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Jan 2018 European journal of medicinal chemistry

Synthesis and biological evaluation of some novel diastereoselective benzothiazole β-lactam conjugates.

Auteurs

Alborz M, Jarrahpour A, Pournejati R, Karbalaei-Heidari HR, Sinou V, Latour C, Sharghi H, Aberi M, Turos E, Wojtas L

Résumé

Highly diastereoselective synthesis of some novel benzothiazole-substituted β-lactam hybrids was achieved starting from (benzo[d]thiazol-2-yl)phenol as an available precursor. This is the first time (benzo[d]thiazol-2-yl)phenoxyacetic acid has been used as ketene source in synthesizing monocyclic 2-azetidinones. These compounds were evaluated for their antimicrobial activities against a large panel of Gram-positive and Gram-negative bacterial strains and moderate activities were encountered. Antimalarial data revealed that adding methoxyphenyl or ethoxyphenyl group on the β-lactam ring makes compounds that are more potent. Moreover, hemolytic activity and mammalian cell toxicity survey of the compounds showed their potential as a medicine.

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