Hydroxyl may not be indispensable for raltegravir: Design, synthesis and SAR Studies of raltegravir derivatives as HIV-1 inhibitors

European Journal of Medicinal Chemistry

Volumn 50, Issue , 2012, Pages 361-369

  Wang, Ziwen ^a   Wang, Mingxiao ^a   Yao, Xue ^a   Li, Yue ^a   Qiao, Wentao ^a   Geng, Yunqi ^a   Liu, Yuxiu ^a   Wang, Qingmin ^a  

^a NANKAI UNIVERSITY   (China)

Author keywords

5 Hydroxyl modification; Anti HIV activity; High throughput cell based assay method; Pseudotyped virus stocks; Raltegravir derivatives; Subpicomole IC 50 value

Indexed keywords

2 (2 (2 (DIETHYLAMINO) 2 OXOACETAMIDO)PROPAN 2 YL) 4 (4 FLUOROBENZYLCARBAMOYL) 1 METHYL 6 OXO 1,6 DIHYDROPYRIMIDIN 5 YL 2,4,6 TRIMETHYLBENZENESULFONATE; 2 (2 (2 (DIETHYLAMINO) 2 OXOACETAMIDO)PROPAN 2 YL) 4 (4 FLUOROBENZYLCARBAMOYL) 1 METHYL 6 OXO 1,6 DIHYDROPYRIMIDIN 5 YL ACETATE; 2 (2 (2 (DIETHYLAMINO) 2 OXOACETAMIDO)PROPAN 2 YL) 4 (4 FLUOROBENZYLCARBAMOYL) 1 METHYL 6 OXO 1,6 DIHYDROPYRIMIDIN 5 YL METHANESULFONATE; 2 (2 (2 (DIETHYLAMINO) 2 OXOACETAMIDO)PROPAN 2 YL) 4 (4 FLUOROBENZYLCARBAMOYL) 1 METHYL 6 OXO 1,6 DIHYDROPYRIMIDIN 5YL BENZOATE; 2 (2 (2 (DIETHYLAMINO) 2 OXOACETAMIDO)PROPAN 2 YL) 4 (4 FLUOROBENZYLCARBAMOYL) 6 METHOXYPYRIMIDIN 5 YL ACETATE; 2 (2 (2 (DIETHYLAMINO) 2 OXOACETAMIDO)PROPAN 2 YL) 4 (4 FLUOROBENZYLCARBAMOYL) 6 METHOXYPYRIMIDIN 5 YL METHANESULFONATE; 4 (4 FLUOROBENZYLCARBAMOYL) 1 METHYL 2 (2 (5 METHYL 1,3,4 OXADIAZOLE 2 CARBOXAMIDO)PROPAN 2 YL) 6 OXO 1,6 DIHYDROPYRIMIDIN 5 YL 2,4,6 TRIMETHYLBENZENESULFONATE; 4 (4 FLUOROBENZYLCARBAMOYL) 1 METHYL 2 (2 (5 METHYL 1,3,4 OXADIAZOLE 2 CARBOXAMIDO)PROPAN 2 YL) 6 OXO 1,6 DIHYDROPYRIMIDIN 5 YL ACETATE; 4 (4 FLUOROBENZYLCARBAMOYL) 1 METHYL 2 (2 (5 METHYL 1,3,4 OXADIAZOLE 2 CARBOXAMIDO)PROPAN 2 YL) 6 OXO 1,6 DIHYDROPYRIMIDIN 5 YL BENZOATE; 4 (4 FLUOROBENZYLCARBAMOYL) 1 METHYL 2 (2 (5 METHYL 1,3,4 OXADIAZOLE 2 CARBOXAMIDO)PROPAN 2 YL) 6 OXO 1,6 DIHYDROPYRIMIDIN 5 YL METHANESULFONATE; 4 (4 FLUOROBENZYLCARBAMOYL) 6 METHOXY 2 (2 (5 METHYL 1,3,4 OXADIAZOLE 2 CARBOXAMIDO)PROPAN 2 YL)PYRIMIDIN 5 YL 2,4,6 TRIMETHYLBENZENESULFONATE; 4 (4 FLUOROBENZYLCARBAMOYL) 6 METHOXY 2 (2 (5 METHYL 1,3,4 OXADIAZOLE 2 CARBOXAMIDO)PROPAN 2 YL)PYRIMIDIN 5 YL ACETATE; 4 (4 FLUOROBENZYLCARBAMOYL) 6 METHOXY 2 (2 (5 METHYL 1,3,4 OXADIAZOLE 2 CARBOXAMIDO)PROPAN 2 YL)PYRIMIDIN 5 YL BENZOATE; 4 (4 FLUOROBENZYLCARBAMOYL) 6 METHOXY 2 (2 (5 METHYL 1,3,4 OXADIAZOLE 2 CARBOXAMIDO)PROPAN 2 YL)PYRIMIDIN 5 YL METHANESULFONATE; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; HYDROXYL GROUP; METHYL 5 (BENZOYLOXY) 2 (2 (2 (DIETHYLAMINO) 2 OXOACETAMIDO)PROPAN 2 YL) 1 METHYL 6 OXO 1,6 DIHYDROPYRIMIDINE 4 CARBOXYLATE; METHYL 5 (BENZOYLOXY) 2 (2 (2 (DIETHYLAMINO) 2 OXOACETAMIDO)PROPAN 2 YL) 6 METHOXYPYRIMIDINE 4 CARBOXYLATE; N (2 (4 (4 FLUOROBENZYLAMINO) 6 (4 FLUOROBENZYLCARBAMOYL) 5 HYDROXYPYRIMIDIN 2 YL)PROPAN 2 YL) 5 METHYL 1,3,4 OXADIAZOLE 2 CARBOXAMIDE; N (2 (4 (4 FLUOROBENZYLCARBAMOYL) 5 HYDROXY 6 METHOXYPYRIMIDIN 2 YL)PROPAN 2 YL) 5 METHYL 1,3,4 OXADIAZOLE 2 CARBOXAMIDE; N1,N1 DIETHYL N2 (2 (4 (4 FLUOROBENZYLCARBAMOYL) 5 HYDROXY 1 METHYL 6 OXO 1,6 DIHYDROPYRIMIDIN 2 YL)PROPAN 2 YL)OXALAMIDE; N1,N1 DIETHYL N2 (2 (4 (4 FLUOROBENZYLCARBAMOYL) 5 HYDROXY 6 METHOXYPYRIMIDIN 2 YL)PROPAN 2 YL)OXALAMIDE; POTASSIUM 4 (4 FLUOROBENZYLCARBAMOYL) 6 METHOXY 2 (2 (5 METHYL 1,3,4 OXADIAZOLE 2 CARBOXAMIDO)PROPAN 2 YL)PYRIMIDIN 5 OLATE; RALTEGRAVIR; UNCLASSIFIED DRUG;

ANTIVIRAL ACTIVITY; ARTICLE; CELL LINE; CHEMICAL MODIFICATION; CYTOTOXICITY; DRUG DESIGN; DRUG SCREENING; DRUG SYNTHESIS; IC 50; STRUCTURE ACTIVITY RELATION;

ANTI-HIV AGENTS; BENZOATES; CELL PROLIFERATION; CELLS, CULTURED; DRUG DESIGN; HIV INFECTIONS; HIV-1; HUMANS; MOLECULAR STRUCTURE; OXADIAZOLES; PYRIMIDINONES; PYRROLIDINONES; REVERSE TRANSCRIPTASE INHIBITORS; STRUCTURE-ACTIVITY RELATIONSHIP; VIRUS REPLICATION;

EID: 84862778047     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2012.02.015     Document Type: Article

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