Title : Design synthesis and pharmacological evaluation of sulfonamide derivatives of Indole and Benzopyran as 5HT6R antagonists

Type of Material: Thesis
Title: Design synthesis and pharmacological evaluation of sulfonamide derivatives of Indole and Benzopyran as 5HT6R antagonists
Researcher: Rajesh Kumar B.
Guide: Ramakrishna N V S, Mukkanti K
Department: Department of Chemistry
Publisher: Jawaharlal Nehru Technological University, Hyderabad
Place: Hyderabad
Year: 2016
Language: English
Subject: Benzopyran
Chemistry
Chemistry Multidisciplinary
Indole
Physical Sciences
Sulfonamide derivatives
Dissertation/Thesis Note: PhD; Department of Chemistry, Jawaharlal Nehru Technological University, Hyderabad, Hyderabad; 2016
Fulltext: Shodhganga

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035__|a(IN-AhILN)th_454282
040__|aJNTU_500028|dIN-AhILN
041__|aeng
100__|aRajesh Kumar B.|eResearcher
110__|aDepartment of Chemistry|bJawaharlal Nehru Technological University, Hyderabad|dHyderabad|ein|0U-0017
245__|aDesign synthesis and pharmacological evaluation of sulfonamide derivatives of Indole and Benzopyran as 5HT6R antagonists
260__|aHyderabad|bJawaharlal Nehru Technological University, Hyderabad|c2016
300__|a216p.|dDVD
502__|bPhD|cDepartment of Chemistry, Jawaharlal Nehru Technological University, Hyderabad, Hyderabad|d2016
518__|oDate of Award|dMay 2016
518__|oDate of Registration|d2008-01-01
520__|aThe theme of the research work is design and synthesis of novel molecules which have a potent affinity towards 5-HT6 receptors. Based on this concept, design and synthesis of novel (3-halo)-4-(piperazin-1-yl methyl)-N1-arylsulfonyl-1H-indole derivatives, [3-[(1-methylpiperidin-4-yl) methyl] arylsulfonyl]-1H-indole derivatives and (spiro)benzopyran derivatives was undertaken and evaluated the in-vitro activity of these derivatives. 4-(Piperazin-1-yl methyl)-N1-arylsulfonyl-1H-indole derivatives were found to have moderate to potent affinity towards 5-HT6 receptors. So some select compounds from this series were taken up for further evaluation in in-vivo animal studies. They have good selectivity over other closely related receptors and no CYP liabilities. These derivatives were further profiled in animal models of cognition like Object Recognition Test (ORT). Oral administration of these compounds has shown improvement in performance of rats in ORT indicating cognitive improvement potential of them.newline
653__|aBenzopyran
653__|aChemistry
653__|aChemistry Multidisciplinary
653__|aIndole
653__|aPhysical Sciences
653__|aSulfonamide derivatives
700__|aRamakrishna N V S, Mukkanti K|eGuide
856__|uhttp://shodhganga.inflibnet.ac.in/handle/10603/292969|yShodhganga
905__|afromsg

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