Pharmacophore and structure-activity relationships of integrase inhibition within a dual inhibitor scaffold of HIV reverse transcriptase and integrase

Bioorganic and Medicinal Chemistry

Volumn 18, Issue 12, 2010, Pages 4202-4211

  Wang, Zhengqiang ^a   Tang, Jing ^a   Salomon, Christine E ^a   Dreis, Christine D ^a   Vince, Robert ^a  

^a UNIVERSITY OF MINNESOTA   (United States)

Author keywords

Diketoacid; HIV; Integrase; Pharmacophore; SAR

Indexed keywords

4 [3 [4 [(4 BENZYL 5 ETHYL 6 OXO 1,6 DIHYDROPYRIMIDIN 2 YLTHIO)METHYL]BENZYL]PHENYL] 2 HYDROXY 4 OXOBUT 2 ENOIC ACID; 4 [3 [4 [[[6 (3,5 DIMETHYLBENZYL) 5 ETHYL 2,4 DIOXO 3,4 DIHYDROPYRIMIDIN 1 (2H) YL]METHOXY]METHYL]BENZYL]PHENYL] 2 HYDROXY 4 OXOBUT 2 ENOIC ACID; 4 [3 [4 [[[6 (3,5 DIMETHYLBENZYL) 5 ISOPROPYL 2,4 DIOXO 3,4 DIHYDROPYRIMIDIN 1 (2H)YL]METHOXY]METHYL]BENZYL]PHENYL] 2 HYDROXY 4 OXOBUT 2 ENOIC ACID; 4 [3 [4 [[[6 BENZYL 5 ETHYL 2,4 DIOXO 3,4 DIHYDROPYRIMIDIN 1 (2H) YL]METHOXY]METHYL]BENZYL]PHENYL] 2 HYDROXY 4 OXOBUT 2 ENOIC ACID; 4 [3 [4 [[[6 BENZYL 5 ISOPROPYL 2,4 DIOXO 3,4 DIHYDROPYRIMIDIN 1 (2H)YL]METHOXY]METHYL]BENZYL]PHENYL] 2 HYDROXY 4 OXOBUT 2 ENOIC ACID; 4 [4 [2 [4 BENZYL 5 ISOPROPYL 2,6 DIOXO 2,3 DIHYDROPYRIMIDIN 1 (6H)YL]ETHYL]PHENYL] 2 HYDROXY 4 OXOBUT 2 ENOIC ACID; 4 [4 [2 [[6 BENZYL 5 ISOPROPYL 2,4 DIOXO 3,4 DIHYDROPYRIMIDIN 1 (2H) YL]METHOXY]ETHYL]PHENYL] 2 HYDROXY 4 OXOBUT 2 ENOIC ACID; 4 [4 [3 [[6 BENZYL 5 ISOPROPYL 2,4 DIOXO 3,4 DIHYDROPYRIMIDIN 1 (2H) YL]METHOX]PROPYL]PHENYL] 2 HYDROXY 4 OXO BUT 2 ENOIC ACID; 4 [4 [4 [4 BENZYL 5 ISOPROPYL 2,6 DIOXO 2,3 DIHYDROPYRIMIDIN 1 (6H)YL]BUTYL]PHENYL] 2 HYDROXY 4 OXOBUT 2 ENOIC ACID; 4 [4 [6 [4 BENZYL 5 ISOPROPYL 2,6 DIOXO 2,3 DIHYDROPYRIMIDIN 1 (6H)YL]HEXYL]PHENYL] 2 HYDROXY 4 OXOBUT 2 ENOIC ACID; 4 [4 [[4 BENZYL 5 ETHYL 6 OXO 1,6 DIHYDROPYRIMIDIN 2 YLTHIO]METHYL]PHENYL] 2 HYDROXY 4 OXOBUT 2 ENOIC ACID; INTEGRASE INHIBITOR; RNA DIRECTED DNA POLYMERASE INHIBITOR; UNCLASSIFIED DRUG; ZIDOVUDINE; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; HETEROCYCLIC COMPOUND; INTEGRASE; RNA DIRECTED DNA POLYMERASE;

ANTIVIRAL ACTIVITY; ARTICLE; CELL ASSAY; CELL PROTECTION; CONTROLLED STUDY; DRUG CYTOTOXICITY; DRUG DESIGN; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN IMMUNODEFICIENCY VIRUS 1; IC 50; NONHUMAN; PHARMACOPHORE; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; VIRUS INHIBITION; ANTAGONISTS AND INHIBITORS; CHEMISTRY; HUMAN; METABOLISM; STEREOISOMERISM; SYNTHESIS;

ANTI-HIV AGENTS; DRUG DESIGN; HETEROCYCLIC COMPOUNDS; HIV INTEGRASE; HIV INTEGRASE INHIBITORS; HIV REVERSE TRANSCRIPTASE; HUMANS; REVERSE TRANSCRIPTASE INHIBITORS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

HUMAN IMMUNODEFICIENCY VIRUS;

EID: 77953127859     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2010.05.004     Document Type: Article

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