Literature DB >> 18445525

Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.

Junko Tamiya1, Brian Dyck, Mingzhu Zhang, Kasey Phan, Beth A Fleck, Anna Aparicio, Florence Jovic, Joe A Tran, Troy Vickers, Jonathan Grey, Alan C Foster, Chen Chen.   

Abstract

A series of milnacipran analogs were synthesized and studied as monoamine transporter inhibitors, and several potent compounds with moderate lipophilicity were identified from the 1S,2R-isomers. Thus, 15l exhibited IC(50) values of 1.7nM at NET and 25nM at SERT, which were, respectively, 20- and 13-fold more potent than 1S,2R-milnacipran 1-II.

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Year:  2008        PMID: 18445525     DOI: 10.1016/j.bmcl.2008.04.025

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


  1 in total

1.  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

  1 in total

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