Novel spirodihydrobenzofuranlactams as antagonists of endothelin and as inhibitors of HIV-1 protease produced by Stachybotrys Sp. I. Fermentation, isolation and biological activity.

Important note: Information in this article was accurate in 1996. The state of the art may have changed since the publication date.

Novel spirodihydrobenzofuranlactams as antagonists of endothelin and as inhibitors of HIV-1 protease produced by Stachybotrys Sp. I. Fermentation, isolation and biological activity.

J Antibiot (Tokyo). 1996 Jan;49(1):13-9. Unique Identifier : AIDSLINE MED/96180343
Roggo BE; Petersen F; Sills M; Roesel JL; Moerker T; Peter HH; Core Drug Discovery Technologies, Pharmaceutical Division,; Ciba-Geigy Limited, Basel, Switzerland.

Abstract: Six novel spirodihydrobenzofuranlactams I - VI (1 - 6) and a related spirodihydrobenzofuranalcohol, the previously described natural compound L-671,776 (7), were isolated from cultures of two different Stachybotrys species. These secondary metabolites showed antagonistic effects in the endothelin receptor binding assay and inhibited HIV-1 protease. Both biological activities are novel for L-671,776 (7). The pseudosymmetric spirodihydrobenzofuranlactam VI (6) is the most potent representative of this class of compounds exhibiting IC50 values of 1.5 microM in the ET-A receptor binding assay and 11 microM in the HIV-1 protease inhibition assay.

Keywords: Animal Endothelins/*ANTAGONISTS & INHIB *Fermentation HIV Protease Inhibitors/*ISOLATION & PURIF/PHARMACOLOGY Lactams/*ISOLATION & PURIF/PHARMACOLOGY Rats Stachybotrys/*METABOLISM JOURNAL ARTICLE
960830
M9681197

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