Spirocyclic sulfonamides with carbonic anhydrase inhibitory and anti-neuropathic pain activity |
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Institution: | 1. Department of Chemistry, GITAM School of Science, GITAM (Deemed to be University), Rudraram, Sangareddy, Hyderabad, Telangana, 502329, India;2. Nirmala College of Pharmacy, Mangalagiri, Andhra Pradesh, India;3. Dr. Reddy''s Institute of Life Sciences, University of Hyderabad Campus, Hyderabad 500046, India |
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Abstract: | A novel series of 4-oxo-spirochromane bearing primary sulfonamide group were synthetized as Carbonic Anhydrase inhibitors (CAIs) and tested for their management of neuropathic pain. Indeed, CAs have been recently validated as novel therapeutic targets in neuropathic pain. All compounds, here reported, showed strong activity against hCA II and hCA VII with KI values in the low or sub-nanomolar range. Two compounds (6d and 6l) showed good neuropathic pain attenuating effects and longer duration than drug reference acetazolamide in an animal model of oxaliplatin induced neuropathy. |
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Keywords: | Carbonic Anhydrases (CAs) Carbonic Anhydrase inhibitors (CAIs) Metalloenzymes Neuropathic pain |
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