Literature DB >> 20974533

Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 ion channel blockers. Part 2.

Curt D Haffner1, Stephen A Thomson, Yu Guo, Kimberly Petrov, Andrew Larkin, Pierette Banker, Gregory Schaaf, Scott Dickerson, Jeff Gobel, Dan Gillie, J Patrick Condreay, Chuck Poole, Tiffany Carpenter, John Ulrich.   

Abstract

We report the synthesis and in vitro activity of a series of novel substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs. These analogs showed potent inhibitory activity against Kv1.3. Several demonstrated similar potency to the known Kv1.3 inhibitor PAP-1 when tested under the IonWorks patch clamp assay conditions. Two compounds 13i and 13rr were advanced further as potential tool compounds for in vivo validation studies.
Copyright © 2010. Published by Elsevier Ltd.

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Year:  2010        PMID: 20974533     DOI: 10.1016/j.bmcl.2010.09.131

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


  4 in total

Review 1.  Discovery of KV 1.3 ion channel inhibitors: Medicinal chemistry approaches and challenges.

Authors:  Špela Gubič; Louise A Hendrickx; Žan Toplak; Maša Sterle; Steve Peigneur; Tihomir Tomašič; Luis A Pardo; Jan Tytgat; Anamarija Zega; Lucija P Mašič
Journal:  Med Res Rev       Date:  2021-05-01       Impact factor: 12.944

2.  N-(2-Oxo-2-phenyl-acet-yl)benzamide.

Authors:  Hoong-Kun Fun; Jia Hao Goh; Dongdong Wu; Yan Zhang
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-12-18

3.  Crystal structure of 4-methyl-N-[2-(piperidin-1-yl)eth-yl]benzamide monohydrate.

Authors:  B K Revathi; D Reuben Jonathan; S Sathya; K Prathebha; G Usha
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-04-30

4.  Cu(I)-catalyzed N,N'-diarylation of natural diamines and polyamines with aryl iodides.

Authors:  Svetlana Petrovna Panchenko; Alexei Dmitrievich Averin; Maksim Viktorovich Anokhin; Olga Aleksandrovna Maloshitskaya; Irina Petrovna Beletskaya
Journal:  Beilstein J Org Chem       Date:  2015-11-24       Impact factor: 2.883

  4 in total

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