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Caffeoylglycolic and caffeoylamino acid derivatives, halfmers of L-chicoric acid, as new HIV-1 integrase inhibitors
- Issue Date
- Oct-2007
- Publisher
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
- Keywords
- human immunodeficiency virus; integrase inhibitor; L-chicoric acid; caffcoylglycolic acid; caffeoylamino acid
- Citation
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.42, no.10, pp 1309 - 1315
- Pages
- 7
- Journal Title
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 42
- Number
- 10
- Start Page
- 1309
- End Page
- 1315
- ISSN
- 0223-5234
1768-3254
- Abstract
- Human immunodeficiency virus (HIV) integrase (IN) catalyzes the integration of HIV DNA copy into the host cell DNA. L-Chicoric acid (1) has been found to be one of the most potent HIV-1 integrase inhibitor. Caffeoylglycolic and caffeoylamino acid derivatives' halfmeric structures Of L-chicoric acid 2 were synthesized for the purpose of simplifying the structure Of L-Chicoric acid. Among synthesized, compounds 2c and 3f showed HIV-1 IN inhibitory activities with IC50 values of 10.5 and 12.0 mu M, respectively, comparable to that of parent compound L-chicoric acid (IC50 = 15.7 mu M). (c) 2007 Elsevier Masson SAS. All fights reserved.
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