Syntheses and exploration of new biological activities in ethyl 6/7-substituted and 6, 7-disubstituted quinolin-4-one-3-carboxylates
摘要:
Syntheses of a number of ethyl 1H, 4H-quinolin-4-one-3-carboxylates carrying substituted piperidinedione ring at position 6 (25 & 31-35), tetrahydrofuranone (37) or tetraydropyridazinone ring (39) at position 7 and hydroxy and hydroxymethyl substituents at positions 6 and 7 respectively (41) of the quinolone ring, are reported here, of these compounds on the in vitro heme polymerase activity of Plasmodia and on the in vitro fungal growth are described.
6-Aryl-4,5-dihydro-3(2H)-pyridazinones. A new class of compounds with platelet aggregation inhibiting and hypotensive activities
作者:M. Thyes、H. D. Lehmann、J. Gries、H. Koenig、R. Kretzschmar、J. Kunze、R. Lebkuecher、D. Lenke
DOI:10.1021/jm00360a004
日期:1983.6
This paper reports on the synthesis and pharmacological activity of 6-aryl-4,5-dihydro-3(2H)-pyridazinone derivatives. The compounds exhibit an aggregationinhibiting action on human platelets in vitro and on rat platelets under ex vivo conditions, as well as a hypotensive action on rats. The strongest pharmacological effects were found with dihydropyridazinones, which have a 6-[p-[(chloroalkanoyl)amino]phenyl]