Design, synthesis, and pharmacological evaluation of piperidin-4-yl amino aryl sulfonamides: novel, potent, selective, orally active, and brain penetrant 5-HT6 receptor …

…, A Shinde, A Daulatabad, R Kambhampati…

文献索引：Nirogi, Ramakrishna; Shinde, Anil; Daulatabad, Anand; Kambhampati, Ramasastri; Gudla, Parandhama; Shaik, Mohammad; Gampa, Muralimohan; Balasubramaniam, Suresh; Gangadasari, Pamuletinarasimhareddy; Reballi, Veena; Badange, Rajeshkumar; Bojja, Kumar; Subramanian, Ramkumar; Bhyrapuneni, Gopinadh; Muddana, Nageswararao; Jayarajan, Pradeep Journal of Medicinal Chemistry, 2012 , vol. 55, # 21 p. 9255 - 9269,15

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被引用次数: 16

摘要

Our initial findings around aryl sulfonamide series led to N-(3, 5-dichloro-2-methoxyphenyl)- 3-(1-methylpiperidin-4-ylamino)-4-methoxy benzenesulfonamide as potent and selective 5- HT6 receptor (5-HT6R) antagonist with reasonable pharmacokinetic properties and activity in animal models of cognition. However, lack of brain penetration and P-glycoprotein liability makes this scaffold unsuitable for further development. Our goal was to identify small ...