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Molecules 2017, 22(7), 1049; doi:10.3390/molecules22071049

Novel Sulfamide-Containing Compounds as Selective Carbonic Anhydrase I Inhibitors

1
NEUROFARBA Department, Sezione di Scienze Farmaceutiche e Nutraceutiche, Università degli Studi di Firenze, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Florence), Italy
2
Department of Biotechnology, Chemistry and Pharmacy, University of Siena, viale Aldo Moro 2, 53100 Siena, Italy
3
Sbarro Institute for Cancer Research and Molecular Medicine, Center for Biotechnology, College of Science 1.and Technology, Temple University, BioLife Science Building, Suite 333, 1900 N 12th Street, Philadelphia, PA 19122, USA
4
Center for Organic and Medicinal Chemistry, School of Advanced Sciences, VIT University, Vellore, 632014 Tamil Nadu, India
5
Department of Neurosciences, Psychology, Drug’s Research and Child’s Health (NEUROFARBA), University of Florence, Italy; Section of Pharmacology and Toxicology, viale Pieraccini 6, 50100 Firenze, Italy
These authors contributed equally.
These authors contributed equally.
*
Authors to whom correspondence should be addressed.
Received: 19 May 2017 / Revised: 12 June 2017 / Accepted: 19 June 2017 / Published: 24 June 2017
(This article belongs to the Special Issue Sulfonamides)
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Abstract

The development of isoform selective inhibitors of the carbonic anhydrase (CA; EC 4.2.1.1) enzymes represents the key approach for the successful development of druggable small molecules. Herein we report a series of new benzenesulfamide derivatives (-NH-SO2NH2) bearing the 1-benzhydrylpiperazine tail and connected by means of a β-alanyl or nipecotyl spacer. All compounds 6al were investigated in vitro for their ability to inhibit the physiological relevant human (h) CA isoforms such as I, II, IV and IX. Molecular modeling provided further structural support to enzyme inhibition data and structure-activity relationship. In conclusion the hCA I resulted the most inhibited isoform, whereas all the remaining ones showed different inhibition profiles. View Full-Text
Keywords: carbonic anhydrase inhibitors (CAIs); sulfamides; structure-activity-relationship (SAR) carbonic anhydrase inhibitors (CAIs); sulfamides; structure-activity-relationship (SAR)
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Berrino, E.; Bua, S.; Mori, M.; Botta, M.; Murthy, V.S.; Vijayakumar, V.; Tamboli, Y.; Bartolucci, G.; Mugelli, A.; Cerbai, E.; Supuran, C.T.; Carta, F. Novel Sulfamide-Containing Compounds as Selective Carbonic Anhydrase I Inhibitors. Molecules 2017, 22, 1049.

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