The synthesis of novel pyrazole-3,4-dicarboxamides bearing 5-amino-1,3,4-thiadiazole-2-sulfonamide moiety with effective inhibitory activity against the isoforms of human cytosolic carbonic anhydrase I and II

Mert, Samet; Alım, Zuhal; İşgör, Mehmet Mustafa; Beydemır, Şükrü; Kasımoğulları, Rahmi

doi:10.1016/j.bioorg.2016.07.006

Cited by 19 publications

(15 citation statements)

References 56 publications

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“…Sarıkaya et al reported that some phenol derivatives inhibit the esterase activity in a non‐competitive manner. Additionally, Beydemir and co‐workers reported that some thiadiazole‐substituted sulphonamides and some anti‐inflammatory agents (fluorometholone acetate and dexamethasone) inhibit esterase activity in a non‐competitive manner. The non‐competitive inhibition of esterase activity is limited to these reports and our results are new contribution for the non‐competitive inhibition of esterase activity.…”

Section: Resultsmentioning

confidence: 99%

Microwave‐assisted synthesis of 1‐substituted‐1H‐benzimidazolium salts: Non‐competitive inhibition of human carbonic anhydrase I and II

Karlık

Gençer²,

Karataş

et al. 2019

Archiv der Pharmazie

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A series of 1-substituted-1H-benzimidazolium p-toluenesulfonate salts were synthesized in good yields by the reaction of 1-substituted benzimidazole derivatives and p-toluenesulfonic acid under microwave irradiation. Two iodide salts were synthesized by the anion exchange reaction of the corresponding p-toluenesulfonate salt and NaI.All compounds were characterized by 1 H NMR, 13 C NMR, IR, LC-MS spectroscopic methods, and elemental analyses. The crystal structure of 1-methoxyethyl-1Hbenzimidazolium p-toluenesulfonate 2d showed that cation and anion are interconnected by N−H···O and C−H···O hydrogen bonds. All compounds were examined as inhibitor of human carbonic anhydrase (hCA) I and II, and all of them inhibited hCA I and hCA II. Kinetic investigation results revealed that these compounds inhibit hCA I and hCA II in a non-competitive manner. The iodide salts had higher inhibitory activity than their corresponding p-toluenesulfonate salts.

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Section: Resultsmentioning

confidence: 99%

Microwave‐assisted synthesis of 1‐substituted‐1H‐benzimidazolium salts: Non‐competitive inhibition of human carbonic anhydrase I and II

Karlık

Gençer²,

Karataş

et al. 2019

Archiv der Pharmazie

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“…33) for hCA I (K i ¼ 0.119 mM) and the compound 285 (Fig. 33) for hCA II (K i ¼ 0.084 mM) showed the highest inhibitory activity compared to the rest of the analogues [208].…”

Section: Carbonic Anhydrase Inhibitionmentioning

confidence: 93%

Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review

Zhao

Rakesh

Ravidar

et al. 2019

European Journal of Medicinal Chemistry

406

183

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a b s t r a c tSulfur (S VI ) based moieties, especially, the sulfonyl or sulfonamide based analogues have showed a variety of pharmacological properties, and its derivatives propose a high degree of structural diversity that has established useful for the finding of new therapeutic agents. The developments of new less toxic, low cost and highly active sulfonamides containing analogues are hot research topics in medicinal chemistry. Currently, more than 150 FDA approved Sulfur (S VI )-based drugs are available in the market, and they are widely used to treat various types of diseases with therapeutic power. This comprehensive review highlights the recent developments of sulfonyl or sulfonamides based compounds in huge range of therapeutic applications such as antimicrobial, anti-inflammatory, antiviral, anticonvulsant, antitubercular, antidiabetic, antileishmanial, carbonic anhydrase, antimalarial, anticancer and other medicinal agents. We believe that, this review article is useful to inspire new ideas for structural design and developments of less toxic and powerful Sulfur (S VI ) based drugs against the numerous death-causing diseases.

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“…Almost all substances display their toxic effects in a similar way. Particularly, some enzymes are called as drug-target such as carbonic anhydrase, paraoxonase and sorbitol dehydrogenase (Mert et al, 2016;Alım and Beydemir 2016;Aslan And Beydemir, 2017). Antibiotics are indispensable drugs especially for the treatment of bacterial infections.…”

Section: Nad+ Nadh + H+mentioning

confidence: 99%

Alcohol Dehydrogenase from Sheep Liver: Purification, Characterization and Impacts of Some Antibiotics

Demir¹,

Şengül²,

Erğun³

et al. 2017

jist

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Alcohol dehydrogenase (ADH) is a dimeric enzyme in which each subunit of the enzyme has a Zn 2+ metal-containing catalytic domain and a cofactor-binding domain. This enzyme converts the alcohol to aldehyde. The present article focuses on the purification, characterization and in vitro effects of some antibiotics on alcohol dehydrogenase from sheep liver. ADH was purified with specific activity of 0.5 U/mg proteins and approximately 52.03-fold from sheep liver by DEAE-Sephadex A-50 ion exchange chromatography and gel filtration on Sephadex G-100. The subunit and the natural molecular weights of the enzyme were determined by gel filtration and SDS-PAGE 80.49 and 38.16 kDa, respectively. The optimum ionic strenght, temperature and, pH of ADH was 400 mM, 40°C and, 10.5, respectively. The inhibitory effects of the antibiotics were tested at various concentrations. IC 50 values for kanamycin sulfate, amikacin sulfate, gentamicin, lincomycin, and clindamycin were found to be 43. 31, 36.47, 20.38, 18.73 and 1.31 mM, respectively.

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The synthesis of novel pyrazole-3,4-dicarboxamides bearing 5-amino-1,3,4-thiadiazole-2-sulfonamide moiety with effective inhibitory activity against the isoforms of human cytosolic carbonic anhydrase I and II

Cited by 19 publications

References 56 publications

Microwave‐assisted synthesis of 1‐substituted‐1H‐benzimidazolium salts: Non‐competitive inhibition of human carbonic anhydrase I and II

Microwave‐assisted synthesis of 1‐substituted‐1H‐benzimidazolium salts: Non‐competitive inhibition of human carbonic anhydrase I and II

Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review

Alcohol Dehydrogenase from Sheep Liver: Purification, Characterization and Impacts of Some Antibiotics

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