| abstract |
Tetrazolyl derivatives of β-lactams are found to be potent elsstase inhibitors and thereby useful anti-inflammatory/antidegenerative agents. n Those compounds have the structural formula:n wherein T isn orn wherein n is an integer of 0 to 2; M is, e.g., trifluoromethyl; chloro or fluoro; or -CH 2 A wherein A represents:n (a) R a -CO-O-; (b) R.HN-CO-O-; (c) R a O-CO-CH 2 NH-CO-O-; or (d) R a -S-; R' is, e.g.,n (1) C 1-6 alkyl; (2) hydroxy; (3) OR a where R. isn (a) C 1-6 alkyl; (b) -C 6 H 5 ; (c) -CN 2 C 6 H 5 ; (d) -CH 2 CH 2 C 6 N 5 ; (e)n , where R h represents hydrogen, C 1-6 alkyl, phenyl, benzyl, or C 1-6 alkylamino; or (4) fluoro or chloro; (5) halo; (6) -SO 2 R h ; (7) phenyl; or (8) haloC 1-6 alkyl-CO-NH-; R 2 is H; -O-C 1-6 alkyl; halo; or C 1-6 alkyl;n Q' and Q 2 independently are, e.g., (1) hydrogen; (2) methyl, ethyl or i-or n-propyl; (3) methylene; (4) phenylthiomethyl or phenyl sulfonylmethyl; (5) benzyl of formulan wherein X, and X 2 independently are H, OCH 3 , -COOH, C 1- 6 alkyl, -COOC 1-6 -alkyl, -CH 2 COOH, or CH 2 COOC 1-6 -alkyl; or (6) -CH 2 -CO-OR h ; and R is R a . |