Journal of Antibiotics 1994-05-01

Benzomalvins, new substance P inhibitors from a Penicillium sp.

H H Sun, C J Barrow, D M Sedlock, A M Gillum, R Cooper

Index: J. Antibiot. 47(5) , 515-22, (1994)

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Abstract

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.