| Literature DB >> 11133079 |
A J Souers1, A Rosenquist, E M Jarvie, M Ladlow, W Feniuk, J A Ellman.
Abstract
Constrained analogues 5-7 of the potent and subtype selective somatostatin mimetic 1 were prepared by incorporating conformational constraints into the nine-membered heterocyclic scaffold. Each constrained peptidomimetic showed an altered activity profile relative to lead compound 1, with compound 7 exhibiting a 25-fold and 2-fold binding enhancement against somatostatin receptor subtypes sst4 and sst5, respectively.Mesh:
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Year: 2000 PMID: 11133079 DOI: 10.1016/s0960-894x(00)00552-7
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823