Structure and absolute stereochemistry of HIV-1 integrase inhibitor integric acid.: A novel eremophilane sesquiterpenoid produced by a Xylaria sp.

被引：83

作者：

Singh, SB

Zink, D

Polishook, J

Valentino, D

Shafiee, A

Silverman, K

Felock, P

Teran, A

Vilella, D

Hazuda, DJ

Lingham, RB

机构：

[1] Merck Res Labs, Nat Prod Drug Discovery, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Antiviral Res, West Point, PA 19486 USA

[3] Labs Merck Sharp & Dohme Espana SA, Ctr Invest Basica, Nat Prod Drug Discovery, Madrid 28027, Spain

来源：

TETRAHEDRON LETTERS | 1999年 / 40卷 / 50期

关键词：

D O I：

10.1016/S0040-4039(99)01878-X

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

HIV-1 integrase is critical for viral replication and is absent in the host, and therefore is a potential target for the development of non-toxic antiviral therapy. From the screening of natural product libraries we have discovered integric acid, a novel eremophilane sesquiterpenoid, from a Xylaria sp. It inhibited 3'-end processing, strand transfer and disintegration reactions catalyzed by HIV-1 integrase with IC50 values of 3-10 mu M. The isolation, structure elucidation, relative, and absolute stereochemistry of integric acid are described. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：8775 / 8779

页数：5

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