Literature DB >> 23164660

Synthesis and biological evaluation of 2,3-diarylimidazo[1,2-a]pyridines as antileishmanial agents.

Sophie Marhadour1, Pascal Marchand, Fabrice Pagniez, Marc-Antoine Bazin, Carine Picot, Olivier Lozach, Sandrine Ruchaud, Maud Antoine, Laurent Meijer, Najma Rachidi, Patrice Le Pape.   

Abstract

A novel series of 2,3-diarylimidazo[1,2-a]pyridines was synthesized and evaluated for their antileishmanial activities. Four derivatives exhibited good activity against the promastigote and intracellular amastigote stages of Leishmania major, coupled with a low cytotoxicity against the HeLa human cell line. The impact of compound lipophilicity on antiparasitic activities was investigated by Log D comparison. Although LmCK1 could be the parasitic target for three compounds (13, 18, 21), the inhibition of another target is under study to explain the antileishmanial effect of the most promising compounds.
Copyright © 2012 Elsevier Masson SAS. All rights reserved.

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Year:  2012        PMID: 23164660     DOI: 10.1016/j.ejmech.2012.10.048

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  10 in total

1.  8-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type 1 nitroreductases.

Authors:  Cyril Fersing; Clotilde Boudot; Julien Pedron; Sébastien Hutter; Nicolas Primas; Caroline Castera-Ducros; Sandra Bourgeade-Delmas; Alix Sournia-Saquet; Alain Moreau; Anita Cohen; Jean-Luc Stigliani; Geneviève Pratviel; Maxime D Crozet; Susan Wyllie; Alan Fairlamb; Alexis Valentin; Pascal Rathelot; Nadine Azas; Bertrand Courtioux; Pierre Verhaeghe; Patrice Vanelle
Journal:  Eur J Med Chem       Date:  2018-08-01       Impact factor: 6.514

2.  Metal-free, efficient hydrazination of imidazo[1,2-a]pyridine with diethyl azodicarboxylate in neutral media.

Authors:  Yuanxiang Wang; Brendan Frett; Nick McConnell; Hong-Yu Li
Journal:  Org Biomol Chem       Date:  2015-03-14       Impact factor: 3.876

Review 3.  Structure, regulation, and (patho-)physiological functions of the stress-induced protein kinase CK1 delta (CSNK1D).

Authors:  Pengfei Xu; Chiara Ianes; Fabian Gärtner; Congxing Liu; Timo Burster; Vasiliy Bakulev; Najma Rachidi; Uwe Knippschild; Joachim Bischof
Journal:  Gene       Date:  2019-07-31       Impact factor: 3.688

4.  Efficient access to 2,3-diarylimidazo[1,2-a]pyridines via a one-pot, ligand-free, palladium-catalyzed three-component reaction under microwave irradiation.

Authors:  Yuanxiang Wang; Brendan Frett; Hong-yu Li
Journal:  Org Lett       Date:  2014-05-22       Impact factor: 6.005

Review 5.  Dangerous Duplicity: The Dual Functions of Casein Kinase 1 in Parasite Biology and Host Subversion.

Authors:  Najma Rachidi; Uwe Knippschild; Gerald F Späth
Journal:  Front Cell Infect Microbiol       Date:  2021-03-22       Impact factor: 5.293

6.  Metal-free C-H arylation of imidazoheterocycles with aryl hydrazines.

Authors:  Sourav Jana; Sadhanendu Samanta; Avik K Bagdi; Valerii Z Shirinian; Alakananda Hajra
Journal:  RSC Adv       Date:  2018-04-03       Impact factor: 3.361

7.  Synthesis, study of antileishmanial and antitrypanosomal activity of imidazo pyridine fused triazole analogues.

Authors:  Adinarayana Nandikolla; Singireddi Srinivasarao; Banoth Karan Kumar; Sankaranarayanan Murugesan; Himanshu Aggarwal; Louise L Major; Terry K Smith; Kondapalli Venkata Gowri Chandra Sekhar
Journal:  RSC Adv       Date:  2020-10-19       Impact factor: 4.036

8.  Synthesis of new 3-acetyl-1,3,4-oxadiazolines combined with pyrimidines as antileishmanial and antiviral agents.

Authors:  Saida Lachhab; Az-Eddine El Mansouri; Ahmad Mehdi; Indira Dennemont; Johan Neyts; Dirk Jochmans; Graciela Andrei; Robert Snoeck; Yogesh S Sanghvi; Mustapha Ait Ali; Philippe M Loiseau; Hassan B Lazrek
Journal:  Mol Divers       Date:  2022-10-17       Impact factor: 3.364

9.  Collaborative virtual screening to elaborate an imidazo[1,2-a]pyridine hit series for visceral leishmaniasis.

Authors:  Yuichiro Akao; Stacie Canan; Yafeng Cao; Kevin Condroski; Ola Engkvist; Sachiko Itono; Rina Kaki; Chiaki Kimura; Thierry Kogej; Kazuya Nagaoka; Akira Naito; Hiromi Nakai; Garry Pairaudeau; Constantin Radu; Ieuan Roberts; Mitsuyuki Shimada; David Shum; Nao-Aki Watanabe; Huanxu Xie; Shuji Yonezawa; Osamu Yoshida; Ryu Yoshida; Charles Mowbray; Benjamin Perry
Journal:  RSC Med Chem       Date:  2021-01-21

10.  A Multilayer Network Approach for Guiding Drug Repositioning in Neglected Diseases.

Authors:  Ariel José Berenstein; María Paula Magariños; Ariel Chernomoretz; Fernán Agüero
Journal:  PLoS Negl Trop Dis       Date:  2016-01-06
  10 in total

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