Literature DB >> 26502160

A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines.

Claire Le Manach, Tanya Paquet, Christel Brunschwig1, Mathew Njoroge1, Ze Han, Diego Gonzàlez Cabrera, Sridevi Bashyam2, Rajkumar Dhinakaran2, Dale Taylor1, Janette Reader3, Mariette Botha3, Alisje Churchyard3, Sonja Lauterbach3, Theresa L Coetzer4, Lyn-Marie Birkholtz3, Stephan Meister5, Elizabeth A Winzeler5, David Waterson6, Michael J Witty6, Sergio Wittlin7,8, María-Belén Jiménez-Díaz9, María Santos Martínez9, Santiago Ferrer9, Iñigo Angulo-Barturen9, Leslie J Street, Kelly Chibale.   

Abstract

Toward improving pharmacokinetics, in vivo efficacy, and selectivity over hERG, structure-activity relationship studies around the central core of antimalarial imidazopyridazines were conducted. This study led to the identification of potent pyrazolopyridines, which showed good in vivo efficacy and pharmacokinetics profiles. The lead compounds also proved to be very potent in the parasite liver and gametocyte stages, which makes them of high interest.

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Year:  2015        PMID: 26502160     DOI: 10.1021/acs.jmedchem.5b01605

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  9 in total

1.  UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.

Authors:  Christel Brunschwig; Nina Lawrence; Dale Taylor; Efrem Abay; Mathew Njoroge; Gregory S Basarab; Claire Le Manach; Tanya Paquet; Diego Gonzàlez Cabrera; Aloysius T Nchinda; Carmen de Kock; Lubbe Wiesner; Paolo Denti; David Waterson; Benjamin Blasco; Didier Leroy; Michael J Witty; Cristina Donini; James Duffy; Sergio Wittlin; Karen L White; Susan A Charman; Maria Belén Jiménez-Díaz; Iñigo Angulo-Barturen; Esperanza Herreros; Francisco Javier Gamo; Rosemary Rochford; Dalu Mancama; Theresa L Coetzer; Mariëtte E van der Watt; Janette Reader; Lyn-Marie Birkholtz; Kennan C Marsh; Suresh M Solapure; John E Burke; Jacob A McPhail; Manu Vanaerschot; David A Fidock; Paul V Fish; Peter Siegl; Dennis A Smith; Grennady Wirjanata; Rintis Noviyanti; Ric N Price; Jutta Marfurt; Kigbafori D Silue; Leslie J Street; Kelly Chibale
Journal:  Antimicrob Agents Chemother       Date:  2018-08-27       Impact factor: 5.191

2.  Antiplasmodial imidazopyridazines: structure-activity relationship studies lead to the identification of analogues with improved solubility and hERG profiles.

Authors:  Peter Mubanga Cheuka; Nina Lawrence; Dale Taylor; Sergio Wittlin; Kelly Chibale
Journal:  Medchemcomm       Date:  2018-09-06       Impact factor: 3.597

3.  Antimalarial agents against both sexual and asexual parasites stages: structure-activity relationships and biological studies of the Malaria Box compound 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine (MMV019918) and analogues.

Authors:  Alessandra Vallone; Sarah D'Alessandro; Simone Brogi; Margherita Brindisi; Giulia Chemi; Gloria Alfano; Stefania Lamponi; Soon Goo Lee; Joseph M Jez; Karin J M Koolen; Koen J Dechering; Simona Saponara; Fabio Fusi; Beatrice Gorelli; Donatella Taramelli; Silvia Parapini; Reto Caldelari; Giuseppe Campiani; Sandra Gemma; Stefania Butini
Journal:  Eur J Med Chem       Date:  2018-03-10       Impact factor: 6.514

4.  Three-Component Coupling of Aldehydes, Aminopyrazoles, and Sulfoxonium Ylides via Rhodium(III)-Catalyzed Imidoyl C-H Activation: Synthesis of Pyrazolo[1,5- a]pyrimidines.

Authors:  Gia L Hoang; Andrew D Streit; Jonathan A Ellman
Journal:  J Org Chem       Date:  2018-12-10       Impact factor: 4.354

5.  New approach toward the synthesis of deuterated pyrazolo[1,5-a]pyridines and 1,2,4-triazolo[1,5-a]pyridines.

Authors:  Aleksey Yu Vorob'ev; Vyacheslav I Supranovich; Gennady I Borodkin; Vyacheslav G Shubin
Journal:  Beilstein J Org Chem       Date:  2017-05-02       Impact factor: 2.883

6.  The Plasmodium PI(4)K inhibitor KDU691 selectively inhibits dihydroartemisinin-pretreated Plasmodium falciparum ring-stage parasites.

Authors:  L Dembele; X Ang; M Chavchich; G M C Bonamy; J J Selva; M Yi-Xiu Lim; C Bodenreider; B K S Yeung; F Nosten; B M Russell; M D Edstein; J Straimer; D A Fidock; T T Diagana; P Bifani
Journal:  Sci Rep       Date:  2017-05-24       Impact factor: 4.379

7.  Synthesis of Some New 1,3,4-Thiadiazole, Thiazole and Pyridine Derivatives Containing 1,2,3-Triazole Moiety.

Authors:  Nadia A Abdelriheem; Ali M M Mohamed; Abdou O Abdelhamid
Journal:  Molecules       Date:  2017-02-10       Impact factor: 4.411

Review 8.  The Development of Novel Compounds Against Malaria: Quinolines, Triazolpyridines, Pyrazolopyridines and Pyrazolopyrimidines.

Authors:  Luiz C S Pinheiro; Lívia M Feitosa; Marilia O Gandi; Flávia F Silveira; Nubia Boechat
Journal:  Molecules       Date:  2019-11-13       Impact factor: 4.411

9.  Reliable Functionalization of 5,6-Fused Bicyclic N-Heterocycles Pyrazolopyrimidines and Imidazopyridazines via Zinc and Magnesium Organometallics.

Authors:  Saroj Kumar Rout; Agonist Kastrati; Harish Jangra; Kuno Schwärzer; Alisa S Sunagatullina; Maximilien Garny; Fabio Lima; Cara E Brocklehurst; Konstantin Karaghiosoff; Hendrik Zipse; Paul Knochel
Journal:  Chemistry       Date:  2022-05-11       Impact factor: 5.020

  9 in total

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