Replacement of the metabolically labile methyl esters in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors with isoxazolone …
BL Deng, TL Hartman, RW Buckheit… - Journal of medicinal …, 2006 - ACS Publications
BL Deng, TL Hartman, RW Buckheit, C Pannecouque, E De Clercq, M Cushman
Journal of medicinal chemistry, 2006•ACS PublicationsThe alkenyldiarylmethanes (ADAMs) are a unique class of non-nucleoside reverse
transcriptase inhibitors that have potential value in the treatment of HIV/AIDS. However, the
potential usefulness of the ADAMs is limited by the presence of metabolically labile methyl
ester moieties. A series of novel ADAMs were therefore designed and synthesized in order
to replace the metabolically labile methyl ester moieties of the existing ADAM lead
compounds with hydrolytically stable, fused isoxazolone, isoxazole, oxazolone, or cyano …
transcriptase inhibitors that have potential value in the treatment of HIV/AIDS. However, the
potential usefulness of the ADAMs is limited by the presence of metabolically labile methyl
ester moieties. A series of novel ADAMs were therefore designed and synthesized in order
to replace the metabolically labile methyl ester moieties of the existing ADAM lead
compounds with hydrolytically stable, fused isoxazolone, isoxazole, oxazolone, or cyano …
The alkenyldiarylmethanes (ADAMs) are a unique class of non-nucleoside reverse transcriptase inhibitors that have potential value in the treatment of HIV/AIDS. However, the potential usefulness of the ADAMs is limited by the presence of metabolically labile methyl ester moieties. A series of novel ADAMs were therefore designed and synthesized in order to replace the metabolically labile methyl ester moieties of the existing ADAM lead compounds with hydrolytically stable, fused isoxazolone, isoxazole, oxazolone, or cyano substituents on the aromatic rings. The methyl ester and methoxy substituents on both of the aromatic rings in the parent compound 1 were successfully replaced with metabolically stable moieties with retention of anti-HIV activity and a general decrease in cytotoxicity.
ACS Publications
以上显示的是最相近的搜索结果。 查看全部搜索结果