Leydet A, Barthelemy P, Boyer B, Lamaty G, Roque J P, Bousseau A, Evers M, Hénin Y, Snoeck R, Andrei G
Laboratoire de Chimie Organique Physique, Université Montpellier II, France.
J Med Chem. 1995 Jun 23;38(13):2433-40. doi: 10.1021/jm00013a019.
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-1 within the concentration range of 0.1-3 micrograms/mL while not being toxic to the host cells (CEM, MT-4) at concentrations up to 100 micrograms/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.
合成了一系列聚阴离子化合物,并评估了它们对人类免疫缺陷病毒(HIV-1、HIV-2)以及各种其他RNA和DNA病毒的活性。几种化合物,即2p、3p、8p、13p、14p、15p、17p、18p和19p,在0.1 - 3微克/毫升的浓度范围内对HIV-1具有活性,而在浓度高达100微克/毫升或更高时对宿主细胞(CEM、MT-4)无毒。通常,这些聚阴离子化合物对许多其他包膜病毒也具有活性,尽管其活性所需浓度略高于抑制HIV-1所需的浓度,这些病毒包括HIV-2、人类巨细胞病毒、甲型流感病毒、呼吸道合胞病毒和沙粒病毒(胡宁病毒和塔卡里伯病毒)。在最有效的HIV-1抑制剂中,化合物18p和19p排名靠前,它们是由10-十一碳烯酰氯和ω-氨基链烷酸制备的单体聚合得到的N-甲基酰胺的钠盐。