CD4-MIMETIC INHIBITORS OF HIV-1 ENTRY AND METHODS OF USE THEREOF

Described herein are small-molecule mimics of CD4, which both enter the Phe43 cavity and target Asp368 of gp120, the HIV-1 envelope protein. Also described herein are methods of using these compounds to inhibit the transmission or progression of HIV infection. These compounds exhibit antiviral poten...

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Main Authors LE-KHAC MATTHEW, PRINCIOTTO AMY M, MASCOLA JOHN R, HENDRICKSON WAYNE A, SUN ALEXANDER W, SOETA TAKAHIRO, FREIRE EMESTO, COURTER JOEL R, JONES DAVID M, KOBAYASHI TOYOHARU, MADANI NAVID, LALONDE JUDITH M, KWONG PETER D, SMITH, III AMOS B, WU XUELING, KWON YOUNG DO, SCHON AME, SODROSKI JOSEPH
Format Patent
LanguageEnglish
Published 27.11.2014
Subjects
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary:Described herein are small-molecule mimics of CD4, which both enter the Phe43 cavity and target Asp368 of gp120, the HIV-1 envelope protein. Also described herein are methods of using these compounds to inhibit the transmission or progression of HIV infection. These compounds exhibit antiviral potency greater than that of a known antiviral, NBD-556, with 100% breadth against clade B and C viruses. Importantly, the compounds do not activate HIV infection of CD4-negative, CCR5-positive cells, in contrast to NBD-556.
Bibliography:Application Number: US201214365389