| 摘要 |
1-(4-amidino phenyl)-4-substituted piperazinone derivatives (I) are new. (I) are of formula (Q): R1 = H, 1-4C alkyl, or phenyl 1-4C alkyl; oxo group = may be in position 2 or 3 of the piperazine ring; R2 = H, OH, or a group protecting the amidino group; R3 = H, 1-5C alkyl, 3-12C mono- or bicyclic cycloalkyl, 2-4C alkenyl, or alkynyl, (these groups being optionally substituted by halogens or OH), 6-14C mono- bi- or tri-cyclic aryl, pyridyl, thienyl, furanyl, quinolyl, benzodioxanyl, benzodioxolyl, benzothienyl, benzofuranyl, pyrazinyl, phenyl 1-4C alkyl, naphthyl 1-4C alkyl, (both optionally substituted on the aryl ring) or piperonyl; R4 and R5 = H, 1-5C alkyl or, together with the N atom, form piperidinyl or morpholinyl, aryl and heteroaryl groups being optionally substituted by halogens, 1-4C alkyl, CF3, 1-4C alkylthio, alkoxy, alkylsulfonyl, NO2, -COOR, -CH2-COOR, or -O-CH2-COOR, and R = 1-4C alkyl.
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