PMID: 7525984Dec 1, 1994Paper

Resistance pattern of human immunodeficiency virus type 1 reverse transcriptase to quinoxaline S-2720

Journal of Virology
Jan BalzariniJ P Kleim

Abstract

The human immunodeficiency virus type 1 (HIV-1)-specific reverse transcriptase (RT) inhibitor quinoxaline S-2720 showed a more-potent inhibitory effect on HIV-1-induced cytopathicity in CEM cells than either nevirapine, pyridinone L-697,661, bis-heteroarylpiperazine (BHAP) U-88204, TSAO ([2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5 "- (4-amino-1",2"-oxathiole-2",2"-dioxide)-N3-ethylthymine, or 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk][1,4-benzodiazepin-2(I H)-one (TIBO) R82913. The quinoxaline derivative was also markedly more inhibitory to the mutant HIV-1 strains containing in their RT Ile-100, Asn-103, Ala-106, Lys-138, Cys-181, or His-188 substitutions than were the other HIV-1-specific RT inhibitors. Moreover, quinoxaline S-2720 totally prevented HIV-1 infection and emergence of drug-resistant mutant virus strains in CEM cell cultures at concentrations (i.e., 0.35 microM) that are 10- to 25-fold lower than those required for BHAP U-88204 and nevirapine to knock out the virus. Also, the concentration-response curve for S-2720 was markedly steeper than for BHAP and nevirapine, as reflected by the ratio of the 95% to the 50% antivirally effective concentration. Lower concentrations of quinoxaline...Continue Reading

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Citations

May 21, 2011·Organic & Biomolecular Chemistry·Victoria A VaillardSandra E Martín
Jan 13, 2011·Journal of Enzyme Inhibition and Medicinal Chemistry·Yusuf M Al-HiariMustafa M El-Abadelah
Apr 16, 2013·Organic & Biomolecular Chemistry·Etienne BrachetMouâd Alami
Jan 2, 2020·European Journal of Medicinal Chemistry·Lucas FabianAlbertina Moglioni
Sep 10, 2009·Chemical Reviews·Marcos A P MartinsPablo Machado
Jan 1, 1996·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·E De Clercq
Oct 23, 1997·Clinical Microbiology Reviews·E De Clercq
Aug 14, 2010·Organic Letters·Xuehong LuoMirosław J Tomaszewski
Apr 14, 2017·The Journal of Organic Chemistry·Abhishek GuptaNidhi Jain

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