The Design Of Cyclopropane Derivatives, Synthesis And Biological Activity

Cyclopropane is a kind of structure with very excellent bioactivity. Compounds with it are mostly important media in the metabolism of both animals and plants. Therefore, it is an ideal and widely used material in drug design of the heterocyclic and polypeptides drugs and pesticide such as pyrethrum and pyrethroid insecticides.This research focuses on the synthesis of a series of unique compounds on the basis of cyclopropanecarboxylic acid, which is totally harmless to human body and degradable. The essential structure of the cyclopropanecarboxylic acid being preserved, onto the carboxyl, highly active groups, such as acyl thiourea, salicylic, and sugar, and heterocyclic structures, such as pyridine,pyrimidine,pyrazole and thiazole will be added. All together, 34 new compounds belonging to 5 series have been synthesized, all being tested by HNMR, element analyse, and some of them pass x-ray. Tests of their bioactivity show that a couple of these compounds deserve further study.