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Synthesis and Structure-Activity Relationships of Novel Neocryptolepine Derivatives

Synthesis and Structure-Activity Relationships of Novel Neocryptolepine Derivatives
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摘要 Herein we reported the synthesis of a novel series of neocryptolepine(5-methyl-5H-indolo[2,3-b]quinoline) derivatives containing different substituents at Cll using methyl 1H-indole-3-carboxylate and N-methylaniline as starting material. The target 21 compounds were evaluated for their axltibacterial activity in vitro against gram-positive bacteria(B, subtilis and S. aureus) and gram-negative bacteria(E, coli and S.typhi). Almost all the tested compounds showed moderate to high activities against the four bacterial strains at the minimum inhibitory concentrations(MICs) of 1-10μg/mL. The obtained results suggest that part of the novel synthetic neocryptolepine derivatives exhibit significant antibacterial effect against all the tested organisms. Herein we reported the synthesis of a novel series of neocryptolepine(5-methyl-5H-indolo[2,3-b]quinoline) derivatives containing different substituents at Cll using methyl 1H-indole-3-carboxylate and N-methylaniline as starting material. The target 21 compounds were evaluated for their axltibacterial activity in vitro against gram-positive bacteria(B, subtilis and S. aureus) and gram-negative bacteria(E, coli and S.typhi). Almost all the tested compounds showed moderate to high activities against the four bacterial strains at the minimum inhibitory concentrations(MICs) of 1-10μg/mL. The obtained results suggest that part of the novel synthetic neocryptolepine derivatives exhibit significant antibacterial effect against all the tested organisms.
出处 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2017年第3期373-377,共5页 高等学校化学研究(英文版)
关键词 Neocryptolepine Indoloquinolme ANTIBACTERIAL Neocryptolepine Indoloquinolme Antibacterial
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