Roggo B E, Petersen F, Sills M, Roesel J L, Moerker T, Peter H H
Core Drug Discovery Technologies, Pharmaceutical Division, Ciba-Geigy Limited, Basel, Switzerland.
J Antibiot (Tokyo). 1996 Jan;49(1):13-9. doi: 10.7164/antibiotics.49.13.
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.
从两种不同的葡萄穗霉属菌种培养物中分离出六种新型螺二氢苯并呋喃内酰胺I - VI（1 - 6）以及一种相关的螺二氢苯并呋喃醇，即先前描述的天然化合物L-671,776（7）。这些次生代谢产物在内皮素受体结合试验中显示出拮抗作用，并能抑制HIV-1蛋白酶。这两种生物活性对于L-671,776（7）来说都是新发现的。假对称螺二氢苯并呋喃内酰胺VI（6）是这类化合物中最有效的代表，在ET-A受体结合试验中的IC50值为1.5微摩尔，在HIV-1蛋白酶抑制试验中的IC50值为11微摩尔。
