Preliminary SAR and biological evaluation of antitubercular triazolothiadiazine derivatives against drug-susceptible and drug-resistant Mtb strains

Design, Synthesis, and Antifungal Activities of Novel 1,2,4‐Triazole Schiff Base Derivatives

“…Target compounds were synthesized via 4-amino-5-substituted-1,2,4-triazolethione with substituted benzaldehyde using glacial acetic acid as catalyst and solvent. Their structures were confirmed by IR, 1 H-NMR, 13 C-NMR, melting point, elemental analysis, and mass spectra. In addition, their antifungal activities against Pythium solani, Gibberlla nicotiancola, Fusarium oxysporium f. sp.…”

“…Compounds 1a – 1g were prepared according to literatures. [ ][ ] Compounds 2a – 2g , 3a – 3g , and 4a – 4g were synthesized through compounds 1a – 1g and solutions of absolute ethanol containing pyridine‐4‐carbaldehyde (5 mL), 3‐bromo‐6‐hydroxy‐2‐methoxybenzaldehyde (5 mL), and 4‐(1 H ‐imidazol‐1‐yl)benzaldehyde (5 mL) in the presence of glacial acetic acid (2 mL). The mixture was refluxed for about 4 h. TLC was used to monitor the reaction until all raw material disappeared.…”

“…Compounds 1a -1g were prepared according to literatures. [10] [13][14][15] Compounds 2a -2g, 3a -3g, and 4a -4g were synthesized through compounds 1a -1g and solutions of absolute ethanol containing pyridine-4carbaldehyde (5 mL…”

“…Their biological activity showed that parts of the compounds have excellent antifungal activity compared with triadimefon, this result inspires us with passion to synthesize more 1,2,4‐triazole Schiff bases. Some research reported introducing heterocyclic skeleton into structure can enhance the biological activity, on the basis of the above information, we designed and synthesized a series of 1,2,4‐triazole Schiff bases containing pyridine ring, imidazole ring, and halogenated benzene ring, respectively, expecting to find leading compound with higher antifungal activity. Target compounds were synthesized via 4‐amino‐5‐substituted‐1,2,4‐triazolethione with substituted benzaldehyde using glacial acetic acid as catalyst and solvent.…”

1,3‐Oxazole‐isoniazid hybrids: Synthesis, antitubercular activity, and their docking studies

“…Nitrogen‐containing heterocycles constitute a major part of natural products and possess a wide range of applications in medicinal chemistry . Isoniazid (INH) is isonicotinic acid hydrazide, which is a widely employed first‐line drug used for the treatment of TB for more than 60 years and it still rests one of the furthermost effective anti‐TB drug agents.…”