Synthesis, characterization and antiglaucoma activity of some novel pyrazole derivatives of 5-amino-1,3,4-thiadiazole-2-sulfonamide

Heterocyclic compounds as carbonic anhydrase inhibitor

“…A number of side effects of this drug are however experienced such as numbness and tingling in the fingers and toes, taste alterations, blurred vision, kidney stones, and an increase in urination 21 . To overcome these side effects Rahmi et al 22 synthesized various novel pyrazole carboxylic acid derivatives of 5-amino-1-,3,4-thiadiazole-2-sulfonamide, [2a-b, 3, 4a-g]. They also reported the inhibitory effects of all newly synthesized amides on hydratase and esterase activities of carbonic anhydrase isoenzymes (hCA-I and hCA-II) in vitro.…”

“…Brzozowski et al 29 synthesized a series of novel 4-substituted-3-pyridinesulfonamides [14][15][16][17][18][19][20][21][22] and [23a-c] and investigated as inhibitors of five isoforms of zinc enzyme carbonic anhydrase that is, the cytosolic, ubiquitous isozymes CA I and II, and transmembrane isozymes CA IX, XII (cancer-associated) and XIV. The newly synthesized compounds showed inhibition constants in the range of 0.078-11.7 μM.…”

Inhibitory effect of novel pyrazole carboxamide derivatives on human carbonic anhydrase enzyme

“…In order to reduce the side effects of acetazolamide, alternative sulfonamide derivatives have been investigated 14,15 . This study was conducted in order to design, synthesize, characterize and evaluate the biological activity of 4-benzoyl-1-(3-nitrophenyl)-5-phenyl-N-(4-sulfamoylphenyl)-1H-pyrazole-3-carboxamide (2) and its derivatives in order to extend our previous researches in synthesizing novel pyrazole derivatives 16,17 . In this current attempt, our main aim has been to check whether the new derivatives studied during the course of the current work could show even stronger inhibition effect on CA enzymes, with respect to the compounds previously investigated by our group 16,17 .…”

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“…Fluorine incorporated benzothiazole and 1,3,4 -thiadiazole derivatives individually known to possess a variety of biological properties like anti-microbial 1 , anti-inflammatory 2 , anti-tumor 3 , anti-viral 4 , antitubercular 5 , anti-convulsant 6 , anthelmintic 7 , antioxidants 8 , anti-diabetic 9 , diuretic 10 , analgesic 11 anti-depressants 12 , etc., It was felt interesting to bring these two biologically active moieties within a molecular frame work with a view to study their additive effect on biological properties.…”

“…In the mass spectrum of the synthesized compounds produced (M 10 , and SH 11 respectively corresponds to their molecular formulas.…”