title: A series of thiazole derivatives bearing thiazolidin-4-one as non-competitive ADAMTS-5 (aggrecanase-2) inhibitors.
abstract: A series of thiazole bearing thiazolidin-4-one was discovered via high-throughput screening as non-competitive inhibitors of ADAMTS-5. Compound 31 appeared to give the best ADAMTS-5 inhibition and good selectivity over other metalloproteases.
authors: Pharmaceutical Research Center, Asahi Kasei Pharma Corporation, 632-1 Mifuku, Izunokuni-shi, Shizuoka 410-2321, Japan. atobe.mb@om.asahi-kasei.co.jp
authors: Masakazu
authors: M
authors: Atobe
authors: Naomi
authors: N
authors: Maekawara
authors: Noriko
authors: N
authors: Ishiguro
authors: Shinya
authors: S
authors: Sogame
authors: Yoshihito
authors: Y
authors: Suenaga
authors: Masashi
authors: M
authors: Kawanishi
authors: Hiroko
authors: H
authors: Suzuki
authors: Norimasa
authors: N
authors: Jinno
authors: Eiichi
authors: E
authors: Tanaka
authors: Shiro
authors: S
authors: Miyoshi
mesh_terms: D051722:ADAM Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000071116:ADAMTS5 Protein; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D004791:Enzyme Inhibitors; D013844:Thiazoles; D051722:ADAM Proteins; D000071116:ADAMTS5 Protein; C121532:ADAMTS5 protein, human