Novel pyrrolobenzoxaboroles: Design, synthesis, and biological evaluation against Trypanosoma brucei

European Journal of Medicinal Chemistry

Volumn 81, Issue , 2014, Pages 59-75

  Wu, Puhua ^a   Zhang, Jiong ^a   Meng, Qingqing ^a   Nare, Bakela ^b   Jacobs, Robert T ^b   Zhou, Huchen ^a  

^a Shanghai Jiao Tong University   (China)

^b SCYNEXIS Inc   (United States)

Author keywords

Antitrypanosomal agent; Human African trypanosomiasis; Indolobenzoxaboroles; Pyrrolobenzoxaboroles; Structure activity relationship

Indexed keywords

(4 AMINOPHENYL) [1 (1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROL 6 YL)PYRROL 3 YL]METHANONE; (4 ETHYLPHENYL) [1 (1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROL 6 YL)PYRROL 3 YL]METHANONE; (4 HYDROXYPHENYL) [1 (1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROL 6 YL)PYRROL 3 YL]METHANONE; (5 METHYLTHIOPHEN 2 YL) [1 (1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROL 6 YL)PYRROL 3 YL]METHANONE; 1,3 DIHYDRO 1 HYDROXY 6 (INDOL 1 YL) 2,1 BENZOXABOROLE; 1,3 DIHYDRO 1 HYDROXY 6 (PYRROL 1 YL) 2,1 BENZOXABOROLE; 2 (2 BROMO 4 FLUOROPHENYL) 1,3 DIOXOLANE; 2 BROMO 4 (PYRROL 1 YL)BENZYL ALCOHOL; 2 BROMO 4 AMINOBENZOIC ACID METHYL ESTER; 2 BROMO 4 NITROBENZOIC ACID; 2 BROMO 4 NITROBENZOIC ACID METHYL ESTER; 2 [2 BROMO 4 (INDOL 1 YL)PHENYL] 1,3 DIOXOLANE; 6 [3 (2 HYDROXYPHENYLSULFENYL)INDOL 1 YL] 1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROLE; 6 [3 (3 CHLOROPHENYLSULFENYL)INDOL 1 YL] 1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROLE; 6 [3 (3,4 DICHLOROPHENYLSULFENYL)INDOL 1 YL] 1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROLE; 6 [3 (4 CHLOROPHENYLSULFENYL)INDOL 1 YL] 1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROLE; 6 [3 (4 FLUOROPHENYLSULFENYL)INDOL 1 YL] 1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROLE; 6 [3 (4 HYDROXYPHENYLSULFENYL) INDOL 1 YL] 1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROLE; 6 [3 (4 METHOXYPHENYLSULFENYL)INDOL 1 YL] 1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROLE; 6 [3 (4 METHOXYPHENYLSULFINYL)INDOL 1 YL] 1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROLE; 6 [3 (4 METHOXYPHENYLSULFONYL)INDOL 1 YL] 1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROLE; 6 [3 (4 NITROPHENYLSULFENYL)INDOL 1 YL] 1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROLE; 6 [3 (NAPHTHALEN 2 YLSULFENYL)INDOL 1 YL] 1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROLE; ANTITRYPANOSOMAL AGENT; ORGANOBORON DERIVATIVE; PENTAMIDINE; PHENYL [1 (1,3 DIHYDRO 1 HYDROXY 2,1 BENZOXABOROL 6 YL) PYRROL 3 YL]METHANONE; SURAMIN; UNCLASSIFIED DRUG; UNINDEXED DRUG; [2 BROMO 4 (INDOL 1 YL)]BENZYL ALCOHOL; BORON DERIVATIVE; PYRROLE DERIVATIVE;

AFRICAN TRYPANOSOMIASIS; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIPROTOZOAL ACTIVITY; ANTITRYPANOSOMAL ACTIVITY; ARTICLE; CONTROLLED STUDY; DRUG CYTOTOXICITY; DRUG DESIGN; DRUG EFFICACY; DRUG STRUCTURE; DRUG SYNTHESIS; FEMALE; GROWTH INHIBITION; IC 50; IN VITRO STUDY; IN VIVO STUDY; L929 CELL LINE; MOUSE; MOUSE MODEL; NONHUMAN; PARASITE CLEARANCE; PROTON NUCLEAR MAGNETIC RESONANCE; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS; SURVIVAL RATE; SURVIVAL TIME; TRYPANOSOMA BRUCEI; ANIMAL; BAGG ALBINO MOUSE; CELL LINE; CELL SURVIVAL; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG EFFECTS; DRUG SENSITIVITY; GROWTH, DEVELOPMENT AND AGING; SYNTHESIS; TRYPANOSOMA BRUCEI BRUCEI; TRYPANOSOMIASIS, AFRICAN; VETERINARY;

ANIMALS; BORON COMPOUNDS; CELL LINE; CELL SURVIVAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; FEMALE; MICE; MICE, INBRED BALB C; MOLECULAR STRUCTURE; PARASITIC SENSITIVITY TESTS; PYRROLES; STRUCTURE-ACTIVITY RELATIONSHIP; TRYPANOCIDAL AGENTS; TRYPANOSOMA BRUCEI BRUCEI; TRYPANOSOMIASIS, AFRICAN;

EID: 84900475325     PISSN: 02235234     EISSN: 17683254     Source Type: Journal    
DOI: 10.1016/j.ejmech.2014.04.079     Document Type: Article

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