Literature DB >> 30108934

Recent updates in the discovery and development of novel antimalarial drug candidates.

John Okombo1, Kelly Chibale1,2.   

Abstract

Though morbidity and mortality due to malaria have declined in the last 15 years, emerging resistance to first-line artemisinin-based antimalarials, absence of efficacious vaccines and limited chemotherapeutic alternatives imperil the consolidation of these gains. As a blueprint to steer future designs of new medicines, malaria drug discovery recently adopted a descriptive proposal for the ideal candidate molecules and drugs likely to successfully progress into the final stages of clinical development. As an audit of recent developments in the chemotherapy of malaria in the last five years, this review captures a landscape of diverse molecules at various stages of drug development and discusses their progress. In brief, we also discuss how omics data on Plasmodium has been extensively leveraged to identify potential vaccine candidates and putative targets of molecules in development and clinical use as well as map loci implicit in their modes of resistance. Future perspective on malaria drug development should involve a reconciliation of some of the challenges of the target candidate profiles (TCPs), specifically TCP3, with the promise of effective anti-hypnozoite medicines. Similarly, with the recent development of a humanized mouse model that can evaluate the prophylactic potential of candidate drugs, we argue for increased effort at identifying more liver-stage molecules, which are often only secondarily prioritized in conventional screening programs.

Entities:  

Year:  2018        PMID: 30108934      PMCID: PMC6071755          DOI: 10.1039/c7md00637c

Source DB:  PubMed          Journal:  Medchemcomm        ISSN: 2040-2503            Impact factor:   3.597


  92 in total

1.  Randomized dose-ranging study of the safety and efficacy of WR 238605 (Tafenoquine) in the prevention of relapse of Plasmodium vivax malaria in Thailand.

Authors:  D S Walsh; S Looareesuwan; P Wilairatana; D G Heppner; D B Tang; T G Brewer; W Chokejindachai; P Viriyavejakul; D E Kyle; W K Milhous; B G Schuster; J Horton; D J Braitman; R P Brueckner
Journal:  J Infect Dis       Date:  1999-10       Impact factor: 5.226

2.  Prodrugs of bisthiazolium salts are orally potent antimalarials.

Authors:  Henri J Vial; Sharon Wein; Christine Farenc; Clemens Kocken; Olivier Nicolas; Marie Laure Ancelin; Francoise Bressolle; Alan Thomas; Michèle Calas
Journal:  Proc Natl Acad Sci U S A       Date:  2004-10-18       Impact factor: 11.205

3.  A major genome region underlying artemisinin resistance in malaria.

Authors:  Ian H Cheeseman; Becky A Miller; Shalini Nair; Standwell Nkhoma; Asako Tan; John C Tan; Salma Al Saai; Aung Pyae Phyo; Carit Ler Moo; Khin Maung Lwin; Rose McGready; Elizabeth Ashley; Mallika Imwong; Kasia Stepniewska; Poravuth Yi; Arjen M Dondorp; Mayfong Mayxay; Paul N Newton; Nicholas J White; François Nosten; Michael T Ferdig; Timothy J C Anderson
Journal:  Science       Date:  2012-04-06       Impact factor: 47.728

4.  Identification of an antimalarial synthetic trioxolane drug development candidate.

Authors:  Jonathan L Vennerstrom; Sarah Arbe-Barnes; Reto Brun; Susan A Charman; Francis C K Chiu; Jacques Chollet; Yuxiang Dong; Arnulf Dorn; Daniel Hunziker; Hugues Matile; Kylie McIntosh; Maniyan Padmanilayam; Josefina Santo Tomas; Christian Scheurer; Bernard Scorneaux; Yuanqing Tang; Heinrich Urwyler; Sergio Wittlin; William N Charman
Journal:  Nature       Date:  2004-08-19       Impact factor: 49.962

5.  Structure-activity relationships for antiplasmodial activity among 7-substituted 4-aminoquinolines.

Authors:  D De; F M Krogstad; L D Byers; D J Krogstad
Journal:  J Med Chem       Date:  1998-12-03       Impact factor: 7.446

6.  Antimalarial Activity of KAF156 in Falciparum and Vivax Malaria.

Authors:  Nicholas J White; Tran T Duong; Chirapong Uthaisin; François Nosten; Aung P Phyo; Borimas Hanboonkunupakarn; Sasithon Pukrittayakamee; Podjanee Jittamala; Kittiphum Chuthasmit; Ming S Cheung; Yiyan Feng; Ruobing Li; Baldur Magnusson; Marc Sultan; Daniela Wieser; Xiaolei Xun; Rong Zhao; Thierry T Diagana; Peter Pertel; F Joel Leong
Journal:  N Engl J Med       Date:  2016-09-22       Impact factor: 91.245

7.  Artemisinin resistance in Plasmodium falciparum malaria.

Authors:  Arjen M Dondorp; François Nosten; Poravuth Yi; Debashish Das; Aung Phae Phyo; Joel Tarning; Khin Maung Lwin; Frederic Ariey; Warunee Hanpithakpong; Sue J Lee; Pascal Ringwald; Kamolrat Silamut; Mallika Imwong; Kesinee Chotivanich; Pharath Lim; Trent Herdman; Sen Sam An; Shunmay Yeung; Pratap Singhasivanon; Nicholas P J Day; Niklas Lindegardh; Duong Socheat; Nicholas J White
Journal:  N Engl J Med       Date:  2009-07-30       Impact factor: 91.245

8.  An antifungal agent inhibits an aminoacyl-tRNA synthetase by trapping tRNA in the editing site.

Authors:  Fernando L Rock; Weimin Mao; Anya Yaremchuk; Mikhail Tukalo; Thibaut Crépin; Huchen Zhou; Yong-Kang Zhang; Vincent Hernandez; Tsutomu Akama; Stephen J Baker; Jacob J Plattner; Lucy Shapiro; Susan A Martinis; Stephen J Benkovic; Stephen Cusack; M R K Alley
Journal:  Science       Date:  2007-06-22       Impact factor: 47.728

Review 9.  Quinine, an old anti-malarial drug in a modern world: role in the treatment of malaria.

Authors:  Jane Achan; Ambrose O Talisuna; Annette Erhart; Adoke Yeka; James K Tibenderana; Frederick N Baliraine; Philip J Rosenthal; Umberto D'Alessandro
Journal:  Malar J       Date:  2011-05-24       Impact factor: 2.979

10.  The effect of malaria control on Plasmodium falciparum in Africa between 2000 and 2015.

Authors:  S Bhatt; D J Weiss; E Cameron; D Bisanzio; B Mappin; U Dalrymple; K Battle; C L Moyes; A Henry; P A Eckhoff; E A Wenger; O Briët; M A Penny; T A Smith; A Bennett; J Yukich; T P Eisele; J T Griffin; C A Fergus; M Lynch; F Lindgren; J M Cohen; C L J Murray; D L Smith; S I Hay; R E Cibulskis; P W Gething
Journal:  Nature       Date:  2015-09-16       Impact factor: 49.962

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  5 in total

Review 1.  An epigrammatic status of the 'azole'-based antimalarial drugs.

Authors:  Mousmee Sharma; Parteek Prasher
Journal:  RSC Med Chem       Date:  2019-12-23

2.  Physicochemical Profiling and Comparison of Research Antiplasmodials and Advanced Stage Antimalarials with Oral Drugs.

Authors:  Amritansh Bhanot; Sandeep Sundriyal
Journal:  ACS Omega       Date:  2021-02-25

3.  Easy-To-Access Quinolone Derivatives Exhibiting Antibacterial and Anti-Parasitic Activities.

Authors:  Richard M Beteck; Audrey Jordaan; Ronnett Seldon; Dustin Laming; Heinrich C Hoppe; Digby F Warner; Setshaba D Khanye
Journal:  Molecules       Date:  2021-02-20       Impact factor: 4.411

4.  Chemoprotective antimalarials identified through quantitative high-throughput screening of Plasmodium blood and liver stage parasites.

Authors:  Dorjbal Dorjsuren; Richard T Eastman; Anton Simeonov; David A Fidock; Kathryn J Wicht; Daniel Jansen; Daniel C Talley; Benjamin A Sigmon; Alexey V Zakharov; Norma Roncal; Andrew T Girvin; Yevgeniya Antonova-Koch; Paul M Will; Pranav Shah; Hongmao Sun; Carleen Klumpp-Thomas; Sachel Mok; Tomas Yeo; Stephan Meister; Juan Jose Marugan; Leila S Ross; Xin Xu; David J Maloney; Ajit Jadhav; Bryan T Mott; Richard J Sciotti; Elizabeth A Winzeler; Norman C Waters; Robert F Campbell; Wenwei Huang
Journal:  Sci Rep       Date:  2021-01-22       Impact factor: 4.379

Review 5.  Thienopyrimidine: A Promising Scaffold to Access Anti-Infective Agents.

Authors:  Prisca Lagardère; Cyril Fersing; Nicolas Masurier; Vincent Lisowski
Journal:  Pharmaceuticals (Basel)       Date:  2021-12-27
  5 in total

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