U. M. Kocyigit, Yakup Budak, M. Gürdere
Mar 2, 2019
Citations
0
Influential Citations
26
Citations
Quality indicators
Journal
Monatshefte für Chemie - Chemical Monthly
Abstract
A series of novel 1,3,5-trisubstituted pyrazoline derivatives, (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones, were synthesized and evaluated for their antimicrobial and anticancer activities. In addition, the compounds were tested against acetylcholinesterase (AChE) enzyme and two physiologically relevant carbonic anhydrase I and II isozymes (hCA I and II). In this study, inhibition of hCA I and hCA II by the novel synthesized 1,3,5-trisubstituted pyrazolines was impressive, with Ki values in the range of 3.33–7.90 nM for hCA I and 2.07–8.47 nM for hCA II, while the Ki values of these compounds for AChE were recorded in the range of 9.61–48.42 nM, respectively. Two compounds can be investigated as the leader compounds because of their lowest Ki values to make further detailed CA inhibition studies.Graphical abstract