Literature DB >> 24981843

Accelerating lead development by microwave-enhanced medicinal chemistry.

William D Shipe1, Scott E Wolkenberg1, Craig W Lindsley2.   

Abstract

Microwave-assisted organic synthesis (MAOS) addresses the need for accelerated chemical synthesis by providing many advantages over classical thermal conditions. Microwave instruments produced by Biotage, CEM and Milestone enable chemistry to be safely and reproducibly performed on various scales and in a parallel fashion. To illustrate the high utility of this technology for lead development, our Akt kinase program will be described wherein MAOS played a pivotal role in the identification of isozyme-selective Akt inhibitors.:
© 2005 Elsevier Ltd . All rights reserved.

Entities:  

Year:  2005        PMID： 24981843     DOI： 10.1016/j.ddtec.2005.05.002

Source DB:  PubMed          Journal:  Drug Discov Today Technol        ISSN： 1740-6749


  10 in total

1.  The flow synthesis of heterocycles for natural product and medicinal chemistry applications.

Authors:  Marcus Baumann; Ian R Baxendale; Steven V Ley
Journal:  Mol Divers       Date:  2010-10-20       Impact factor: 2.943

Review 2.  Controlled microwave heating in modern organic synthesis: highlights from the 2004-2008 literature.

Authors:  C Oliver Kappe; Doris Dallinger
Journal:  Mol Divers       Date:  2009-04-21       Impact factor: 2.943

3.  Recent advances in the design and development of novel negative allosteric modulators of mGlu(5).

Authors:  Kyle A Emmitte
Journal:  ACS Chem Neurosci       Date:  2011-08-17       Impact factor: 4.418

4.  (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction.

Authors:  Craig W Lindsley; Brittney S Bates; Usha N Menon; Satyawan B Jadhav; Alexander S Kane; Carrie K Jones; Alice L Rodriguez; P Jeffrey Conn; Christopher M Olsen; Danny G Winder; Kyle A Emmitte
Journal:  ACS Chem Neurosci       Date:  2011-08-17       Impact factor: 4.418

5.  Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.

Authors:  Andrew S Felts; Sam A Saleh; Uyen Le; Alice L Rodriguez; C David Weaver; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2009-10-09       Impact factor: 2.823

6.  Novel microwave-assisted synthesis of the immunomodulator organotellurium compound ammonium trichloro(dioxoethylene-O,O')tellurate (AS101).

Authors:  M Pilar Vázquez-Tato; Alberto Mena-Menéndez; Xesús Feás; Julio A Seijas
Journal:  Int J Mol Sci       Date:  2014-02-21       Impact factor: 5.923

Review 7.  MAOS and medicinal chemistry: some important examples from the last years.

Authors:  Nailton M Nascimento-Júnior; Arthur E Kümmerle; Eliezer J Barreiro; Carlos A M Fraga
Journal:  Molecules       Date:  2011-11-07       Impact factor: 4.411

8.  A facile and efficient synthesis of diaryl amines or ethers under microwave irradiation at presence of KF/Al2O3 without solvent and their anti-fungal biological activities against six phytopathogens.

Authors:  Liang-Zhu Huang; Pan Han; You-Qiang Li; Ying-Meng Xu; Tao Zhang; Zhen-Ting Du
Journal:  Int J Mol Sci       Date:  2013-09-12       Impact factor: 5.923

9.  Synthesis of gamma-nitro aliphatic methyl esters via Michael additions promoted by microwave irradiation.

Authors:  Jaime Escalante; Francisco D Díaz-Coutiño
Journal:  Molecules       Date:  2009-04-21       Impact factor: 4.411

10.  Optimizing the Synthetic Route of Chromone-2-carboxylic Acids: A Step forward to Speed-Up the Discovery of Chromone-Based Multitarget-Directed Ligands.

Authors:  Fernando Cagide; Catarina Oliveira; Joana Reis; Fernanda Borges
Journal:  Molecules       Date:  2019-11-20       Impact factor: 4.411
  10 in total

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