Synthesis and investigation of anticancer, antibacterial activities and carbonic anhydrase, acetylcholinesterase inhibition profiles of novel (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 View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2019-04

AUTHORS

Umit M. Kocyigit, Yakup Budak, Meliha Burcu Gürdere, Neşe Dürü, Parham Taslimi, İlhami Gülçin, Mustafa Ceylan

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. More... »

PAGES

721-731

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/s00706-019-2350-z

DOI

http://dx.doi.org/10.1007/s00706-019-2350-z

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1112504101


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