Synthesis and bioactivities of 1-(4-hydroxyphenyl)-2-((heteroaryl)thio)ethanones as carbonic anhydrase I, II and acetylcholinesterase inhibitors
Cem Yamalı, Halise İnci Gül, Yeliz Demir, Cavit Kazaz, İlhami Gülçın
Abstract
C NMR, and HRMS. The compounds 2 and 4 were found potent AChE inhibitors with the Ki values of 22.13 ±1.96 nM and 23.71 ±2.95 nM, respectively, while the compounds 2 (Ki = 8.61 ±0.90 nM, on hCA I) and 1 (Ki = 8.76 ±0.84 nM, on hCA II) had considerable CAs inhibitory potency. The lead compounds may help the scientists for the rational designing of an innovative class of drug candidates targeting enzyme-based diseases.
Topics & Concepts
ChemistryThio-AcetylcholinesteraseCarbonic Anhydrase ICarbonic anhydraseAchéStereochemistryEnzymeProton NMRPotencyCarbonic anhydrase IIThiadiazolesCombinatorial chemistryIn vitroBiochemistryMedicinal chemistryEnzyme function and inhibitionCholinesterase and Neurodegenerative DiseasesPhenothiazines and Benzothiazines Synthesis and Activities