POLYANION INHIBITORS OF HUMAN-IMMUNODEFICIENCY-VIRUS AND OTHER VIRUSES .1. POLYMERIZED ANIONIC SURFACTANTS

被引:20
作者
LEYDET, A
BARTHELEMY, P
BOYER, B
LAMATY, G
ROQUE, JP
BOUSSEAU, A
EVERS, M
HENIN, Y
SNOECK, R
ANDREI, G
IKEDA, S
REYMEN, D
DECLERCQ, E
机构
[1] UNIV MONTPELLIER 2, CHIM PHYS ORGAN LAB, F-34095 MONTPELLIER 05, FRANCE
[2] RHONE POULENC RORER, CTR RECH VITRY ALFORTVILLE, DEPT CHIM PHARMACEUT & BIOL, F-94403 Vitry Sur Seine, FRANCE
[3] KATHOLIEKE UNIV LEUVEN, REGA INST MED RES, B-3000 LOUVAIN, BELGIUM
关键词
D O I
10.1021/jm00013a019
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of polyanionic compounds was synthesized and evaluated for their activity against human immunodeficiency virus (HIV-1, HIV-2) and various other RNA and DNA viruses. Several compounds, i.e., 2p, 3p, 8p, 13p, 14p, 15p, 17p, 18p, and 19p, proved active against HIV-I within the concentration range of 0.1-3 mu g/mL while not being toxic to the host cells (GEM, MT-4) at concentrations up to 100 mu g/mL or higher. As a rule, these polyanionic compounds proved also active, albeit at somewhat higher concentrations than those required for HIV-1 inhibition, against a number of other enveloped viruses, including HIV-2, human cytomegalovirus, influenza A virus, respiratory syncytial virus, and arenaviruses (Junin and Tacaribe). Among the most potent HIV-1 inhibitors ranked compounds 18p and 19p, the sodium salts of N-methylamides obtained by polymerization of monomers prepared starting from 10-undecenoyl chloride and omega-aminoalkanoic acids.
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收藏
页码:2433 / 2440
页数:8
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