Literature DB >> 19748778

Pyrazole NNRTIs 4: selection of UK-453,061 (lersivirine) as a development candidate.

Charles E Mowbray1, Catherine Burt, Romuald Corbau, Simon Gayton, Michael Hawes, Manos Perros, Isabelle Tran, David A Price, Faye J Quinton, Matthew D Selby, Paul A Stupple, Rob Webster, Anthony Wood.   

Abstract

We prepared three discreet cohorts of potent non-nucleoside HIV reverse transcriptase inhibitors (NNRTIs) based on the recently reported 3-cyanophenoxypyrazole lead 3. Several of these compounds displayed very promising anti-HIV activity in vitro, safety, pharmacokinetic and pharmaceutical profiles. We describe our analysis and conclusions leading to the selection of alcohol 5 (UK-453,061, lersivirine) for clinical development.

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Year:  2009        PMID： 19748778     DOI： 10.1016/j.bmcl.2009.08.080

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


  10 in total

Review 1.  Nitrile-containing pharmaceuticals: efficacious roles of the nitrile pharmacophore.

Authors:  Fraser F Fleming; Lihua Yao; P C Ravikumar; Lee Funk; Brian C Shook
Journal:  J Med Chem       Date:  2010-08-30       Impact factor: 7.446

2.  A bulky biaryl phosphine ligand allows for palladium-catalyzed amidation of five-membered heterocycles as electrophiles.

Authors:  Mingjuan Su; Stephen L Buchwald
Journal:  Angew Chem Int Ed Engl       Date:  2012-03-30       Impact factor: 15.336

Review 3.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

4.  Docking-based 3D-QSAR analyses of pyrazole derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.

Authors:  Elena Cichero; Paola Fossa
Journal:  J Mol Model       Date:  2011-07-30       Impact factor: 1.810

5.  Hydrazine-mediated cyclization of Ugi products to synthesize novel 3-hydroxypyrazoles.

Authors:  Arthur Y Shaw; Jonathan A McLaren; Gary S Nichol; Christopher Hulme
Journal:  Tetrahedron Lett       Date:  2012-03-24       Impact factor: 2.415

Review 6.  Investigational reverse transcriptase inhibitors for the treatment of HIV.

Authors:  Theodore J Cory; Narasimha M Midde; Pss Rao; Santosh Kumar
Journal:  Expert Opin Investig Drugs       Date:  2015-06-19       Impact factor: 6.206

7.  Lersivirine, a nonnucleoside reverse transcriptase inhibitor with activity against drug-resistant human immunodeficiency virus type 1.

Authors:  Romuald Corbau; Julie Mori; Chris Phillips; Lesley Fishburn; Alex Martin; Charles Mowbray; Wendy Panton; Caroline Smith-Burchnell; Adele Thornberry; Heather Ringrose; Thorsten Knöchel; Steve Irving; Mike Westby; Anthony Wood; Manos Perros
Journal:  Antimicrob Agents Chemother       Date:  2010-07-26       Impact factor: 5.191

8.  Direct N-heterocyclization of hydrazines to access styrylated pyrazoles: synthesis of 1,3,5-trisubstituted pyrazoles and dihydropyrazoles.

Authors:  Vunnam Venkateswarlu; Jaspreet Kour; K A Aravinda Kumar; Praveen Kumar Verma; G Lakshma Reddy; Yaseen Hussain; Aliya Tabassum; Shilpi Balgotra; Sorav Gupta; Abhinandan D Hudwekar; Ram A Vishwakarma; Sanghapal D Sawant
Journal:  RSC Adv       Date:  2018-07-24       Impact factor: 4.036

9.  A new class of heterocycles: 1,4,3,5-oxathiadiazepane 4,4-dioxides.

Authors:  Amel Bendjeddou; Tahar Abbaz; Zine Regainia; Nour-Eddine Aouf
Journal:  Molecules       Date:  2012-02-14       Impact factor: 4.411

10.  Prioritization of anti-malarial hits from nature: chemo-informatic profiling of natural products with in vitro antiplasmodial activities and currently registered anti-malarial drugs.

Authors:  Samuel Ayodele Egieyeh; James Syce; Sarel F Malan; Alan Christoffels
Journal:  Malar J       Date:  2016-01-29       Impact factor: 2.979
  10 in total

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