2. Academic Validation
  3. 2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists

2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists

  • Bioorg Med Chem Lett. 2003 Jul 21;13(14):2369-72. doi: 10.1016/s0960-894x(03)00403-7.
Michael D Ennis 1,  Robert L Hoffman,  Nabil B Ghazal,  Rebecca M Olson,  Christopher S Knauer,  Chris L Chio,  Deborah K Hyslop,  Jeffery E Campbell,  Lawrence W Fitzgerald,  Nanette F Nichols,  Kjell A Svensson,  Robert B McCall,  Christopher L Haber,  Michelle L Kagey,  Dac M Dinh
Affiliations

Affiliation

  • 1 Medicinal Chemistry III, Pharmacia Corporation, 301 Henrietta Street, 49009, Kalamazoo, MI, USA. d.ennis@pharmacia.com
PMID: 12824036 DOI: 10.1016/s0960-894x(03)00403-7
Abstract

The design and synthesis of the novel 2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,7-a]indole 5 is described. This azepinoindole has excellent affinity for 5-HT(2C) (K(i) 4.8 nM) and modest selectivity over 5-HT(2A) ( approximately 4-fold). Several N- and C(11)-substituted analogues of 5 were prepared, as were a number of biaryl indoline derivatives. The anxiolytic potential for the azepinoindole template 5 is demonstrated by activity in a mouse shock-aggression assay.

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