Design, synthesis and preliminary screening of novel 3-(2-N,N-dimethylaminoethylthio) indole derivatives as potential 5-HT(6) receptor ligands |
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Authors: | Kambhampati Ramasastri Konda Jagadishbabu Reballi Veena Shinde Anil K Dubey Pramod K Nirogi Ramakrishna V S |
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Institution: | Medicinal Chemistry, Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Hyderabad, India. |
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Abstract: | The synthesis and potential 5-hydroxytryptamine(6) 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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