Synthesis and biological activity of novel thiourea derivatives as carbonic anhydrase inhibitors

2014 ◽  
Vol 30 (1) ◽  
pp. 75-80 ◽  
Author(s):  
Neslihan Korkmaz ◽  
Oday A. Obaidi ◽  
Murat Senturk ◽  
Demet Astley ◽  
Deniz Ekinci ◽  
...  
Keyword(s):  
Biological Activity ◽  
Carbonic Anhydrase ◽  
Carbonic Anhydrase Inhibitors ◽  
Thiourea Derivatives

scholarly journals Synthesis and Evaluation of New Phthalazine Urea and Thiourea Derivatives as Carbonic Anhydrase Inhibitors

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Nurcan Berber ◽  
Mustafa Arslan ◽  
Emre Yavuz ◽  
Cigdem Bilen ◽  
Nahit Gencer
Keyword(s):  
Carbonic Anhydrase ◽  
Nitro Group ◽  
Zinc Ion ◽  
Inhibitory Effect ◽  
Carbonic Anhydrases ◽  
Coumarin Derivatives ◽  
Inhibitory Effects ◽  
Carbonic Anhydrase Inhibitors ◽  
Thiourea Derivatives ◽  
Amine Derivative

A new series of phthalazine substituted urea and thiourea derivatives were synthesized, and their inhibitory effects on the activity of purified human carbonic anhydrases (hCAs I and II) were evaluated. 2H-Indazolo[2,1-b]phthalazine-trione derivative(1)was prepared with 4-nitrobenzaldehyde, dimedone, and phthalhydrazide in the presence of TFA in DMF, and nitro group was reduced to amine derivative(2)with SnCl2·2H2O. The compound was reacted with isocyanates and isothiocyanates to get the final products(3a–p). The results showed that all the synthesized compounds inhibited the CA isoenzymes activity.3a(IC50= 6.40 µM for hCA I and 6.13 µM for hCA II) has the most inhibitory effect. The synthesized compounds are very bulky to be able to bind near the zinc ion, and they much more probably bind as the coumarin derivatives.

C-cinnamoyl Glycosides: An Emerging “Tail” for the Development of Selective Carbonic Anhydrase Inhibitors

2019 ◽  
Vol 26 (15) ◽  
pp. 2601-2608
Author(s):  
Helberth Llantén Martínez ◽  
Leonardo E. Riafrecha ◽  
Pedro A. Colinas
Keyword(s):  
Biological Activity ◽  
Carbonic Anhydrase ◽  
Carbonic Anhydrase Inhibitors ◽  
Wide Range

Attachment of different tails to the well-known carbonic anhydrase (CA) pharmacophores has led to the development of several new CA inhibitors (CAIs). A very good example of such “tails” is constituted by carbohydrates, which represent a wide range of chemotypes, leading thus to a high number of new CAIs. In the last years, several C-cinnamoyl glycosides containing different scaffolds have been prepared and investigated as carbonic anhydrase inhibitors, showing that some of them are very potent and selective CAIs. This article will review the latest developments in the synthesis and biological activity of these Cglycosides.

Synthesis and Biological Evaluation of New 4-Thiazolidinone Derivatives as Carbonic Anhydrase Inhibitors

2017 ◽  
Vol 14 (2) ◽  
pp. 80-85 ◽  
Author(s):  
Hayriye Genc ◽  
Busra Ceken ◽  
Cigdem Bilen ◽  
Zubeyde Sackes ◽  
Nahit Gencer ◽  
...  
Keyword(s):  
Carbonic Anhydrase ◽  
Biological Evaluation ◽  
Carbonic Anhydrase Inhibitors ◽  
Synthesis And Biological Evaluation

In-Silico Analysis of Chromone Containing Sulfonamide Derivatives as Human Carbonic Anhydrase Inhibitors

2013 ◽  
Vol 9 (4) ◽  
pp. 608-616 ◽  
Author(s):  
Zaheer Ul-Haq ◽  
Saman Usmani ◽  
Uzma Mahmood ◽  
Mariya al-Rashida ◽  
Ghulam Abbas
Keyword(s):  
Carbonic Anhydrase ◽  
In Silico ◽  
In Silico Analysis ◽  
Carbonic Anhydrase Inhibitors ◽  
Human Carbonic Anhydrase ◽  
Silico Analysis
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