A series of new benzimidazole derivatives, namely 2-acylbenzimidazoles 2–9, a dihydroquinoxaline 10, a benzoxazine 11, quinolines 13–15 and fused 1,2,4-triazines 17–24 were synthesized. Structure elucidation of the compounds was conducted using IR, 1H NMR, 13C NMR, mass spectral data and elemental analysis. These products were evaluated for in vitro antitumor activity against MCF7 cell line (human breast cancer). Compounds 13–15 and 24 manifested significant antitumor activity.
Three new thiosemicarbazides (1 a‐c) were prepared from N‐[4‐phenyl‐5‐(2‐thienyl)‐1,2,4‐triazol‐3‐yl]mercaptoacetohydrazide. Reaction of (1 a‐c) with the appropriate phenacyl bromide afforded thiazoline derivatives (2 a‐i) whereas their reaction with chloroacetic acid or maleic anhydride gave the corresponding thiazolidine derivatives (3 a,b) and (4 a,b). Cyclodesulfurization of (1 a‐c) with DCCD in toluene yielded 5‐substituted‐amino‐1,3,4‐oxadiazoles (5 a,b), while their dehydration with PPA gave the corresponding 5‐substituted‐amino‐1,3,4‐thiadiazoles (6 a‐c). Six representative compounds were tested for their in‐vitro antimicrobial activity against some pathogenic microorganisms, some of them were proved to be active.
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