Literature DB >> 15210156

Synthesis and binding properties of novel selective 5-HT3 receptor ligands.

Maria Modica1, Giuseppe Romeo, Luisa Materia, Filippo Russo, Alfredo Cagnotto, Tiziana Mennini, Róbert Gáspár, George Falkay, Ferenc Fülöp.   

Abstract

This work reports on the synthesis and affinities for the 5-HT(3) versus the 5-HT(4) receptor of new piperazinyl-substituted thienopyrimidine derivatives 20-45 with a view to identify potent and selective ligands for the 5-HT(3) receptor. Some of the new compounds show good affinity for the 5-HT(3) receptor and, notably, do not display any affinity for the 5-HT(4) receptor. 4-(4-Methyl-1-piperazinyl)-2-methylthio-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidine 31 exhibits the highest affinity for the 5-HT(3) receptor (Ki = 33 nM) and behaves as noncompetitive antagonist.

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Year:  2004        PMID： 15210156     DOI： 10.1016/j.bmc.2004.04.043

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  4 in total

1.  Ethyl 5-methyl-4-oxo-3-phenyl-2-propyl-amino-3,4-dihydro-thieno[2,3-d]pyrimidine-6-carboxyl-ate.

Authors:  Ai-Hua Zheng; Yan-Mei Ren; Jing Xu
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-08-29

2.  Ethyl 2-isopropyl-amino-5-methyl-4-oxo-3-phenyl-3,4-dihydro-thieno[2,3-d]pyrimidine-6-carboxyl-ate.

Authors:  Ai-Hua Zheng; Liang-Yong Huang; E Chen; Hong Luo
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-11-04

3.  In-Silico Screening of Novel Synthesized Thienopyrimidines Targeting Fms Related Receptor Tyrosine Kinase-3 and Their In-Vitro Biological Evaluation.

Authors:  Elshaymaa I Elmongy; Najla Altwaijry; Nashwah G M Attallah; Manal Mubarak AlKahtani; Hanan Ali Henidi
Journal:  Pharmaceuticals (Basel)       Date:  2022-01-29

4.  Design, synthesis and biological evaluation of a new thieno[2,3-d]pyrimidine-based urea derivative with potential antitumor activity against tamoxifen sensitive and resistant breast cancer cell lines.

Authors:  Marwa Sharaky; Marwa Kamel; Marwa A Aziz; Mervat Omran; Monira M Rageh; Khaled A M Abouzid; Samia A Shouman
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051
  4 in total

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