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与吲哚部分偶联的五元环杂环的合成及抗菌活性

Syntheses and antimicrobial activities of five-membered ring heterocycles coupled to indole moieties.

作者信息

Pereira E R, Sancelme M, Towa J J, Prudhomme M, Martre A M, Mousset G, Rapp M

机构信息

Université Blaise Pascal, Laboratoire de Chimie Organique Biologique, Aubière, France.

出版信息

J Antibiot (Tokyo). 1996 Apr;49(4):380-5. doi: 10.7164/antibiotics.49.380.

Abstract

Indole-substituted oxazolidinones, oxazolones, pyrrolidinone, imidazolidinone and imidazolones were synthesized. Their inhibitory potencies towards protein kinase C and protein kinase A were determined and their in vitro activities against Streptomyces chartreusis, Streptomyces griseus, Bacillus cereus, Candida albicans and Escherichia coli were examined. The inhibition of Streptomyces sporulation observed for some of them could not be linked to in vitro protein kinase C inhibition. All proved inactive against C. albicans but three of them exhibited a marked activity towards E. coli. This effect extends to other Gram-negative bacteria.

摘要

合成了吲哚取代的恶唑烷酮、恶唑酮、吡咯烷酮、咪唑烷酮和咪唑酮。测定了它们对蛋白激酶C和蛋白激酶A的抑制效力,并检测了它们对浅绿链霉菌、灰色链霉菌、蜡状芽孢杆菌、白色念珠菌和大肠杆菌的体外活性。观察到其中一些化合物对链霉菌孢子形成的抑制作用与体外蛋白激酶C抑制作用无关。所有化合物对白色念珠菌均无活性,但其中三种对大肠杆菌表现出显著活性。这种作用扩展到其他革兰氏阴性菌。

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