Literature DB >> 19167884

The design and discovery of novel amide CCR5 antagonists.

David C Pryde1, Martin Corless, David R Fenwick, Helen J Mason, Blanda C Stammen, Peter T Stephenson, David Ellis, David Bachelor, David Gordon, Christopher G Barber, Anthony Wood, Donald S Middleton, David C Blakemore, Gemma C Parsons, Rachel Eastwood, Michelle Y Platts, Keith Statham, Kerry A Paradowski, Catherine Burt, Wolfgang Klute.   

Abstract

The synthesis of a range of novel amine-containing structures and their primary potency as inhibitors of HIV-1 fusion via blocking of the CCR5 receptor is described. The development of the medicinal chemistry strategy and SAR's which led to the identification of the piperidine amide compounds 33 and 36 as excellent leads for further evaluation is described, along with key physicochemical data which highlighted their lead potential.

Entities:  

Mesh:

Substances:

Year:  2009        PMID: 19167884     DOI: 10.1016/j.bmcl.2009.01.012

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


  3 in total

Review 1.  CCR5 receptor antagonists in preclinical to phase II clinical development for treatment of HIV.

Authors:  Michelle B Kim; Kyle E Giesler; Yesim A Tahirovic; Valarie M Truax; Dennis C Liotta; Lawrence J Wilson
Journal:  Expert Opin Investig Drugs       Date:  2016-12       Impact factor: 6.206

2.  Design, Synthesis, and Optimization of Balanced Dual NK1/NK3 Receptor Antagonists.

Authors:  Stephen Hanessian; Thomas Jennequin; Nicolas Boyer; Vincent Babonneau; Udaykumar Soma; Clotilde Mannoury la Cour; Mark J Millan; Guillaume De Nanteuil
Journal:  ACS Med Chem Lett       Date:  2014-02-13       Impact factor: 4.345

3.  Discovery of Novel CCR5 Ligands as Anticolorectal Cancer Agents by Sequential Virtual Screening.

Authors:  Mariam A El-Zohairy; Darius P Zlotos; Martin R Berger; Hassan H Adwan; Yasmine M Mandour
Journal:  ACS Omega       Date:  2021-04-16
  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.