87013-80-7

Upstream product

• 41104-55-6 4-(sulfonylphenyl)carbamic acid ethyl ester 
• 5657-41-0 N³-(4-sulfamoylphenyl)urea 
• 63-74-1 sulfanilamide 
• 41104-56-7 phenyl (4-sulfamoylphenyl)carbamate 

Downstream Products

• 87013-81-8 p-<(3,5-dimethylpyrazol-1-yl)carbamoyl>benzenesulfonamide 

Relevant academic research and scientific papers

Aryl-4,5-dihydro-1H-pyrazole-1-carboxamide derivatives bearing a sulfonamide moiety show single-digit nanomolar-to-subnanomolar inhibition constants against the tumor-associated human carbonic anhydrases IX and XII

A series of new 3-phenyl-5-aryl-N-(4-sulfamoylphenyl)-4,5-dihydro-1H-pyrazole-1-carboxamide derivatives was designed here, synthesized, and studied for carbonic anhydrase (CAs, EC 4.2.1.1) inhibitory activity against the human (h) isozymes I, II, and VII (cytosolic, off-target isoforms), and IX and XII (anticancer drug targets). Generally, CA I was not effectively inhibited, whereas effective inhibitors were identified against both CAs II (KIs in the range of 5.2-233 nM) and VII (KIs in the range of 2.3-350 nM). Nonetheless, CAs IX and XII were the most susceptible isoforms to this class of inhibitors. In particular, compounds bearing an unsubstituted phenyl ring at the pyrazoline 3 position showed 1.3-1.5 nM KIs against CA IX. In contrast, a subset of derivatives having a 4-halo-phenyl at the same position of the aromatic scaffold even reached subnanomolar KIs against CA XII (0.62-0.99 nM). Docking studies with CA IX and XII were used to shed light on the derivative binding mode driving the preferential inhibition of the tumor-associated CAs. The identified potent and selective CA IX/XII inhibitors are of interest as leads for the development of new anticancer strategies.

Inhibition of carbonic anhydrase isoforms I, II, IX and XII with Schiff's bases incorporating iminoureido moieties

A series of new Schiff's bases was obtained from the sulfanilamide semicarbazone (4-aminosulfonylphenyl semicarbazide) and aromatic/heterocyclic aldehydes. The new compounds were designed to incorporate moieties known to induce effective inhibitory activi

Carbonic anhydrase inhibitors: Design, synthesis, and biological evaluation of novel sulfonyl semicarbazide derivatives

A series of novel sulfonyl semicarbazides 5-13 was designed, synthesized, and evaluated for human carbonic anhydrase (hCA) inhibition. The new sulfonyl semicarbazides were tested against a panel of hCA isoforms I, II, IX, and XII, using acetazolamide (AZA

Synthesis and characterization of vanillin semicarbazones

Semicarbazones have a great interest because of their chemistry and biological activities for the treatment of various human ailments. A series of seven vanillin semicarbazones (3a-g) were synthesized by reflux of aryl semicarbazides with appropriate carbonyl compound in the presence of glacial acetic acid. The aryl semicarbazides (2a-g) were synthesized from aryl carbamates by reacting with hydrazine hydrate and ethanol on hydrazinolysis. The aryl carbamates (1a-g) were obtained by the reaction between phenyl chloro formate and aniline/substituted aniline in anhydrous ether in the presence of sodium hydroxide. The structure of the newly synthesized compounds was established by various analytical techniques such as IR, 1H NMR and MASS spectral studies.

4-Sulphamoylphenyl semicarbazones with anticonvulsant activity

A series of 4-sulphamoylphenyl semicarbazone derivatives were prepared starting from sulphanilamide and screened for anticonvulsant activity. The results indicated that greater protection was obtained in the maximal electroshock screen (MES) and subcutane

Synthesis and biological evaluations of sulfa derivatives bearing heterocyclic moieties.

Some new sulfa derivatives bearing a heterocyclic moieties fural, pyrimidinone, thiazolidinone, benzimidazole and 1,2,4-triazinone and the related compounds 2-19 have been synthesized from treatment of sulfa drugs with thioisocyanate, acid chlorides, 3-chloro-1,2,4-triazines, aldehydes, esters and/or 2-methylbenzoxazole followed by ring closure reactions. Structures of the products have been deduced from their elemental analysis and spectral data. Significant antimicrobial activities were observed in vitro for some members of the series. Compounds 9b, 16 are highly active, while compounds 4b, 6d, 7,9a, 10 and 14 showing a moderate active towards gramme positive bacterium (b.subtilis). gramme negative bacterium (E. coli) and two fungi namely (A.nidulans & A.terreus).

Antidiabetic activity of some 1-substituted 3,5-dimethylpyrazoles

Several new 1-substituted 3,5-dimethylpyrazoles were prepared for testing as hypoglycemic agents. A number of these containing para-substituted 1-carbonylphenylurea and para-substituted 1-carbamoylbenzenesulfonylurea derivatives were found to possess potent hypoglycemic activity.