132483-77-3Relevant articles and documents
Nucleophilic aromatic substitution using Et3SiH/cat. t-Bu-P4 as a system for nucleophile activation
Ueno, Masahiro,Yonemoto, Misato,Hashimoto, Masahiro,Wheatley, Andrew E. H.,Naka, Hiroshi,Kondo, Yoshinori
, p. 2264 - 2266 (2008/01/03)
A novel type of deprotonative arylation of nucleophiles was conducted using Et3SiH/cat. t-Bu-P4 and the powerful SNAr reactions of aryl fluorides were accomplished using alcohols and malonates as nucleophiles. The Royal Society of Ch
Preparation and biological activity of 2-[4-(thiazol-2-yl)phenyl]propionic acid derivatives inhibiting cyclooxygenase
Naito,Goto,Akahoshi,Ono,Yoshitomi,Okano,Sugiyama,Abe,Hanada,Hirata,Watanabe,Fukaya,Yokoyama,Fujita
, p. 2323 - 2332 (2007/10/02)
A series of 2-[4-(thiazol-2-yl)phenyl]propionic acids substituted at various positions were prepared by the reaction of diethyl 2-methyl-2-(4-thiocarbamoylphenyl)malonates with α-bromoaldehyde diethyl acetals or α-haloketones followed by hydrolysis of esters. The inhibition of prostaglandin H synthetase (cyclooxygenase) was assayed by use of an enzyme preparation from guinea pig polymorphonuclear leukocytes. Examination of the structure-activity relationship of these compounds indicated that the substitution pattern with halogens at position 3 (R1) of the benzene ring and a methyl group in position 4 (R2) and/or 5 (R3) of the thiazole ring were favorable for inhibitory activity. The compounds bearing bulky alkyl or polar functional groups at the R2 position were weak inhibitors. The potent inhibitors of cyclooxygenase were tested for their ability to reduce carrageenin-induced inflammation of rat paws. These derivatives had strong anti-inflammatory activity based on their strong inhibition of cyclooxygenase, with some exceptions, including those with a thiomethyl group at R1.
