Journal ArticleDOI
Synthesis of N-alkyl (aril)-tetra pyrimidine thiones and investigation of their human carbonic anhydrase I and II inhibitory effects.
Afsun Sujayev,Leyla Polat Kose,Emin Garibov,İlhami Gülçin,Vagif Farzaliev,Saleh Alwasel,Claudiu T. Supuran +6 more
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TLDR
Tetrahydropyrimidine thiones, which are cyclic thiocarbamides derivatives, were synthesised from thiourea, β-diketones and substituted benzaldehydes, and tested for inhibition of the cytosolic human isoforms I and II.Abstract:
Tetrahydropyrimidine thiones, which are cyclic thiocarbamides derivatives, were synthesised from thiourea, β-diketones and substituted benzaldehydes. A tautomeric form of these derivatives incorporates the thiol functionality, which is known to interact with metal ions from metalloenzymes active sites, such as the carbonic anhydrases (CAs, EC 4.2.1.1) among others. This is a superfamily of widespread enzymes, which catalyses a crucial biochemical reaction, the reversible hydration of carbon dioxide to bicarbonate and protons (H(+)). The newly synthesised N-alkyl (aril)-tetrahydropyrimidine thiones were tested for inhibition of the cytosolic human isoforms I and II (hCA I and II). Both isoforms were effectively inhibited by the newly synthesised thiones. Ki values were in the range of 218.5 ± 23.9-261.0 ± 41.5 pM for hCA I, and of 181.8 ± 41.9-273.6 ± 41.4 pM for hCA II, respectively. This under-investigated class of derivatives may bring interesting insights in the field of non-sulphonamide CA inhibitors.read more
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Synthesis, characterization, inhibition effects, and molecular docking studies as acetylcholinesterase, α-glycosidase, and carbonic anhydrase inhibitors of novel benzenesulfonamides incorporating 1,3,5-triazine structural motifs
Nebih Lolak,Suleyman Akocak,Cüneyt Türkeş,Parham Taslimi,Mesut Işık,Şükrü Beydemir,İlhami Gülçin,Mustafa Durgun +7 more
TL;DR: The novel synthesized compounds (MZ1-MZ11) have a higher enzyme inhibitory potential than ACR, TAC, and AZA, respectively and may have the potential to be used as alternative medicines after further research in the treatment of many diseases such as diabetes, Alzheimer's disease, heart failure, ulcer, and epilepsy.
Novel Sulphamides and Sulphonamides Incorporating the Tetralin Scaffold as Carbonic Anhydrase and Acetylcholine
TL;DR: Sulphamides and sulphonamides are important biologically active compounds as mentioned in this paper and have potential use in the treatment of depression,neuropathic and inflammatory pains.
Journal ArticleDOI
Synthesis and biological evaluation of aminomethyl and alkoxymethyl derivatives as carbonic anhydrase, acetylcholinesterase and butyrylcholinesterase inhibitors.
İlhami Gülçin,Malahat T. Abbasova,Parham Taslimi,Zübeyir Huyut,Leyla Safarova,Afsun Sujayev,Vagif Farzaliyev,Şükrü Beydemir,Saleh Alwasel,Claudiu T. Supuran +9 more
TL;DR: Compounds containing nitrogen and sulfur atoms can be widely used in various fields such as industry, medicine, biotechnology and chemical technology and the inhibitory effects of these molecules were investigated against acetylcholinesterase, butyrylcholinersterase and carbonic anhydrase I, and II isoenzymes.
Journal ArticleDOI
Synthesis and bioactivity of several new hetaryl sulfonamides
Parham Taslimi,Afsun Sujayev,Sevgi Mamedova,Pınar Kalın,İlhami Gülçin,Nastaran Sadeghian,Şükrü Beydemir,Ö. İrfan Küfrevioğlu,Saleh Alwasel,Vagif Farzaliyev,S. A. Mamedov +10 more
TL;DR: Newly synthesized hetaryl sulfonamides exhibited impressive inhibition profiles with Ki values in the range of 1.42–6.58’nM against hCA I, 1.72–7.41 nMAgainst AChE and BChE, respectively, and acetazolamide showed Ki values of 43.69 ± 6.82 − 2.08 against AChe and BE.
Journal ArticleDOI
The synthesis of novel sulfamides derived from β-benzylphenethylamines as acetylcholinesterase, butyrylcholinesterase and carbonic anhydrase enzymes inhibitors.
Akın Akıncıoğlu,Ebutalib Kocaman,Hulya Akincioglu,Ramin Ekhteiari Salmas,Serdar Durdagi,İlhami Gülçin,Claudiu T. Supuran,Süleyman Göksu +7 more
TL;DR: The inhibitory effects of the synthesized novel sulfamides derived from β-benzylphenethylamines were compared to those of acetazolamide and dorzolamide as clinical hCA I and II isoenzymes inhibitors and tacrine as a clinical AChE and BChE enzymes inhibitors.
References
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Journal ArticleDOI
Antiglaucoma carbonic anhydrase inhibitors: a patent review.
TL;DR: There is an urgent need for new antiglaucoma CAIs/approaches to treat and diagnose this disease in the very near future, as the last drug which has been discovered in the field dates back > 10 years ago.
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Carbonic anhydrase inhibitors and activators for novel therapeutic applications
TL;DR: Inhibition of mammalian α-CAs is exploited by some diuretics, whereas antiglaucoma, anticonvulsant, anti-obesity, altitude sickness and anti-tumor drugs/diagnostic agents target various of the 15 isoforms described so far in these organisms.
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Sulfa and trimethoprim-like drugs – antimetabolites acting as carbonic anhydrase, dihydropteroate synthase and dihydrofolate reductase inhibitors
TL;DR: The state of the art in the field of antibacterials based on inhibitors of these three enzyme families is revue, when several X-ray crystal structures of such enzymes in complex with their inhibitors were reported.
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Exploiting the hydrophobic and hydrophilic binding sites for designing carbonic anhydrase inhibitors.
TL;DR: The authors rationalize the drug design strategies of inhibitors belonging to the first two classes, based on recent X-ray crystallographic data, by analyzing how the hydrophobic and hydrophilic halves of the enzyme active site interact with inhibitors.
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Diuretics: from classical carbonic anhydrase inhibitors to novel applications of the sulfonamides.
TL;DR: It has been proposed that the recently observed beneficial effect of indapamide for the treatment of patients with hypertension and type 2 diabetes might be due to its potent inhibition of CA isoforms present in kidneys and blood vessels, which would explain both the blood pressure lowering effects as well as organ-protective activity of the drug.