An efficient method for the synthesis of novel derivatives 4-{5-[4-(4-amino-5-mercapto-4H-[1,2,4]triazol-3-yl)-phenyl]-3-trifluoromethyl-pyrazol-1-yl}-benzenesulfonamide and their anti-inflammatory potential. 2019

Ghulam Mustafa, and Andrea Angeli, and Muhammad Zia-Ur-Rehman, and Nosheen Akbar, and Saiqa Ishtiaq, and Claudiu T Supuran
Department of Chemistry, Hafiz Hayat Campus, University of Gujrat, Gujrat, Pakistan.

The present work describe the synthesis of a novel series of celecoxib derivatives (6a-m) and they were evaluated as Carbonic Anhydrase (CA, EC 4.2.1.1) inhibitors against the human (h) isoforms hCA I, II, IV and IX which are involved in a variety of diseases such as glaucoma, retinitis pigmentosa, epilepsy and tumors etc. These compounds showed interesting inhibitory activity for these isoforms, with several low nanomolar derivatives identified against all these enzymes. The in-vivo anti-inflammatory activity of the synthesized compounds were evaluated using Celecoxib as reference standard by paw Oedema model on albino Wistar. Most of the compounds showed higher in-vivo anti-inflammatory activity compared to Celecoxib.

UI MeSH Term Description Entries
D007527 Isoenzymes Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics. Alloenzyme,Allozyme,Isoenzyme,Isozyme,Isozymes,Alloenzymes,Allozymes
D008297 Male Males
D011720 Pyrazoles Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
D002256 Carbonic Anhydrases A family of zinc-containing enzymes that catalyze the reversible hydration of carbon dioxide. They play an important role in the transport of CARBON DIOXIDE from the tissues to the LUNG. EC 4.2.1.1. Carbonate Dehydratase,Carbonic Anhydrase,Anhydrases, Carbonic,Dehydratase, Carbonate
D002257 Carbonic Anhydrase Inhibitors A class of compounds that reduces the secretion of H+ ions by the proximal kidney tubule through inhibition of CARBONIC ANHYDRASES. Carbonate Dehydratase Inhibitor,Carbonate Dehydratase Inhibitors,Carbonic Anhydrase Inhibitor,Carboxyanhydrase Inhibitor,Carboxyanhydrase Inhibitors,Anhydrase Inhibitor, Carbonic,Dehydratase Inhibitor, Carbonate,Inhibitor, Carbonate Dehydratase,Inhibitor, Carbonic Anhydrase,Inhibitor, Carboxyanhydrase,Inhibitors, Carbonate Dehydratase,Inhibitors, Carbonic Anhydrase,Inhibitors, Carboxyanhydrase
D004305 Dose-Response Relationship, Drug The relationship between the dose of an administered drug and the response of the organism to the drug. Dose Response Relationship, Drug,Dose-Response Relationships, Drug,Drug Dose-Response Relationship,Drug Dose-Response Relationships,Relationship, Drug Dose-Response,Relationships, Drug Dose-Response
D004487 Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE. Dropsy,Hydrops,Anasarca
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000096926 Benzenesulfonamides A group of compounds that contain sulfonamide group S-linked to a benzene ring. Many benzenesulfonamide derivatives are pharmaceuticals (e.g., BOSENTAN; SULFAPYRIDINE; and SULFADIAZINE; CELECOXIB) as their sulfonamide moiety target various enzymes (e.g., CARBONIC ANHYDRASES; ACETYLCHOLINESTERASE; BUTYRYLCHOLINESTERASE; and CYCLOOXYNENASE 2). Benzenesulfonamide,Benzenesulfonamide Derivatives,Benzenesulfonamide Monosodium Salt,Benzenesulphonamides,Benzosulfonamides
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia

Related Publications

Ghulam Mustafa, and Andrea Angeli, and Muhammad Zia-Ur-Rehman, and Nosheen Akbar, and Saiqa Ishtiaq, and Claudiu T Supuran
January 2011, Acta crystallographica. Section E, Structure reports online,
Ghulam Mustafa, and Andrea Angeli, and Muhammad Zia-Ur-Rehman, and Nosheen Akbar, and Saiqa Ishtiaq, and Claudiu T Supuran
September 2012, Acta crystallographica. Section E, Structure reports online,
Ghulam Mustafa, and Andrea Angeli, and Muhammad Zia-Ur-Rehman, and Nosheen Akbar, and Saiqa Ishtiaq, and Claudiu T Supuran
January 2009, Acta crystallographica. Section E, Structure reports online,
Ghulam Mustafa, and Andrea Angeli, and Muhammad Zia-Ur-Rehman, and Nosheen Akbar, and Saiqa Ishtiaq, and Claudiu T Supuran
May 2012, Acta crystallographica. Section E, Structure reports online,
Ghulam Mustafa, and Andrea Angeli, and Muhammad Zia-Ur-Rehman, and Nosheen Akbar, and Saiqa Ishtiaq, and Claudiu T Supuran
July 2008, Acta crystallographica. Section E, Structure reports online,
Ghulam Mustafa, and Andrea Angeli, and Muhammad Zia-Ur-Rehman, and Nosheen Akbar, and Saiqa Ishtiaq, and Claudiu T Supuran
March 2016, Spectrochimica acta. Part A, Molecular and biomolecular spectroscopy,
Ghulam Mustafa, and Andrea Angeli, and Muhammad Zia-Ur-Rehman, and Nosheen Akbar, and Saiqa Ishtiaq, and Claudiu T Supuran
June 2015, Acta crystallographica. Section E, Crystallographic communications,
Ghulam Mustafa, and Andrea Angeli, and Muhammad Zia-Ur-Rehman, and Nosheen Akbar, and Saiqa Ishtiaq, and Claudiu T Supuran
December 2007, Acta crystallographica. Section E, Structure reports online,
Ghulam Mustafa, and Andrea Angeli, and Muhammad Zia-Ur-Rehman, and Nosheen Akbar, and Saiqa Ishtiaq, and Claudiu T Supuran
August 2011, Acta crystallographica. Section E, Structure reports online,
Ghulam Mustafa, and Andrea Angeli, and Muhammad Zia-Ur-Rehman, and Nosheen Akbar, and Saiqa Ishtiaq, and Claudiu T Supuran
November 2008, Acta crystallographica. Section E, Structure reports online,
Copied contents to your clipboard!