National Institutes of Health, a Component of the US Dept. of Health & Human Services

Barry Johnson

Yves Pommier

Terrence R Burke, Jr

Stephen H Hughes

Christophe Marchand

Xue Zhi Zhao

Steven Smith

Mathieu Metifiot

A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is N, C(OH), or CH;Y is H or OH;each of Z-Zis independently H or halogen;Ris H, OH, NH, NHR, NRRor R;R, R, and Ris each independently H, halogen, OR, R, NHR, NRR, COR, CONRR, SONRR, or Rand Rtogether with the carbon atoms to which Rand Rare attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; andRand Ris each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or Rand Rtogether with the nitrogen to which Rand Rare attached form an optionally-substituted heterocycle.

Compounds for inhibiting drug-resistant strains of HIV-1 integrase

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Chincoteague, VA, United States of America

Barry Johnson