Chinese Journal of Organic Chemistry >
Synthesis and Antimicrobial Activity of C(3)-1,2,4-Triazolyl-1,5-benzothiazepines
Received date: 2019-01-25
Revised date: 2019-04-01
Online published: 2019-05-06
Supported by
Project supported by the Natural Science Foundation of Hebei Province (No. B2017205100) and the Graduate Student Innovation Fundation of Hebei Normal University (No. CXZZSS201804).
Three kinds of C(3)-1,2,4-triazolyl-1,5-benzothiazepines, 2,3-dihydro/2,5-dihydro/2,3,4,5-tetrahydro-3-(1,2,4-tria-zolyl)-4-aryl-1,5-benzothiazepines, were designed and synthesized. The synthesis conditions of intermediates and target products were studied, and the structures of two by-products were determined. The antimicrobial activity test of the target products showed that 2,3-dihydro/2,5-dihydro-3-(1,2,4-triazolyl)-4-aryl-1,5-benzothiazepines exhibited high inhibitory effects on C. neoformans and C. albicans. At concentration of 200 μg/disc, the inhibitory effects of four compounds on C. neoformans were stronger than that of fluconazol, and the inhibitory effects of three compounds on C. albicans were stronger than that of fluconazol. The preliminary study on the structure-activity relationship of antifungal revealed that 1,2,4-triazolyl and C=N double bond were the key function groups in the antifungal activity of 2,3-dihydro-3-(1,2,4-triazolyl)-4-aryl-1,5-benzothiazepines.
Wang Yan , Kong Lingman , Wang Ranran , Tian Keqing , Zhang Ping . Synthesis and Antimicrobial Activity of C(3)-1,2,4-Triazolyl-1,5-benzothiazepines[J]. Chinese Journal of Organic Chemistry, 2019 , 39(9) : 2663 -2670 . DOI: 10.6023/cjoc201901041
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