2,4,5-Trisubstituted thiazole derivatives: A novel and potent class of non-nucleoside inhibitors of wild type and mutant HIV-1 reverse transcriptase

European Journal of Medicinal Chemistry

Volumn 85, Issue , 2014, Pages 27-42

  Xu, Zhongliang ^a   Ba, Mingyu ^b   Zhou, Hua ^a   Cao, Yingli ^b   Tang, Chaojun ^a   Yang, Ying ^b   He, Ricai ^a   Liang, Yu ^a   Zhang, Xuemei ^b   Li, Zhenzhong ^a   Zhu, Lihong ^a   Guo, Ying ^b   Guo, Changbin ^a  

^a CAPITAL NORMAL UNIVERSITY   (China)

^b PEKING UNION MEDICAL COLLEGE   (China)

Author keywords

2,4,5 Trisubstituted thiazole derivatives; HIV 1; Molecular modeling; Non nucleoside reverse transcriptase inhibitors; Three dimensional quantitative structure activity relationship

Indexed keywords

2 [[5 BENZYL 4 (4 METHOXYPHENYL)THIAZOL 2 YLAMINO]METHYL] 4 NITROPHENOL; 2,4,5 TRISUBSTITUTED THIAZOLE DERIVATIVE; 4 [5 BENZYL 2 (DIETHYLAMINO)THIAZOL 4 YL]PHENOL; 4 [[5 BENZYL 4 (4 METHOXYPHENYL)THIAZOL 2 YLAMINO]METHYL] 2 METHOXYPHENOL; 4 [[5 BENZYL 4 (4 METHOXYPHENYL)THIAZOL 2 YLAMINO]METHYL] PHENOL; 4 [[5 BENZYL 4 (4 METHOXYPHENYL)THIAZOL 2 YLAMINO]METHYL]BENZONITRILE; 5 BENZYL 4 (2 FLUOROPHENYL) N (4 METHOXYBENZYL)THIAZOL 2 AMINE; 5 BENZYL 4 (2,4 DIFLUOROPHENYL) N (4 METHOXYBENZYL)THIAZOL 2 AMINE; 5 BENZYL 4 (4 FLUOROPHENYL) N (4 METHOXYBENZYL)THIAZOL 2 AMINE; 5 BENZYL 4 (4 METHOXYPHENYL) N (3 NITROBENZYL)THIAZOL 2 AMINE; 5 BENZYL 4 (4 METHOXYPHENYL) N (3,4,5 TRIMETHOXYBENZYL)THIAZOL 2 AMINE; 5 BENZYL 4 (4 METHOXYPHENYL) N (4 NITROBENZYL)THIAZOL 2 AMINE; 5 BENZYL 4 (4 METHOXYPHENYL) N (NAPHTHALEN 2 YLMETHYL)THIAZOL 2 AMINE; 5 BENZYL 4 (4 METHOXYPHENYL) N (PYRIDIN 3 YLMETHYL)THIAZOL 2 AMINE; 5 BENZYL 4 (4 METHOXYPHENYL) N ,N DIMETHYLTHIAZOL 2 AMINE; 5 BENZYL N (2 METHOXYBENZYL) 4 (4 METHOXYPHENYL)THIAZOL 2 AMINE; 5 BENZYL N (2,6 DICHLOROBENZYL) 4 (4 METHOXYPHENYL)THIAZOL 2 AMINE; 5 BENZYL N (3 METHOXYBENZYL) 4 (4 METHOXYPHENYL)THIAZOL 2 AMINE; 5 BENZYL N (4 FLUOROBENZYL) 4 (4 METHOXYPHENYL)THIAZOL 2 AMINE; 5 BENZYL N (4 METHOXYBENZYL) 4 (4 METHOXYPHENYL)THIAZOL 2 AMINE; 5 BENZYL N [4 (DIMETHYLAMINO)BENZYL] 4 (4 METHOXYPHENYL) THIAZOL 2 AMINE; 5 BENZYL N,N DIETHYL 4 (4 METHOXYPHENYL)THIAZOL 2 AMINE; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; EFAVIRENZ; HUMAN IMMUNODEFICIENCY VIRUS 1 REVERSE TRANSCRIPTASE; N,5 DIBENZYL 4 (4-METHOXYPHENYL)THIAZOL 2 AMINE; NEVIRAPINE; NONNUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITOR; RNA DIRECTED DNA POLYMERASE; UNCLASSIFIED DRUG; UNINDEXED DRUG; REVERSE TRANSCRIPTASE, HUMAN IMMUNODEFICIENCY VIRUS 1; RNA DIRECTED DNA POLYMERASE INHIBITOR; THIAZOLE DERIVATIVE; 4 (5 BENZYL 2 (DIETHYLAMINO)THIAZOL 4 YL)PHENOL; 4 [(5 BENZYL 4 (4 METHOXYPHENYL)THIAZOL 2 YLAMINO)METHYL]PHENOL; 5 BENZYL 4 (2 CHLOROPHENYL) N (4 METHOXYBENZYL)THIAZOL 2 AMINE; 5 BENZYL 4 (4 METHOXYPHENYL) N,N DIMETHYLTHIAZOL 2 AMINE; 5 BENZYL N (4 METHOXYBENZYL) 4 (4 METHOXYPHENYL) N METHYLTHIAZOL 2 AMINE; 5 BENZYL N (4 METHOXYBENZYL) 4 PHENYLTHIAZOL 2 AMINE; 5 BENZYL N (FURAN 2 YLMETHYL) 4 (4 METHOXYPHENYL)THIAZOL 2 AMINE; 5 BENZYL N [4 (DIMETHYLAMINO)BENZYL] 4 (4 METHOXYPHENYL)THIAZOL 2 AMINE; N (4 METHOXYBENZYL) 4 (4 METHOXYPHENYL) 5 METHYLTHIAZOL 2 AMINE; N,5 DIBENZYL 4 (4 METHOXYPHENYL)THIAZOL 2 AMINE;

ARTICLE; COMPARATIVE MOLECULAR FIELD ANALYSIS; COMPARATIVE MOLECULAR SIMILARITY INDICES ANALYSIS; DEMETHYLATION; DRUG SYNTHESIS; HUMAN IMMUNODEFICIENCY VIRUS 1; HYDROGEN BOND; IC 50; MOLECULAR DOCKING; PROTON NUCLEAR MAGNETIC RESONANCE; QUANTITATIVE STRUCTURE ACTIVITY RELATION; VIRUS REPLICATION; VIRUS STRAIN; ANTAGONISTS AND INHIBITORS; ANTIVIRAL RESISTANCE; CHEMICAL STRUCTURE; CHEMISTRY; DRUG DESIGN; DRUG EFFECTS; ENZYMOLOGY; GENETICS; HEK293 CELL LINE; HUMAN; IC50; MUTATION; PROTEIN CONFORMATION; ANTIVIRAL ACTIVITY; CONCENTRATION RESPONSE; CONTROLLED STUDY; CYTOTOXICITY TEST; DRUG CYTOTOXICITY; HUMAN CELL; VIRUS INHIBITION; VIRUS MUTANT; WILD TYPE;

DRUG DESIGN; DRUG RESISTANCE, VIRAL; HEK293 CELLS; HIV REVERSE TRANSCRIPTASE; HIV-1; HUMANS; INHIBITORY CONCENTRATION 50; MODELS, MOLECULAR; MUTATION; PROTEIN CONFORMATION; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP; REVERSE TRANSCRIPTASE INHIBITORS; THIAZOLES;

EID: 84905159374     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2014.07.072     Document Type: Article

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