Literature DB >> 29259752

Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol.

Nada Abla1,2, Sridevi Bashyam3, Susan A Charman4, Béatrice Greco1, Philip Hewitt5, Maria Belén Jiménez-Díaz6, Kasiram Katneni4, Holger Kubas5, Didier Picard7, Yuvaraj Sambandan3, Laura Sanz6, Dennis Smith4, Tai Wang7, Paul Willis2, Sergio Wittlin8,9, Thomas Spangenberg1.   

Abstract

With ∼429,000 deaths in 2016, malaria remains a major infectious disease where the need to treat the fever symptoms, but also to provide relevant post-treatment prophylaxis, is of major importance. An azepanylcarbazole amino alcohol is disclosed with a long- and fast-acting in vivo antiplasmodial efficacy and meets numerous attributes of a desired post-treatment chemoprophylactic antimalarial agent. The synthesis, the parasitological characterization, and the animal pharmacokinetics and pharmacodynamics of this compound are presented along with a proposed target.

Entities:  

Year:  2017        PMID: 29259752      PMCID: PMC5733276          DOI: 10.1021/acsmedchemlett.7b00391

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN: 1948-5875            Impact factor:   4.345


  22 in total

1.  Preface to Hsp90.

Authors:  Didier Picard
Journal:  Biochim Biophys Acta       Date:  2012-03

2.  Physiochemical drug properties associated with in vivo toxicological outcomes.

Authors:  Jason D Hughes; Julian Blagg; David A Price; Simon Bailey; Gary A Decrescenzo; Rajesh V Devraj; Edmund Ellsworth; Yvette M Fobian; Michael E Gibbs; Richard W Gilles; Nigel Greene; Enoch Huang; Teresa Krieger-Burke; Jens Loesel; Travis Wager; Larry Whiteley; Yao Zhang
Journal:  Bioorg Med Chem Lett       Date:  2008-07-24       Impact factor: 2.823

3.  3- and 4-carbazole dialkylaminocarbinols as potential antimalarial agents.

Authors:  V H Brown; M Keyanpour-Rad; J I DeGraw
Journal:  J Med Chem       Date:  1971-06       Impact factor: 7.446

4.  Antiplasmodial activity of mono- and dimeric carbazoles.

Authors:  G Bringmann; A Ledermann; J Holenz; M T Kao; U Busse; H G Wu; G François
Journal:  Planta Med       Date:  1998-02       Impact factor: 3.352

5.  In vitro evaluations of antimalarial drugs and their relevance to clinical outcomes.

Authors:  Eric H Ekland; David A Fidock
Journal:  Int J Parasitol       Date:  2008-04-01       Impact factor: 3.981

6.  P. falciparum in vitro killing rates allow to discriminate between different antimalarial mode-of-action.

Authors:  Laura M Sanz; Benigno Crespo; Cristina De-Cózar; Xavier C Ding; Jose L Llergo; Jeremy N Burrows; Jose F García-Bustos; Francisco-Javier Gamo
Journal:  PLoS One       Date:  2012-02-23       Impact factor: 3.240

Review 7.  New developments in anti-malarial target candidate and product profiles.

Authors:  Jeremy N Burrows; Stephan Duparc; Winston E Gutteridge; Rob Hooft van Huijsduijnen; Wiweka Kaszubska; Fiona Macintyre; Sébastien Mazzuri; Jörg J Möhrle; Timothy N C Wells
Journal:  Malar J       Date:  2017-01-13       Impact factor: 2.979

8.  A framework for assessing the risk of resistance for anti-malarials in development.

Authors:  Xavier C Ding; David Ubben; Timothy N C Wells
Journal:  Malar J       Date:  2012-08-22       Impact factor: 2.979

9.  A murine model of falciparum-malaria by in vivo selection of competent strains in non-myelodepleted mice engrafted with human erythrocytes.

Authors:  Iñigo Angulo-Barturen; María Belén Jiménez-Díaz; Teresa Mulet; Joaquín Rullas; Esperanza Herreros; Santiago Ferrer; Elena Jiménez; Alfonso Mendoza; Javier Regadera; Philip J Rosenthal; Ian Bathurst; David L Pompliano; Federico Gómez de las Heras; Domingo Gargallo-Viola
Journal:  PLoS One       Date:  2008-05-21       Impact factor: 3.240

10.  Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum.

Authors:  Claire Le Manach; Christian Scheurer; Sibylle Sax; Sarah Schleiferböck; Diego Gonzalez Cabrera; Yassir Younis; Tanya Paquet; Leslie Street; Peter Smith; Xavier C Ding; David Waterson; Michael J Witty; Didier Leroy; Kelly Chibale; Sergio Wittlin
Journal:  Malar J       Date:  2013-11-16       Impact factor: 2.979

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  1 in total

1.  The relative rate of kill of the MMV Malaria Box compounds provides links to the mode of antimalarial action and highlights scaffolds of medicinal chemistry interest.

Authors:  Imran Ullah; Raman Sharma; Antonio Mete; Giancarlo A Biagini; Dawn M Wetzel; Paul D Horrocks
Journal:  J Antimicrob Chemother       Date:  2020-02-01       Impact factor: 5.758

  1 in total

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