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在介导HIV进入细胞受体的过程中,非肽类小分子具有重要的药理学意义,开发具有高活性、高选择性及良好药代动力学性质的新药已成为研究的热点,该类小分子具有氯原子、苯甲酰胺、哌啶等活性基团而备受关注.本文合成了哌啶苯甲酰胺的邻对位二取代、对位以及邻位氯化物(7);通过(7)、1-(对氯苯甲氧基)-2-溴甲基-4-溴苯(3)合成了三种新的哌啶基氯代苯甲酰胺类非肽类小分子8a-8c,对三种氯代苯甲酰胺进行了生物活性检测及IR、MS、1H NMR表征.结果表明N-乙基-4-氯-N-(N-(2-对氯苯甲氧基-5-溴苯甲基)-4-哌啶基)苯甲酰胺8a具有较好的生物活性.
Non-peptide small molecules have important pharmacological significance in the process of mediating the entry of HIV into cell receptors. It has become a hot research topic to develop new drugs with high activity, high selectivity and good pharmacokinetic properties. It has attracted much attention due to its active groups such as chlorine atom, benzamide, piperidine, etc. The ortho-para-disubstituted, para- and para-substituted chlorides of piperidine benzamide were synthesized in this paper. (7) (P-chlorophenylmethoxy) -2-bromomethyl-4-bromobenzene (3) Three novel piperidinyl chlorobenzamide non-peptide small molecules 8a-8c Three kinds of chlorobenzamides were tested for biological activity and characterized by IR, MS and 1H NMR.The results showed that N-ethyl-4-chloro-N- (N- (2-chlorobenzyloxy- Benzyl) -4-piperidinyl) benzamide 8a has better biological activity.