Benzomalvins, new substance P inhibitors from a Penicillium sp

Article abstract of DOI:10.7164/antibiotics.47.515

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 μM 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.