Literature DB >> 18207394

Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.

Chen Chen1, Brian Dyck, Beth A Fleck, Alan C Foster, Jonathan Grey, Florence Jovic, Michael Mesleh, Kasey Phan, Junko Tamiya, Troy Vickers, Mingzhu Zhang.   

Abstract

Derivatives of milnacipran were synthesized and studied as monoamine transporter inhibitors. Potent analogs were discovered at NET (9k) and at both NET and SERT (9s and 9u). A pharmacophore model was established based on the conformational analysis of milnacipran in aqueous solution using NMR techniques and was consistent with the SAR results.

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Year:  2008        PMID: 18207394     DOI: 10.1016/j.bmcl.2008.01.011

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


  3 in total

Review 1.  Monoamine transporter structure, function, dynamics, and drug discovery: a computational perspective.

Authors:  Sankar Manepalli; Christopher K Surratt; Jeffry D Madura; Tammy L Nolan
Journal:  AAPS J       Date:  2012-08-24       Impact factor: 4.009

2.  P450-catalyzed asymmetric cyclopropanation of electron-deficient olefins under aerobic conditions.

Authors:  Hans Renata; Z Jane Wang; Rebekah Z Kitto; Frances H Arnold
Journal:  Catal Sci Technol       Date:  2014-10-02       Impact factor: 6.119

3.  Structural basis of norepinephrine recognition and transport inhibition in neurotransmitter transporters.

Authors:  Shabareesh Pidathala; Aditya Kumar Mallela; Deepthi Joseph; Aravind Penmatsa
Journal:  Nat Commun       Date:  2021-04-13       Impact factor: 14.919

  3 in total

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