Discovery of a novel 5-carbonyl-1H-imidazole-4-carboxamide class of inhibitors of the HIV-1 integrase-LEDGF/p75 interaction

Bioorganic and Medicinal Chemistry

Volumn 21, Issue 19, 2013, Pages 5963-5972

  Serrao, Erik ^a,d   Xu, Zhong Liang ^b   Debnath, Bikash ^a,e   Christ, Frauke ^c   Debyser, Zeger ^c   Long, Ya Qiu ^b   Neamati, Nouri ^a  

^a UNIVERSITY OF SOUTHERN CALIFORNIA   (United States)

^b SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

^c DEPARTMENT OF PHARMACEUTICAL AND PHARMACOLOGICAL SCIENCES   (Belgium)

^d DANA FARBER CANCER INSTITUTE   (United States)

^e UNIVERSITY OF MICHIGAN   (United States)

Author keywords

Antiviral; HIV 1; Integrase; LEDGF p75 5 carbonyl 1H Imidazole 4 carboxamide; Protein protein interaction

Indexed keywords

4 (PHENYLCARBAMOYL) 1H IMIDAZOLE 5 CARBOXYLIC ACID; 4 (PYRIDIN 2 YLCARBAMOYL) 1H IMIDAZOLE 5 CARBOXYLIC ACID; 4 [(4 AMINOPHENYL)CARBAMOYL] 1H IMIDAZOLE 5 CARBOXYLIC ACID; 4 [(4 FLUOROBENZYL)CARBAMOYL] 1H IMIDAZOLE 5 CARBOXYLIC ACID; 4 [(4 NITROPHENYL)CARBAMOYL] 1H IMIDAZOLE 5 CARBOXYLIC ACID; 5 (4 HYDROXYPIPERIDINE 1 CARBONYL) N (PYRIDIN 2 YL) 1H IMIDAZOLE 4 CARBOXAMIDE; 5 (PIPERAZINE 1 CARBONYL) N (PYRIDIN 2 YL) 1H IMIDAZOLE 4 CARBOXAMIDE; 5 CARBONYL 1H IMIDAZOLE 4 CARBOXAMIDE DERIVATIVE; 5 FORMYL 1H IMIDAZOLE 4 CARBOXAMIDE DERIVATIVE; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; DIPHENYL 5,10 DIOXO 5,10 DIHYDRODIIMIDAZO[1,5-A:1',5'-D]PYRAZINE 1,6 DICARBOXYLATE; HIV 1 INTEGRASE; INTEGRASE; INTEGRASE INHIBITOR; LENS EPITHELIUM DERIVED GROWTH FACTOR; N (2 HYDROXYPHENYL) 5 (MORPHOLINE 4 CARBONYL) 1H IMIDAZOLE 4 CARBOXAMIDE; N (2 HYDROXYPHENYL) 5 (PIPERIZINE 1 CARBONYL) 1H IMIDAZOLE 4 CARBOXAMIDE; PHENYL 4 (4 TOLYLCARBAMOYL) 1H IMIDAZOLE 5 CARBOXYLATE; PHENYL 4 [[2 (BENZYLOXY)PHENYL]CARBAMOYL] 1H IMIDAZOLE 5 CARBOXYLATE; PROTEIN P75; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; DRUG DESIGN; DRUG IDENTIFICATION; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HIGH THROUGHPUT SCREENING; HUMAN IMMUNODEFICIENCY VIRUS 1; PROTEIN PROTEIN INTERACTION; STRUCTURE ACTIVITY RELATION;

HUMAN IMMUNODEFICIENCY VIRUS 1;

2B4J; 5-CARBONYL-1H-IMIDAZOLE-4-CARBOXAMIDE; 50% CYTOTOXIC CONCENTRATION; 50% EFFECTIVE CONCENTRATION; 50% INHIBITORY CONCENTRATION; ANTIVIRAL; CC(50); CCID(50); CELL CULTURE INFECTIVE DOSE; EC(50); HBA; HBD; HIV-1; HIV-1 INTEGRASE; HYDROGEN BOND ACCEPTOR; HYDROGEN BOND DONOR; IC(50); IN; INTEGRASE; LEDGF/P75; LENS EPITHELIUM-DERIVED GROWTH FACTOR/P75; PROTEIN-PROTEIN INTERACTION;

AMINOIMIDAZOLE CARBOXAMIDE; BINDING SITES; CELLS, CULTURED; DRUG DISCOVERY; ENZYME ACTIVATION; HIV INTEGRASE INHIBITORS; HUMANS; INHIBITORY CONCENTRATION 50; INTERCELLULAR SIGNALING PEPTIDES AND PROTEINS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN BINDING; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84883457183     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2013.07.047     Document Type: Article

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