Literature DB >> 15863320

2,5-Diketopiperazines as potent and selective oxytocin antagonists 1: Identification, stereochemistry and initial SAR.

Paul G Wyatt1, Michael J Allen, Alan D Borthwick, Dave E Davies, Anne M Exall, Richard J D Hatley, Wendy R Irving, David G Livermore, Neil D Miller, Fabrizio Nerozzi, Steve L Sollis, Anna Katrin Szardenings.   

Abstract

This paper covers efforts to discover orally active potent and selective oxytocin antagonists. Screening pooled libraries identified a novel series of 2,5-diketopiperazine derivatives with antagonist activity at the human oxytocin receptor. We report the initial structure-activity relationship investigations and the determination of the stereochemistry of the most potent compounds.

Entities:  

Mesh:

Substances:

Year:  2005        PMID: 15863320     DOI: 10.1016/j.bmcl.2005.03.045

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  12 in total

Review 1.  Chemistry and biology of multicomponent reactions.

Authors:  Alexander Dömling; Wei Wang; Kan Wang
Journal:  Chem Rev       Date:  2012-03-22       Impact factor: 60.622

2.  Concise Two-Step Solution Phase Syntheses of four novel Dihydroquinazoline scaffolds.

Authors:  Justin Dietrich; Christine Kaiser; Nathalie Meurice; Christopher Hulme
Journal:  Tetrahedron Lett       Date:  2010-07-28       Impact factor: 2.415

3.  Rapid synthesis of diketopiperazine macroarrays via Ugi four-component reactions on planar solid supports.

Authors:  Qi Lin; Helen E Blackwell
Journal:  Chem Commun (Camb)       Date:  2006-07-21       Impact factor: 6.222

4.  Crystal structure of the human oxytocin receptor.

Authors:  Yann Waltenspühl; Jendrik Schöppe; Janosch Ehrenmann; Lutz Kummer; Andreas Plückthun
Journal:  Sci Adv       Date:  2020-07-15       Impact factor: 14.136

5.  Synthesis of Constrained Heterocycles Employing Two Post-Ugi Cyclization Methods for Rapid Library Generation with In Cellulo Activity.

Authors:  Nicholas McConnell; Zhigang Xu; Vishnu Kumarasamy; Daekyu Sun; Brendan Frett; Hong-Yu Li
Journal:  ChemistrySelect       Date:  2017-12-19       Impact factor: 2.109

6.  Efficient construction of diketopiperazine macroarrays through a cyclative-cleavage strategy and their evaluation as luminescence inhibitors in the bacterial symbiont Vibrio fischeri.

Authors:  Jennifer Campbell; Helen E Blackwell
Journal:  J Comb Chem       Date:  2009 Nov-Dec

Review 7.  Solid-phase and microwave-assisted syntheses of 2,5-diketopiperazines: small molecules with great potential.

Authors:  Jennifer C O'Neill; Helen E Blackwell
Journal:  Comb Chem High Throughput Screen       Date:  2007-12       Impact factor: 1.339

Review 8.  Isocyanide-based multicomponent reactions towards cyclic constrained peptidomimetics.

Authors:  Gijs Koopmanschap; Eelco Ruijter; Romano Va Orru
Journal:  Beilstein J Org Chem       Date:  2014-03-04       Impact factor: 2.883

Review 9.  Cyclic Dipeptides: The Biological and Structural Landscape with Special Focus on the Anti-Cancer Proline-Based Scaffold.

Authors:  Joanna Bojarska; Adam Mieczkowski; Zyta M Ziora; Mariusz Skwarczynski; Istvan Toth; Ahmed O Shalash; Keykavous Parang; Shaima A El-Mowafi; Eman H M Mohammed; Sherif Elnagdy; Maha AlKhazindar; Wojciech M Wolf
Journal:  Biomolecules       Date:  2021-10-14

10.  Morphology-Controlled Self-Assembly and Synthesis of Biopolyimide Particles from 4-Amino-l-phenylalanine.

Authors:  Thawinda Hirayama; Amit Kumar; Kenji Takada; Tatsuo Kaneko
Journal:  ACS Omega       Date:  2020-02-03
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.