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N3-(4-甲氧基富马酰基)-L-2,3-二氨基丙酸寡肽的抗念珠菌特性

Anticandidal properties of N3-(4-methoxyfumaroyl)-L-2,3-diaminopropanoic acid oligopeptides.

作者信息

Andruszkiewicz R, Milewski S, Zieniawa T, Borowski E

机构信息

Department of Pharmaceutical Technology and Biochemistry, Technical University of Gdansk, Poland.

出版信息

J Med Chem. 1990 Jan;33(1):132-5. doi: 10.1021/jm00163a022.

Abstract

Tri-, tetra-, and pentapeptides containing N3-(4-methoxyfumaroyl)-L-2,3-diaminopropanoic acid (FMDP), an inactivator of glucosamine 6-phosphate synthase of fungal origin (a key enzyme in the biosynthesis of macromolecular components of the fungal cell wall) have been synthesized and investigated as anticandidal agents. Structure-activity relationships of a series of peptides revealed that tripeptides were generally more active than the other peptides examined. In this study, the lysyl peptide, Lys-Nva-FMDP has been found to be the most active compound in the series.

摘要

含有N3-(4-甲氧基富马酰基)-L-2,3-二氨基丙酸(FMDP)的三肽、四肽和五肽已被合成并作为抗念珠菌剂进行研究。FMDP是一种源自真菌的葡糖胺6-磷酸合酶(真菌细胞壁大分子成分生物合成中的关键酶)的灭活剂。一系列肽的构效关系表明,三肽通常比所研究的其他肽更具活性。在本研究中,赖氨酰肽Lys-Nva-FMDP被发现是该系列中活性最高的化合物。

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