Linker-modified quinoline derivatives targeting HIV-1 integrase: synthesis and biological activity
A series of quinoline derivatives linked to an aromatic ring by functionalized spacers was synthesized. The anti-HIV-1 integrase potency was evaluated in both in vitro and ex vivo assays. A novel series of HIV-1 integrase inhibitors was synthesized and tested in both in vitro and ex vivo assays. The...
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Published in | Bioorganic & medicinal chemistry letters Vol. 14; no. 10; pp. 2473 - 2476 |
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Main Authors | , , , , , , , , , , , |
Format | Journal Article |
Language | English |
Published |
Oxford
Elsevier Ltd
17.05.2004
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | A series of quinoline derivatives linked to an aromatic ring by functionalized spacers was synthesized. The anti-HIV-1 integrase potency was evaluated in both in vitro and ex vivo assays.
A novel series of HIV-1 integrase inhibitors was synthesized and tested in both in vitro and ex vivo assays. These inhibitors are featured by the presence of a quinoline subunit and an ancillary aromatic ring linked by functionalized spacers such as amide, hydrazide, urea and 1-hydroxyprop-1-en-3-one moiety. Amide derivatives are the most promising ones and could serve as leads for further developments. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2004.03.005 |