4-Aryl 5-aminoalkyl 4-thiazoline-2-ones and 2-thiones - CNS depressant and cardiovascular agents having anti-inflammatory, adrenolytic and anti-ulcer activity

摘要

Cpds. of formula (I) are their salts (where Ar = mono- or polycarboxylic aryl opt. substd. by alkyl, CF3, alkoxy, alkenyloxy, alkylenedioxy, halo, alkylthio, nitro, opt. substd amino etc. and is partic. phenyl, lower alkylphenyl, trifluoromethylphenyl, lower alkoxy phenyl di(lower alkyl) aminophyenyl, halophenyl or alkylmercaptphenyl. Alk = 1-3C straight or branched, opt. unstatd. radical -NR1R2 = monosubstd. amino (e.g. monoalkylamino, mono-hydroxyalkylamino, monoarylalkylamino, monoaryloxyalkylamino, mono N,N-dialkylamino-alkyl amino) or disubstd. amino (e.g. N,N,-dialkylamino, N-cycloalkyl-N-alkylamino, N-alkyl-N-arylalkylamino, N-hydrozylakyl-N-alkylamino, N,N-dihydroxyalkylamino, N,N-alkyleneimine, N-N-oxoalkyleneimine, N,N-thioalkyleneimine, N,N-azaaalkyleneimine (opt. substd. on the aza function by alkyl, hydroxyalkyl, arylalkyl or aryl (opt. substd. by halo or alkoxy)). Z = O or SR3 = H, lowre alkyl, free or etherified lower hydroxyalkyl, arylalkyl dialkylaminoalkyl, lowre aliphatic or aromatic acyl or carbamoyl).act on the CNS and cardiovascular system and have antiinflammatory adrenolytic and anti-ulcer activity. They have anti-arrhythmic activity, prevent platelet agglutination, have anti-convulsant, cataleptic and some analgesic activity. They may be administered orally, parenterally or rectally in the usual formations. LD50 ip in mice vary from 100 to >1000mg/kg.