Enhancing the pharmacodynamic profile of a class of selective COX-2 inhibiting nitric oxide donors |
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| Institution: | 1. Dipartimento di Chimica e Tecnologie del Farmaco, Università degli Studi di Roma “La Sapienza”, Piazzale Aldo Moro 5, 00185 Roma, Italy;2. Dipartimento di Biotecnologie, Chimica e Farmacia, Università degli Studi di Siena, Via A. Moro 2, 53100 Siena, Italy;3. Dipartimento di Farmacia, Università degli Studi di Pisa, Via Bonanno 6, 56126 Pisa, Italy;4. Dipartimento di Farmacia, Università degli Studi di Napoli “Federico II”, Via D. Montesano 49, 80131 Napoli, Italy;5. Dipartimento di Neurologia, Psicologia, Area del Farmaco e Salute del Bambino, Università degli Studi di Firenze, Viale G. Pieraccini 6, I-50139 Firenze, Italy;6. Rottapharm Madaus, Via Valosa di Sopra 7, 20052 Monza, Italy;7. Neuroscienze e Imaging, Università “G. d’Annunzio” di Chieti and CeSI, Via dei Vestini 31, 66100 Chieti, Italy;1. Department of Obstetrics and Gynecology, Second Affiliated Hospital of Southeast University, Nanjing 210003, China;2. Department of Obstetrics and Gynecology, Huai’an Maternal and Child Health Hospital, 223002, China;3. Department of Obstetrics and Gynecology, Affiliated Hospital of Xuzhou Medical College, Xuzhou 221006, China;1. Crop Protection Chemicals Division, CSIR-Indian Institute of Chemical Technology, Uppal Road, Tarnaka, Hyderabad 500007, India;2. AcSIR-IICT, CSIR-Indian Institute of Chemical Technology, Uppal Road, Tarnaka, Hyderabad 500007, India;3. Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Uppal Road, Tarnaka, Hyderabad 500007, India;1. Chemical Research, Glenmark Pharmaceuticals Limited, Glenmark Research Center, Navi Mumbai, Maharashtra 400709, India;2. Biological Research, Glenmark Pharmaceuticals Limited, Glenmark Research Center, Navi Mumbai, Maharashtra 400709, India;3. Drug Metabolism and Pharmacokinetics, Glenmark Pharmaceuticals Limited, Glenmark Research Center, Navi Mumbai, Maharashtra 400709, India;1. Eskitis Institute for Drug Discovery, Griffith University, Nathan, Queensland 4111, Australia;2. Department of Entomology, University of California, One Shields Avenue, Davis, CA 95616-8584, United States;3. Enamine Ltd, 78 Chervonotkatska Street, Kyiv 02094, Ukraine;4. School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece;5. Moscow Institute of Physics & Technology (State University) Dolgoprudny, Moscow Region 141700, Russia;6. Department of Chemistry, St. Petersburg State University, 26 Universitetskyi Prospekt, Peterhof 198504, Russia;1. Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China;2. Center of Drug Discovery, Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China;1. Department of Pharmaceutical Products, School of Pharmacy, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, MG, Brazil;2. Department of Chemistry, Institute of Exact Sciences, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, MG, Brazil;3. Department of Microbiology, Institute of Biological Sciences, Universidade Federal de Minas Gerais, 31270-901 Belo Horizonte, MG, Brazil |
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| Abstract: | We report herein the development, synthesis, physicochemical and pharmacological characterization of a novel class of pharmacodynamic hybrids that selectively inhibit cyclooxygenase-2 (COX-2) isoform and present suitable nitric oxide releasing properties. The replacement of the ester moiety with the amide group gave access to in vivo more stable and active derivatives that highlighted outstanding pharmacological properties. In particular, the glycine derivative proved to be extremely active in suppressing hyperalgesia and edema. |
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| Keywords: | CINODs Cyclooxygenases Coxibs 1 5-Diarylpyrroles Pharmacodynamic hybrids Nitric oxide |
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