SYNTHESIS AND ANTI-TUBERCULAR ACTIVITY OF SOME 1,2,4-TRIAZOLE DERIVATIVES | ||
| Zagazig Journal of Pharmaceutical Sciences | ||
| Article 4, Volume 11, Issue 1, June 2002, Pages 54-62 PDF (4.63 M) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/zjps.2002.181560 | ||
| Author | ||
| Amal Eissa* | ||
| Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt | ||
| Abstract | ||
| The synthesis of a number of bis-triazole derivatives starting from 2,2 -bis-(4-amino-5-mercapto-4H-1,2,4-triazol-3-yl)diphenyl amine (I) was achieved . Reactions involving its two functional groups for structural diversity was performed. Thus reacting I in DMSO, in CS2/KOH, with acetic anhydride, chloroacetyl chloride, ethyl chloroacetate, epichlorohydrin, 2-chloro-5-nitropyridine, certain-2-chloro aromatic acids (alone or in presence of POCI3), variousα,ß-unsaturated ketones and different aldehydes afforded II-XII respectively. Compounds XIIb(a-h) were further cyclised in nitrobenzene to yield substituted bis-triazolothiadiazoles (XIIIa-h). Compounds I-III, V, VIII, XI, XII, XIII were tested for their anti-tubercular activity. Compounds XIe and XIIIb were found to be active. | ||
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