2,2 - Dimethyl-cyclopropane Derivatives In The Design, Synthesis And Biological Activity Study

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 pesticides and medicines, which can be used to synthesize many kinds of high efficiency new antibacterials such as ciprofloxacin and enoxacin. S-(+)-2, 2-dimethylcyclopropanecarboxylic acid is a critical intermediate to synthesize cilastatin. The compound preparation of cilastatin and imipenem is Tienam. Tienam is especially suitable for mixed infection of various bacteria and mixed infection of aerobic and anaerobic bacteria.This research focuses on the synthesis of a series of unique compounds on the basis of 2,2-dimethylcyclopropanecarboxylic acid, which is totally harmless to human body and degradable. The essential structure of the 2,2-dimethyl-cyclopropanecarboxylic acid being preserved, onto the carboxyl, highly active groups, such as acyl thiourea, salicylic, and sugar, and heterocyclic structures, such as pyridu,pyrimidine,pyrazole and thiazole will be added. All together, 36 new compounds belonging to 6 series have been synthesized, all being tested by ~1H NMR, element analyse, and some of them pass x-ray. Tests of their bioactivity show that a couple of these compounds deserve further study.