Literature DB >> 26808123

The inhibitory effects of phenolic Mannich bases on carbonic anhydrase I and II isoenzymes.

Cem Yamali1,2, Mehtap Tugrak1, Halise Inci Gul1, Muhammet Tanc2, Claudiu T Supuran2.   

Abstract

Phenolic mono Mannich bases [2-[4-hydroxy-3-(aminomethyl)benzylidene]-2,3-dihydro-1H-inden-1-one (8-15)] and bis Mannich bases [2-[4-hydroxy-3,5-bis(aminomethyl)benzylidene]-2, 3-dihydro-1H-inden-1-one (2-7)] were synthesized starting from 2-(4-hydroxybenzylidene)-2, 3-dihydro-inden-1-one (1). This study was designed in order to investigate the carbonic anhydrase (CA, EC 4.2.1.1) inhibitory properties of a library of compounds incorporating the phenol functional group. All prepared compounds showed a low inhibition percentages on both human (h) isoforms hCA I and hCA II compared to the reference sulfonamide acetazolamide. Mannich bases 2-15 had lower inhibition percentages than the compound 1 on hCA I and hCA II, except compound 14, which is a Mannich base derivative of dipropylamine, which had a similar inhibitory power as compound 1 on hCA II. All compounds synthesized 1-15 were 1.3-1.9 times more effective on hCA II comparing with the effectivenes of the compounds on hCA I.

Entities:  

Keywords:  Carbonic anhydrase; Mannich bases; indanone; phenol

Mesh：

Substances：

Year:  2016        PMID： 26808123     DOI： 10.3109/14756366.2015.1126715

Source DB:  PubMed          Journal:  J Enzyme Inhib Med Chem        ISSN： 1475-6366            Impact factor:   5.051


  6 in total

1.  Synthesis and characterization of novel acyl hydrazones derived from vanillin as potential aldose reductase inhibitors.

Authors:  Yeliz Demir; Feyzi Sinan Tokalı; Erbay Kalay; Cüneyt Türkeş; Pelin Tokalı; Osman Nuri Aslan; Kıvılcım Şendil; Şükrü Beydemir
Journal:  Mol Divers       Date:  2022-09-14       Impact factor: 3.364

2.  Microwave-assisted synthesis and bioevaluation of new sulfonamides.

Authors:  Halise Inci Gul; Cem Yamali; Fatma Yesilyurt; Hiroshi Sakagami; Kaan Kucukoglu; Ilhami Gulcin; Mustafa Gul; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2017-12       Impact factor: 5.051

3.  Synthesis, carbonic anhydrase I and II inhibition studies of the 1,3,5-trisubstituted-pyrazolines.

Authors:  Halise Inci Gul; Ebru Mete; Parham Taslimi; Ilhami Gulcin; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2016-10-24       Impact factor: 5.051

4.  Designing, synthesis and bioactivities of 4-[3-(4-hydroxyphenyl)-5-aryl-4,5-dihydro-pyrazol-1-yl]benzenesulfonamides.

Authors:  Halise Inci Gul; Ebru Mete; Sakip Emre Eren; Hiroshi Sakagami; Cem Yamali; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2016-10-23       Impact factor: 5.051

5.  Synthesis, cytotoxicities, and carbonic anhydrase inhibition potential of 6-(3-aryl-2-propenoyl)-2(3H)-benzoxazolones.

Authors:  Sinan Bilginer; Halise Inci Gul; Feyza Sena Erdal; Hiroshi Sakagami; Serkan Levent; Ilhami Gulcin; Claudiu T Supuran
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

6.  Crystal structure and theoretical study of (2E)-1-[4-hy-droxy-3-(morpholin-4-ylmeth-yl)phen-yl]-3-(thio-phen-2-yl)prop-2-en-1-one.

Authors:  Fatma Yesilyurt; Abdullah Aydin; Halise Inci Gul; Mehmet Akkurt; Nefise Dilek Ozcelik
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2018-06-12
  6 in total

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