Novel ketoconazole analogues based on the replacement of 2,4-dichlorophenyl group with 1,4-benzothiazine moiety: Design, synthesis, and microbiological evaluation

Bioorganic and Medicinal Chemistry

Volumn 14, Issue 15, 2006, Pages 5196-5203

  Schiaffella, Fausto ^a   Macchiarulo, Antonio ^a   Milanese, Lara ^a   Vecchiarelli, Anna ^a   Fringuelli, Renata ^a  

^a UNIVERSITY OF PERUGIA   (Italy)

Author keywords

1,4 Benzothiazine; Azoles; Bioisosters; CA CYP51

Indexed keywords

7 [2 (1H IMIDAZOL 1 YLMETHYL) 4 (METHANESULFONYLOXYMETHYL) 1,3 DIOXOLAN 2 YL] 4 METHYL 3,4 DIHYDRO 2H 1,4 BENZOTHIAZIN 3 ONE; 7 [2 (BROMOMETHYL) 4 (BENZOYLOXYMETHYL) 1,3 DIOXOLAN 2 YL] 4 METHYL 3,4 DIHYDRO 2H 1,4 BENZOTHIAZIN 3 ONE; 7 [2 (BROMOMETHYL) 4 (HYDROXYMETHYL) 1,3 DIOXOLAN 2 YL] 4 METHYL 3,4 DIHYDRO 2H 1,4 BENZOTHIAZIN 3 ONE; 7 [4 (BENZOYLOXYMETHYL) 2 (1H IMIDAZOL 1 YLMETHYL) 1,3 DIOXOLAN 2 YL] 4 METHYL 3,4 DIHYDRO 2H 1,4 BENZOTHIAZIN 3 ONE; 7 [4 (HYDROXYMETHYL) 2 (1H IMIDAZOL 1 YLMETHYL) 1,3 DIOXOLAN 2 YL] 4 METHYL 3,4 DIHYDRO 2H 1,4 BENZOTHIAZIN 3 ONE; 7 [4 [[4 (ACETYLPIPERAZIN 1 YL)PHENOXY]METHYL] 2 (1H IMIDAZOL 1 YLMETHYL) 1,3 DIOXOLAN 2 YL] 4 METHYL 3,4 DIHYDRO 2H 1,4 BENZOTHIAZIN 3 ONE; ANTIFUNGAL AGENT; BENZENE DERIVATIVE; BENZOTHIAZINE DERIVATIVE; IMIDAZOLE DERIVATIVE; KETOCONAZOLE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTIBIOTIC SENSITIVITY; ANTIFUNGAL ACTIVITY; ARTICLE; CANDIDA ALBICANS; CANDIDIASIS; CIS ISOMER; COLONY FORMING UNIT; CONTROLLED STUDY; DRUG DESIGN; DRUG SCREENING; DRUG SYNTHESIS; ENZYME INHIBITION; FEMALE; MOLECULAR MODEL; MOUSE; NONHUMAN; QUANTUM MECHANICS; TRANS ISOMER;

ANIMALS; CANDIDA ALBICANS; CANDIDIASIS; CRYSTALLOGRAPHY, X-RAY; CYTOCHROME P-450 ENZYME SYSTEM; DISEASE MODELS, ANIMAL; ENZYME INHIBITORS; FEMALE; FUNGAL PROTEINS; HYDROCARBONS, CHLORINATED; IMMUNOLOGIC TESTS; KETOCONAZOLE; KIDNEY; MICE; MICROBIAL SENSITIVITY TESTS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; THIAZINES;

CANDIDA ALBICANS;

EID: 33745151493     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2006.04.004     Document Type: Article

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