Literature DB >> 28647378

Leishmaniasis drug discovery: recent progress and challenges in assay development.

Bilal Zulfiqar1, Todd B Shelper1, Vicky M Avery2.   

Abstract

Leishmaniasis, caused by the trypanosomatid protozoan Leishmania, is endemic in 98 countries worldwide, with morbidity and mortality increasing daily. Despite available drugs, leishmaniasis faces the challenge of emerging resistance and toxicity concerns for current drug regimes. Identification of anti-leishmanial compounds representing new chemistry and novel mechanisms of action is essential to populate the drug discovery pipeline. The in vitro assays currently available have shown poor translational outcomes, with high compound attrition rates. It is therefore imperative that more physiologically relevant assays are developed to identify anti-leishmanial compounds. This review provides an overview of the disease, current treatment options and compares the various technologies and assay formats currently available for leishmanial drug discovery.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Mesh:

Substances:

Year:  2017        PMID: 28647378     DOI: 10.1016/j.drudis.2017.06.004

Source DB:  PubMed          Journal:  Drug Discov Today        ISSN: 1359-6446            Impact factor:   7.851


  42 in total

1.  Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study.

Authors:  Julien Pedron; Clotilde Boudot; Sébastien Hutter; Sandra Bourgeade-Delmas; Jean-Luc Stigliani; Alix Sournia-Saquet; Alain Moreau; Elisa Boutet-Robinet; Lucie Paloque; Emmanuelle Mothes; Michèle Laget; Laure Vendier; Geneviève Pratviel; Susan Wyllie; Alan Fairlamb; Nadine Azas; Bertrand Courtioux; Alexis Valentin; Pierre Verhaeghe
Journal:  Eur J Med Chem       Date:  2018-06-05       Impact factor: 6.514

Review 2.  Benzophenone: a ubiquitous scaffold in medicinal chemistry.

Authors:  Khemchand Surana; Bharatkumar Chaudhary; Monika Diwaker; Satyasheel Sharma
Journal:  Medchemcomm       Date:  2018-08-23       Impact factor: 3.597

3.  Evaluation of the Efficacy of Amphotericin B and Terbinafine Microemulsions and Their Combination on Cutaneous Leishmaniasis and Comparison with the Conventional Drug Form in BALB/c Mice.

Authors:  Zeynab Baharvandi; Anayatollah Salimi; Reza Arjmand; Ali Jelowdar; Abdollah Rafiei
Journal:  AAPS PharmSciTech       Date:  2022-10-14       Impact factor: 4.026

4.  Susceptibility of promastigotes and intracellular amastigotes from distinct Leishmania species to the calpain inhibitor MDL28170.

Authors:  Pedro Soares de Sousa Araújo; Simone Santiago Carvalho de Oliveira; Claudia Masini d'Avila-Levy; André Luis Souza Dos Santos; Marta Helena Branquinha
Journal:  Parasitol Res       Date:  2018-05-04       Impact factor: 2.289

5.  Cyclic Nucleotide-Specific Phosphodiesterases as Potential Drug Targets for Anti-Leishmania Therapy.

Authors:  Victor Sebastián-Pérez; Sarah Hendrickx; Jane C Munday; Titilola Kalejaiye; Ana Martínez; Nuria E Campillo; Harry de Koning; Guy Caljon; Louis Maes; Carmen Gil
Journal:  Antimicrob Agents Chemother       Date:  2018-09-24       Impact factor: 5.191

6.  Antitrypanosomatid Pharmacomodulation at Position 3 of the 8-Nitroquinolin-2(1H)-one Scaffold Using Palladium-Catalysed Cross-Coupling Reactions.

Authors:  Julien Pedron; Clotilde Boudot; Sandra Bourgeade-Delmas; Alix Sournia-Saquet; Lucie Paloque; Maryam Rastegari; Mansour Abdoulaye; Hussein El-Kashef; Colin Bonduelle; Geneviève Pratviel; Susan Wyllie; Alan H Fairlamb; Bertrand Courtioux; Pierre Verhaeghe; Alexis Valentin
Journal:  ChemMedChem       Date:  2018-09-17       Impact factor: 3.466

7.  Systematic search for benzimidazole compounds and derivatives with antileishmanial effects.

Authors:  Juan Carlos Sánchez-Salgado; Pablo Bilbao-Ramos; María Auxiliadora Dea-Ayuela; Francisco Hernández-Luis; Francisco Bolás-Fernández; José L Medina-Franco; Yareli Rojas-Aguirre
Journal:  Mol Divers       Date:  2018-05-10       Impact factor: 2.943

8.  Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors.

Authors:  Baljinder Singh; Jean A Bernatchez; Laura-Isobel McCall; Claudia M Calvet; Jasmin Ackermann; Julia M Souza; Diane Thomas; Everton M Silva; Kelly A Bachovchin; Dana M Klug; Hitesh B Jalani; Seema Bag; Melissa J Buskes; Susan E Leed; Norma E Roncal; Erica C Penn; Jessey Erath; Ana Rodriguez; Richard J Sciotti; Robert F Campbell; James McKerrow; Jair L Siqueira-Neto; Lori Ferrins; Michael P Pollastri
Journal:  ACS Med Chem Lett       Date:  2020-01-10       Impact factor: 4.345

Review 9.  Promises and Pitfalls of Parasite Patch-clamp.

Authors:  Jeanine Gezelle; Gagandeep Saggu; Sanjay A Desai
Journal:  Trends Parasitol       Date:  2021-02-24

10.  Antileishmanial macrolides from ant-associated Streptomyces sp. ISID311.

Authors:  Humberto E Ortega; Vitor B Lourenzon; Marc G Chevrette; Leonardo L G Ferreira; René F Ramos Alvarenga; Weilan G P Melo; Tiago Venâncio; Cameron R Currie; Adriano D Andricopulo; Tim S Bugni; Mônica T Pupo
Journal:  Bioorg Med Chem       Date:  2021-01-12       Impact factor: 3.641

View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.