barrow-benzomalvinsnew-1994.pdf (466.37 kB)
Download file

Benzomalvins, new substance P inhibitors from a Penicillium sp.

Download (466.37 kB)
journal contribution
posted on 1994-05-01, 00:00 authored by H H Sun, Colin BarrowColin Barrow, D M Sedlock, A M Gillum, R Cooper
In the course of screening microbial broths for neurokinin receptor antagonists, a series of new benzodiazepines, benzomalvins A (1), B (2) and C (3), has been isolated from the culture broth of a fungus identified as a Penicillium sp. Benzomalvin A (1) showed inhibitory activity against substance P with Ki values of 12, 42 and 43 microM at the guinea pig, rat and human neurokinin NK1 receptors, respectively. Benzomalvins B (2) and C (3) were only weakly active. The structures of these compounds were determined by spectroscopic methods including MS measurements and NMR analysis.

History

Journal

Journal of antibiotics

Volume

47

Issue

5

Pagination

515 - 522

Publisher

Japan Antibiotics Research Association

Location

Tokyo, Japan

ISSN

0021-8820

eISSN

1881-1469

Language

eng

Publication classification

C1.1 Refereed article in a scholarly journal

Copyright notice

1994, Japan Antibiotics Research Association