Novel Spirodihydrobenzofuranlactams as Antagonists of Endothelin and as Inhibitors of HIV-1 Protease Produced by Stachybotrys sp. I. Fermentation, Isolation and Biological Activity

BARBARA E. ROGGO; FRANK PETERSEN; MATTHEW SILLS; JOHANNES L. ROESEL; THÉOPHILE MOERKER; HEINRICH H. PETER

doi:10.7164/antibiotics.49.13

Novel Spirodihydrobenzofuranlactams as Antagonists of Endothelin and as Inhibitors of HIV-1 Protease Produced by Stachybotrys sp.

I. Fermentation, Isolation and Biological Activity

BARBARA E. ROGGO, FRANK PETERSEN, MATTHEW SILLS, JOHANNES L. ROESEL, THÉOPHILE MOERKER, HEINRICH H. PETER

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JOURNAL FREE ACCESS

1996 Volume 49 Issue 1 Pages 13-19

DOI https://doi.org/10.7164/antibiotics.49.13

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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 μm in the ET-A receptor binding assay and 11 μM in the HIV-1 protease inhibition assay.

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