Chinese Journal of Organic Chemistry >
Synthesis and Antimicrobial Activity of 1,5-Benzothiazepines Incorporated with Triazole Moiety
Received date: 2020-12-27
Revised date: 2021-02-09
Online published: 2021-03-12
Supported by
Natural Science Foundation of Hebei Province(B2017205100); Graduate Student Innovation Fundation of Hebei Normal University(CXZZSS2021052)
Four kinds of 1,5-benzothiazepines incorporated with triazole moiety: 2,3/2,5-dihydro-3-[(1H-1,2,4-triazol-1-yl) methyl]-4-aryl-1,5-benzothiazepines (9a~9f,10a~10f) and 2,3/2,5-dihydro-3-[(2H-1,2,3-triazol-2-yl)methyl]-4-aryl-1,5- benzothiazepines (17a~17f, 18a~18f) were designed and synthesized. It was found that the isomerization of triazole occurred during the conversion of 15a~15f to the target compounds. Two new compounds 19a and 20a were isolated and their possible formation mechanism was proposed. The antimicrobial activity test of the target products showed that compounds 9a~9d and 10a~10d had moderate to high inhibitory effect on fungi, and compounds 9b, 9c, and 10b showed higher inhibition on C. neoformans than that of fluconazole, which can be used for further investigation for the development of antifungal drugs.
Key words： triazole; 1; 5-benzothiazepine; antimicrobial activity
Yujia Sun , Ziwei Wang , Yan Wang , Tongxiu Xu , Keqing Tian , Ping Zhang . Synthesis and Antimicrobial Activity of 1,5-Benzothiazepines Incorporated with Triazole Moiety[J]. Chinese Journal of Organic Chemistry, 2021 , 41(6) : 2361 -2373 . DOI: 10.6023/cjoc202012044
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