| 摘要 |
Phenoxypropionic acid derivs. of formula (I), their salts with bases and cpds. converted to (I) in vivo, are new: In (I), A is O or S. X1 is halo, H or CH3. R is H or 1-5C alkyl. X2 and X3 are H, halo or 1-5C akyl. R1 is H or 1-5C alkyl. -C(NOR)-is at the 2 or 3 posn. of the heterocycle and the cpd. is in the E and/or Z isomeric forms. (I) have hypocholesterolaemic, hypolipidaemic and uricosuric activities and are useful for treating or preventing cardiovascular disorders and gout. They have a better therapeutic index than the corresp. ketones and their LD50 is higher, generally >1 g./kg. orally in mice. In an example, ethyl 2- 2-bromo-4-(2-thienylhydroxy-iminomethyl)-phenoxy -2-methylprop- ionate was prepd. from the corresp. 4-(2-thenoyl)cpd. and NH2OH hydrochloride. |
