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 |
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| Institution: | 1. Department of Chemistry, Hafiz Hayat Campus, University of Gujrat, Gujrat, Pakistan;2. Department of University of Florence, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy;3. Applied Chemistry Research Centre, PCSIR Laboratories Complex, Ferozepur Road, Lahore 54600, Pakistan;4. Department of Physics, COMSATS University, Islamabad, Lahore Campus, Defence Road, Off-Raiwind Road, Lahore 54000, Pakistan;5. University College of Pharmacy, University of the Punjab, Lahore 54000, Pakistan;1. Departmentof Chemistry, Quaid-i-Azam University-45320, Islamabad, Pakistan;2. University of Florence, NEUROFARBA Department, Pharmaceutical and Nutraceutical Sciences Section, via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy;1. Department of Biothermodynamics and Drug Design, Institute of Biotechnology, Vilnius University, Saul?tekio al. 7, Vilnius LT-10257, Lithuania;2. Department of Organic Chemistry, Faculty of Chemistry and Geosciences, Vilnius University, Naugarduko 24, Vilnius LT-03225, Lithuania;1. Department of Chemistry, Kurukshetra University, Kurukshetra 136119, India;2. Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm 188, and Neurofarba Department, Sezione di Scienze Farmaceutiche, Via U. Schiff 6, I-50019 Sesto Fiorentino (Firenze), Italy;3. Istituto di Bioscienze e Biorisorse, CNR, Via PietroCastellino 111, 80131 Napoli, Italy;1. Saint Petersburg State University, Saint Petersburg 199034, Russian Federation;2. Department of Organic Chemistry, Faculty of Science, RUDN University, 117198, Russian Federation;3. The Ushinsky Yaroslavl State Pedagogical University, Yaroslavl 150000, Russian Federation;4. Department of Pharmacy, University of Pisa, 56126 Pisa, Italy;5. Neurofarba Department, Universita degli Studi di Firenze, Florence, Italy;1. University of Florence, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche e Nutraceutiche, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy;2. University of Pisa, Department of Pharmacy, Via Bonanno 6, 56126 Pisa, Italy;3. University of Florence, NEUROFARBA Dept., Sezione di Farmacologia e Tossicologia, Viale Gaetano Pieraccini 6, 50139 Florence, Italy;4. Institut des Biomolécules Max Mousseron (IBMM), UMR 5247 CNRS, ENSCM, Université de Montpellier, 240 avenue du Professeur Emile Jeanbrau, 34296 Montpellier Cedex 05, France;1. Department of Chemistry, Kurukshetra University, Kurukshetra, Haryana, 136119, India;2. Government College Bherian, Pehowa, Kurukshetra, Haryana, 136128, India;3. Ch. Mani Ram Godara Government College for Women, Bhodia Khera, Fatehabad, Haryana, 125050, India;4. NEUROFARBA Department, Pharmaceutical and Nutraceutical Section, University of Firenze, Via U. Schiff 6, 50019, Sesto Fiorentino, Firenze, Italy;5. NEUROFARBA Department, Pharmaceutical and Nutraceutical Section, Laboratory of Molecular Modeling Cheminformatics & QSAR, University of Firenze, Via U. Schiff 6, 50019, Sesto Fiorentino, Firenze, Italy |
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| Abstract: | 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. |
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| Keywords: | Sulphonamide Celecoxib Anti-inflammatory Carbonic anhydrase Metalloenzyme |
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