title: Synthesis of potent and selective inhibitors of Candida albicans N-myristoyltransferase based on the benzothiazole structure.
abstract: Two parallel synthetic methods using solid-supported reagents were established to examine the rapid optimization of weak hit compound 1. Several compounds showed high potency in the low nanomolar range against N-myristoyltransferase. The structure-activity relationship (SAR) and antifungal activities of a series of novel 2-aminobenzothiazole N-myristoyltransferase inhibitors are presented.
authors.affiliation: Central Research Laboratories, SSP Co., Ltd, 1143 Nanpeidai, Narita, Chiba 286-8511, Japan. kazuo.yamazaki@ssp.co.jp <kazuo.yamazaki@ssp.co.jp>
authors.forename: Kazuo
authors.initials: K
authors.lastname: Yamazaki
authors.forename: Yasushi
authors.initials: Y
authors.lastname: Kaneko
authors.forename: Kie
authors.initials: K
authors.lastname: Suwa
authors.forename: Shinji
authors.initials: S
authors.lastname: Ebara
authors.forename: Kyoko
authors.initials: K
authors.lastname: Nakazawa
authors.forename: Kazuhiro
authors.initials: K
authors.lastname: Yasuno
mesh_terms: D000217:Acyltransferases / Q000037:antagonists & inhibitors*; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D052160:Benzothiazoles; D002176:Candida albicans / Q000187:drug effects / Q000201:enzymology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006367:HeLa Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D000935:Antifungal Agents; D052160:Benzothiazoles; D004791:Enzyme Inhibitors; D013844:Thiazoles; D000217:Acyltransferases; C050480:glycylpeptide N-tetradecanoyltransferase; C005465:benzothiazole