Design and synthesis of HIV-1 protease inhibitors. Novel tetrahydrofuran P2/P2'-groups interacting with Asp29/30 of the HIV-1 protease. Determination of binding from X-ray crystal structure of inhibitor protease complex.

Oscarsson K; Lahmann M; Lindberg JKangasmetsa JUnge TOscarson SHallberg ASamuelsson B

首页> 外文期刊>Bioorganic and medicinal chemistry >Design and synthesis of HIV-1 protease inhibitors. Novel tetrahydrofuran P2/P2'-groups interacting with Asp29/30 of the HIV-1 protease. Determination of binding from X-ray crystal structure of inhibitor protease complex.

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Design and synthesis of HIV-1 protease inhibitors. Novel tetrahydrofuran P2/P2'-groups interacting with Asp29/30 of the HIV-1 protease. Determination of binding from X-ray crystal structure of inhibitor protease complex.

机译：Design and synthesis of HIV-1 protease inhibitors. Novel tetrahydrofuran P2/P2'-groups interacting with Asp29/30 of the HIV-1 protease. Determination of binding from X-ray crystal structure of inhibitor protease complex.

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摘要

A series of HIV-1 protease inhibitors having new tetrahydrofuran P2/P2' groups have been synthesised and tested for protease inhibition and antiviral activity. Six novel 4-aminotetrahydrofuran derivatives were prepared starting from commercially available isopropylidene-alpha-D-xylofuranose yielding six symmetrical and six unsymmetrical inhibitors. Promising sub nanomolar HIV-1 protease inhibitory activities were obtained. The X-ray crystal structure of the most potent inhibitor (23, K(i) 0.25 nM) co-crystallised with HIV-1 protease is discussed and the binding compared with inhibitors 1a and 1b.

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来源
《Bioorganic and medicinal chemistry》 |2003年第6期|1107-1115|共9页
作者
Oscarsson K; Lahmann M; Lindberg JKangasmetsa JUnge TOscarson SHallberg ASamuelsson B;
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作者单位

Department of Organic Chemistry, Arrhenius Laboratory, Floor 6, Stockholm University, S-106 91, Stockholm, Sweden;

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正文语种英语
中图分类药学;生物化学;
关键词
HIV-1; Endopeptidases; Protease Inhibitors; structure; binding; 蛋白酶抑制药;

Design and synthesis of HIV-1 protease inhibitors. Novel tetrahydrofuran P2/P2'-groups interacting with Asp29/30 of the HIV-1 protease. Determination of binding from X-ray crystal structure of inhibitor protease complex.

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