Literature DB >> 19773164

Synthesis and structure-activity relationships of 2-(1,4'-bipiperidin-1'-yl)thiazolopyridine as H3 receptor antagonists.

Ashwin U Rao1, Anandan Palani, Xiao Chen, Ying Huang, Robert G Aslanian, Robert E West, Shirley M Williams, Ren-Long Wu, Joyce Hwa, Christopher Sondey, Jean Lachowicz.   

Abstract

A series of 2-(1,4'-bipiperidine-1'-yl)thiazolopyridines was synthesized and evaluated as a new lead of non-imidazole histamine H(3) receptor antagonists. Introduction of diversity at the 6-position of the pyridine ring was designed to enhance in vitro potency and decrease hERG activity. The structure-activity relationships for these new thiazolopyridine antagonists are discussed.

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Year:  2009        PMID： 19773164     DOI： 10.1016/j.bmcl.2009.09.006

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


  7 in total

1.  Discovery of a potent thiadiazole class of histamine h3 receptor antagonist for the treatment of diabetes.

Authors:  Ashwin U Rao; Ning Shao; Robert G Aslanian; Tin-Yau Chan; Sylvia J Degrado; Li Wang; Brian McKittrick; Mary Senior; Robert E West; Shirley M Williams; Ren-Long Wu; Joyce Hwa; Bhuneshwari Patel; Shuqin Zheng; Christopher Sondey; Anandan Palani
Journal:  ACS Med Chem Lett       Date:  2011-11-21       Impact factor: 4.345

2.  Crystal structure of 2-(2-methyl-phen-yl)-1,3-thia-zolo[4,5-b]pyridine.

Authors:  Gamal A El-Hiti; Keith Smith; Amany S Hegazy; Saud A Alanazi; Benson M Kariuki
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-07-08

3.  Crystal structure of 2-(1-methyl-eth-yl)-1,3-thia-zolo[4,5-b]pyridine.

Authors:  Gamal A El-Hiti; Keith Smith; Amany S Hegazy; Saud A Alanazi; Benson M Kariuki
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-04-02

4.  Non-Imidazole Histamine H₃ Ligands. Part VII. Synthesis, In Vitro and In Vivo Characterization of 5-Substituted-2-thiazol-4-n-propylpiperazines.

Authors:  Roman Guryn; Marek Staszewski; Anna Stasiak; Daniel McNaught Flores; Wiesława Agnieszka Fogel; Rob Leurs; Krzysztof Walczyński
Journal:  Molecules       Date:  2018-02-03       Impact factor: 4.411

5.  Crystal structure of 2-tert-butyl-1,3-thia-zolo[4,5-b]pyridine.

Authors:  Gamal A El-Hiti; Keith Smith; Amany S Hegazy; Ali M Masmali; Benson M Kariuki
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-08-01

6.  Inhibitory Effects of KP-A159, a Thiazolopyridine Derivative, on Osteoclast Differentiation, Function, and Inflammatory Bone Loss via Suppression of RANKL-Induced MAP Kinase Signaling Pathway.

Authors:  Hye Jung Ihn; Doohyun Lee; Taeho Lee; Sang-Hyun Kim; Hong-In Shin; Yong Chul Bae; Jung Min Hong; Eui Kyun Park
Journal:  PLoS One       Date:  2015-11-04       Impact factor: 3.240

7.  Identification of Novel Thiazolo[5,4-b]Pyridine Derivatives as Potent Phosphoinositide 3-Kinase Inhibitors.

Authors:  Liang Xia; Yan Zhang; Jingbo Zhang; Songwen Lin; Kehui Zhang; Hua Tian; Yi Dong; Heng Xu
Journal:  Molecules       Date:  2020-10-12       Impact factor: 4.411
  7 in total

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