| Literature DB >> 8676342 |
F Soler1, C Poujade, M Evers, J C Carry, Y Hénin, A Bousseau, T Huet, R Pauwels, E De Clercq, J F Mayaux, J B Le Pecq, N Dereu.
Abstract
A novel series of omega-aminoalkanoic acid derivatives of betulinic acid were synthesized and evaluated for their activity against human immunodeficiency virus (HIV). The anti-HIV-1 activity of several members of this new series was found to be in the nanomolar range in CEM 4 and MT-4 cell cultures. The optimization of the omega-aminoalkanoic acid side chain is described. The presence of an amide function within the side chain was found important for optimal activity. RPR 103611 (14g), a statine derivative, was found to be inactive against HIV-1 protease, reverse transcriptase, and integrase as well as on gp120/CD4 binding. "Time of addition" experiments suggested interaction with an early step of HIV-1 replication. As syncytium formation, but not virus-cell binding, seems to be affected, betulinic acid derivatives are assumed to interact with the postbinding virus-cell fusion process.Entities:
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Year: 1996 PMID： 8676342 DOI： 10.1021/jm950669u
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446