| 摘要 |
PURPOSE: To obtain a new compound useful as a medicinal resistance overcoming agent low in calcium antagonistic activity, provided with the resistance to chemotherapeutic agents, overcoming the medicinal resistance to cancers or pathogenic microbes and improving the therapeutic effect by chemotherapeutic agents. CONSTITUTION: This compound (a physiologically permissible salt thereof) is expressed by formula I [X and Y are each H or a halogen; R1 is a halogen, alkyl, alkyloxy, or monocyclic or bicyclic aromatic ring which may contain one nitrogen atom in the ring], e.g. 1-(3,3-diphenylpropyl)-4-[2- hydroxy-3-(quinolin-5-yloxy)propyl]piperazine. The compound of formula I is obtained by the following process: a compound of formula III is prepared by reaction of a halogen compound of formula II with piperazine; separately, an epoxy compound of formula V is formed by reaction between a compound of formula IV and an epihalohydrin in the presence of sodium hydride; and the compound of formula III and the epoxy compound of formula V are subjected to ring opening condensation reaction. The microbial infectious diseases associated with this compound are involved in Staphylococcus aureus, Plasmodium, Trypanosoma, etc. |
