Search for biologically active substances among new derivatives of 1,3-thiazole

Abstract

Analysis of the scientific literature indicates that the derivatives of thiazole have a sufficiently wide spectrum of pharmacological activity and a large number of drugs is created on their basis. But despite a large number of publications, there is practically no information in the literature on the physical, chemical and biological properties of compounds that have piperazine, 1,3-thiazole cycles and phenyl fragments together in their structure. As initial substances to synthesize new derivatives of N1-(4-(4-R- phenyl)-1,3thiazolyl-2)-N1-(4'-R'-phenyl)acetamide and ethyl-[2-[R-imin]-4-methyl-3-R1-2,3dihydro-1,3-thiazole-5-carboxylate the asymmetrical thioureas. Prediction of pharmacological activity for new derivatives of N1-(4-(4-Rphenyl)-1,3-thiazolyl-2)-N1-(4'-R'-phenyl)acetamide is made using the PASS program. According to the results obtained, the synthesized compounds have a wide range of pharmacological activity and act as inhibitor ACE, calcium channel N-type blocker, mucomembranous protector, insulin promoter, ubiquinol-cytochrome-c reductase inhibitor, transcription factor STAT3 inhibitor etc. Pharmacological screening for ethyl-[2-[R-imin]-4-methyl-3-R1-2,3-dihydro1,3-thiazole-5-carboxylate hydrochlorides has shown that the obtained substances possess cardiotropic activity.