Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach

Bioorganic and Medicinal Chemistry

Volumn 20, Issue 23, 2012, Pages 6795-6802

  Zhan, Peng ^a   Chen, Wenmin ^a   Li, Zhenyu ^a   Li, Xiao ^a   Chen, Xuwang ^a   Tian, Ye ^a   Pannecouque, Christophe ^b   Clercq, Erik De ^b   Liu, Xinyong ^a  

^a SHANDONG UNIVERSITY   (China)

^b REGA INSTITUTE FOR MEDICAL RESEARCH   (Belgium)

Author keywords

Anti HIV 1 activity; Heterocycle; HIV reverse transcriptase; NNRTIs; Pyrazinylthioacetamide; SAR; Structure based bioisosterism strategy; Synthesis

Indexed keywords

2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO] 1 [3,4 DIHYDROISOQUINOLIN 2(1H) YL]ETHANONE; 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO] 1 [3,4 DIHYDROQUINOLIN 1(2H) YL]ETHANONE; 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO] N (2 CHLOROPYRIDIN 3 YL)ACETAMIDE; 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO] N (2 FLUOROPHENYL)ACETAMIDE; 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO] N (2 NITROPHENYL)ACETAMIDE; 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO] N (2,4 DICHLOROPHENYL)ACETAMIDE; 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO] N (4 METHYL 2 NITROPHENYL)ACETAMIDE; 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO] N (5 METHYLBENZO[D]THIOZOL 2 YL)ACETAMIDE; 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO] N ARYLACETAMIDE DERIVATIVE; 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO] N PHENYLACETAMIDE; ANTIVIRUS AGENT; ETHYL 3 BROMO 4 [2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO]ACETAMIDO]BENZOATE; HETEROCYCLIC COMPOUND; METHYL 3 [2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO]ACETAMIDO]THIOPHENE 2 CARBOXYLATE; METHYL 3 BROMO 4 [2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO]ACETAMIDO]BENZOATE; N (2 BROMO 4 CHLOROPHENYL) 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO]ACETAMIDE; N (2 BROMO 4 METHYLPHENYL) 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO]ACETAMIDE; N (2 BROMOPHENYL) 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO]ACETAMIDE; N (2 CHLOROPHENYL) 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO]ACETAMIDE; N (4 ACETYL 2 BROMOPHENYL) 2 [3 (2 CHLOROPHENYL)PYRAZIN 2 YLTHIO]ACETAMIDE; RNA DIRECTED DNA POLYMERASE INHIBITOR; UNCLASSIFIED DRUG;

ANTIVIRAL ACTIVITY; ARTICLE; DRUG DESIGN; DRUG IDENTIFICATION; DRUG POTENCY; DRUG RESEARCH; DRUG SYNTHESIS; HUMAN IMMUNODEFICIENCY VIRUS 1; IC 50; IN VITRO STUDY; MOLECULAR DOCKING; NONHUMAN; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS; WILD TYPE;

ANTI-HIV AGENTS; DRUG DESIGN; HIV INFECTIONS; HIV REVERSE TRANSCRIPTASE; HIV-1; HUMANS; MODELS, MOLECULAR; STRUCTURE-ACTIVITY RELATIONSHIP; THIOACETAMIDE;

HUMAN IMMUNODEFICIENCY VIRUS 1;

EID: 84869096159     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2012.09.058     Document Type: Article

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