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Title

Effects of the incorporation of IBTM β-turn mimetics into the dipeptoid CCK1 receptor agonist PD 170292

AuthorsMartín-Martínez, Mercedes CSIC ORCID; Latorre, Miriam; García-López, M. Teresa CSIC ; Cenarruzabeitia, Edurne CSIC; Río, Joaquín del CSIC; González-Muñiz, Rosario CSIC ORCID
Issue Date21-Jan-2002
PublisherElsevier
CitationBioorganic and Medicinal Chemistry Letters 12(2): 109-112 (2002)
AbstractReplacement of the 2-Adoc-d-αMeTrp residue in the non-selective CCK1 receptor agonist PD 170292 by the Z-(2R,5R,11bS)-IBTM skeleton, able to fix a type II β-turn-like conformation, led to a conformationally restricted dipeptoid analogue, namely 3a, which exhibited a notable increase in the CCK1 selectivity and antagonist properties. Replacement of the 2-Adoc-d-αMeTrp residue in the non-selective CCK1 receptor agonist PD 170292 by the Z-(2R,5R,11bS)-IBTM skeleton, able to fix a type II β-turn-like conformation, led to a conformationally restricted dipeptoid analogue, namely 3a, which exhibited a notable increase in the CCK1 selectivity and antagonist properties.
Publisher version (URL)http://dx.doi.org/10.1016/S0960-894X(01)00630-8
URIhttp://hdl.handle.net/10261/336145
DOI10.1016/S0960-894X(01)00630-8
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