2. Academic Validation
  3. Design, synthesis and pharmacological evaluation of 4-(piperazin-1-yl methyl)-N₁-arylsulfonyl indole derivatives as 5-HT₆ receptor ligands

Design, synthesis and pharmacological evaluation of 4-(piperazin-1-yl methyl)-N₁-arylsulfonyl indole derivatives as 5-HT₆ receptor ligands

  • Bioorg Med Chem Lett. 2012 Dec 15;22(24):7431-5. doi: 10.1016/j.bmcl.2012.10.057.
Ramakrishna V S Nirogi 1,  Rajeshkumar Badange,  Ramasastri Kambhampati,  Anil Chindhe,  Amol D Deshpande,  Vinaykumar Tiriveedhi,  Vishwottam Kandikere,  Nageswararao Muddana,  Renny Abraham,  Mukkanti Khagga
Affiliations

Affiliation

  • 1 Discovery Research, Suven Life Sciences Limited, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India. nvsrk@suven.com
PMID: 23141912 DOI: 10.1016/j.bmcl.2012.10.057
Abstract

4-(Piperazin-1-yl methyl)-N(1)-arylsulfonyl indole derivatives were designed and synthesized as 5-HT(6) receptor (5-HT(6)R) ligands. The lead compound 6a, from this series shows potent in vitro binding affinity, good PK profile, no CYP liabilities and activity in animal models of cognition.

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