. Neurotoxicity was also assessed. In MES model, compound 4f showed 100% of phenytoin activity after both 0.5 and 4 h. In scPTZ model, compound 4e showed 100% of sodium valproate activity. In Strychnine model, compound 4e showed 120% more delay of onset of convulsion and 124% more delay of time of death relative to sodium valproate. Most of the target compounds showed mild neurotoxicity especially compound 4f which showed excellent activity against electroshock. Pharmacophoric study reveals that the synthesized compounds showed good fitting on the pharmacophoric query with good RMSDX results. [ABSTRACT FROM AUTHOR]

A series of S-alkyl derivatives of 3-(substituted-(1,1′-biphenyl)-3-yl)[1,2,4]triazolo[3,4- b][1,3,4]thiadiazole-6-thiol ( 4a- j) were synthesized by conventional and microwave irradiation methods. Microwave method proved to be a rapid and better yield compare to that of conventional method. The synthesized compounds were characterized by H NMR, C NMR, F NMR, IR, LCMS, and elemental spectroscopic analysis. These compounds were screened for their in vitro anticancer activity by MTT assay. Among the tested compounds, the compound 4c was the most promising anticancer agent with IC value 12 μM in HT29 cell line. [ABSTRACT FROM AUTHOR]

Disubstituted 1,2,4-triazoles 3a- k, 4a- k, and 6a- k have been synthesized from anthranilic acid and nicotinic acid, respectively, through a multi-step reaction sequence via their hydrazides. Synthesized compounds were evaluated for their in vitro antimicrobial activity against two gram-positive bacteria ( S. aureus and B. subtilis), three gram-negative bacteria ( E. coli, S. typhi, and K. pneumonia) as well as four fungi ( A. niger, A. fumigatus, A. flavus, and C. albicans). To explore computational approach, structure-activity relationships were generated statistically using the synthesized compounds and their respective quantitative values of biological activities. These models can be used in future for predicting antimicrobial activity on similar class of compounds. [ABSTRACT FROM AUTHOR]

Ring transformation of sydnone ( 1a- i) to 1,3,4-oxadiazoline-2-one ( 2a- i) was carried out using bromine in acetic anhydride. The compounds ( 2a- i) on heating with hydrazine hydrate gave 1,2,4-triazole ( 3a- i) in good yields. The structure of these unknown compounds was confirmed by IR, H NMR, MS and elemental analysis. Further, these compounds were evaluated for the extent of penetration into biological membranes (clog P) drug likeliness and finally drug score was calculated. The title compounds were also screened for their antihyperglycemic, DNA cleavage and antioxidant activity. [ABSTRACT FROM AUTHOR]

A new series of hydrazinecarboxamides ( 5a- n), bearing various methoxyphenyl and methoxyphenethyl groups, was synthesized by condensation of corresponding acid hydrazides ( 3a- f) with methoxyphenylisocyanates ( 4a- c). Dehydrocyclization of hydrazinecarboxamides ( 5a- n) yielded corresponding methoxyphenyl and methoxyphenethyl substituted triazoles ( 6a- l) by refluxing in 2 N aqueous sodium hydroxide solution. All the synthesized compounds were screened for their β-glucuronidase inhibition activity. Compounds 5a, 5e, 5h, and 5l exhibited an excellent β-glucuronidase inhibitory activity as compared to the standard inhibitor. Graphical Abstract: A new series of hydrazinecarboxamides and their 1,2,4-triazole derivatives has been reported. The synthesized compounds were evaluated for their β-glucuronidase inhibition activity. [Figure not available: see fulltext.] [ABSTRACT FROM AUTHOR]

A novel series of pyrazoles containing benzenesulfonamides, 1,3,4-oxadiazole-2-thiones, 4-substituted-1,2,4-triazole-3-thiones, and 2-substituted-1,3,4-thiadiazoles has been synthesized. Anti-inflammatory activity of some synthesized compounds was evaluated in vivo utilizing a standard acute carrageenan-induced paw edema method. The most active anti-inflammatory agents 3, 8f, and 10f were evaluated for ulcerogenic liability in rats compared to indomethacin and celecoxib as reference standards. Molecular modeling studies were initiated herein to validate the attained pharmacological data and provide understandable evidence for the observed anti-inflammatory behavior. [ABSTRACT FROM AUTHOR]

Triazoles and its derivatives are found to possess diverse applications in the field of medicine and industry. A series of novel 1,2,4-triazole derivatives have been synthesized as novel antimicrobial agents starting from different 4-substituted benzoic acids. The chemical structures of these newly synthesized compounds were elucidated by Fourier transform infrared spectroscopy (FTIR), H NMR, C NMR, FAB-MS spectral data, and elemental analysis. Their antimicrobial activities were investigated against four bacterial strains S. aureus (ATCC-25923), P. aeruginosa (ATCC-27853), E. coli (ATCC-8739), B. subtilis (ATCC-6633) and three fungal strains C. albicans (MTCC-227), A. niger (MTCC-3323), and F. oxysporum (MTCC-2087). Preliminary results indicate that some of them exhibit promising activities and deserve further consideration. [ABSTRACT FROM AUTHOR]

A novel series of 1,3,5-triazine analogs was successfully synthesized through conjugation with benzimidazole or 1,2,4-triazole derivatives via a methylenethio linker. The new analogs were in vitro evaluated against HSV-1 in Vero cells; among these analogs, two compounds exhibited good effect in inhibiting HSV-1 replication (for compound 5p: EC = 3.5 μg/ml, SI = 358; for compound 5r: EC = 5.0 μg/ml, SI = 300) in comparison to acyclovir. [ABSTRACT FROM AUTHOR]

A series of 5-substituted-4-amino-3-mercapto-1,2,4-triazoles were synthesized and were treated with various 3-substituted pyrazole aldehydes to obtain a series of new Schiff bases ( 3a- l). Few of the selected Schiff bases were converted into Mannich bases by reaction with diphenylamine/morpholine in presence of formaldehyde in ethanol media ( 4a- e, 5a- e). These newly synthesized compounds were characterized by elemental analysis, IR, NMR and mass spectrometry studies. A comparative study on the cytotoxic activities of few selected Schiff and Mannich bases was done in HepG2 cells using MTT assay. Few of the screened Schiff bases, 3a, 3d, 3e, 3g and 3h showed dose dependent cytotoxic activity, 3a being the most potent with an IC value of 0.018 g/l comparable to the standard drug doxorubicin. Among the Mannich bases, 5b was the most active with an IC value of 0.034 g/l. The Schiff bases were found to be more active, when compared to Mannich bases derived from them. The morpholine derived Mannich bases were more potent than those obtained from diphenyl amine. [ABSTRACT FROM AUTHOR]