Author： Kambhampati Ramasastri Konda Jagadishbabu Reballi Veena Shinde Anil Dubey Pramod Nirogi Ramakrishna
Publisher： Informa Healthcare
ISSN： 1475-6366
Source： Journal of Enzyme Inhibition and Medicinal Chemistry, Vol.23, Iss.3, 2008-06, pp. : 302-312
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Abstract
The synthesis and potential 5-hydroxytryptamine6 receptor (5-HT6R) antagonist activity of a novel series of N-arylsulfonyl-3-(2-N,N-dimethylaminoethylthio) indoles has been reported. The molecular modeling, synthesis and in-vitro radioligand binding data of this series are discussed. The present article describes 37 derivatives of the title series. It was observed that the increased side-chain length with the insertion of a sulfur atom did not lead to the loss of binding affinity of these compounds, although the affinities were reduced. The compounds exhibited moderate affinity and selectivity to human 5-HT6 receptors.
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