molecules-logo

Journal Browser

Journal Browser

Antimalarial Agents: Design, Synthesis and Biological Evaluation

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (1 May 2020) | Viewed by 11365

Special Issue Editor


E-Mail Website
Guest Editor
Portland State University, Portland, United States
Interests: antimalarial agents; protein structure; protein function; tobacco smoke chemistry

Special Issue Information

Dear Colleagues,

Malaria is still a crucial problem worldwide, in spite of the significant research progress made. A new vaccine that doubtlessly will save lives is now being implemented in several countries, but this will not be enough to eliminate the disease in many regions. Therefore, newer vaccines that might overcome the deficiencies of the one currently available are years away. Policy changes regarding the use of drug combinations, especially artemisinin combination therapies (ACTs), as well as implementation of these policies have swept through much of the malarious world, but resistance has emerged against these drugs. Thus, the discovery and development of new drugs that overcome the mechanisms of resistance to the currently used antimalarial therapies remain a necessity until we actually accomplish the worldwide eradication of the various human malaria parasites. This Special Issue is intended to allow researchers to describe efforts toward discovering and developing new antimalarial drugs as well as new approaches to overcome resistance to the existing drugs.

Prof. David H. Peyton
Guest Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • malaria
  • falciparum
  • vivax
  • plasmodium
  • drug resistance
  • resistance
  • clearance rate
  • k13 gene
  • kelch
  • transmission
  • PfCRT
  • transporter
  • drug discovery
  • drug resistance
  • drug development
  • drug metabolism

Published Papers (3 papers)

Order results
Result details
Select all
Export citation of selected articles as:

Research

Jump to: Review

13 pages, 2028 KiB  
Communication
Predicting Drug Resistance Using Deep Mutational Scanning
by Gur Pines, Reilly G. Fankhauser and Carrie A. Eckert
Molecules 2020, 25(9), 2265; https://doi.org/10.3390/molecules25092265 - 11 May 2020
Cited by 6 | Viewed by 4074
Abstract
Drug resistance is a major healthcare challenge, resulting in a continuous need to develop new inhibitors. The development of these inhibitors requires an understanding of the mechanisms of resistance for a critical mass of occurrences. Recent genome editing technologies based on high-throughput DNA [...] Read more.
Drug resistance is a major healthcare challenge, resulting in a continuous need to develop new inhibitors. The development of these inhibitors requires an understanding of the mechanisms of resistance for a critical mass of occurrences. Recent genome editing technologies based on high-throughput DNA synthesis and sequencing may help to predict mutations resulting in resistance by testing large mutagenesis libraries. Here we describe the rationale of this approach, with examples and relevance to drug development and resistance in malaria. Full article
(This article belongs to the Special Issue Antimalarial Agents: Design, Synthesis and Biological Evaluation)
Show Figures

Figure 1

15 pages, 4176 KiB  
Article
Unsymmetrical Bisquinolines with High Potency against P. falciparum Malaria
by Katherine M. Liebman, Steven J. Burgess, Bornface Gunsaru, Jane X. Kelly, Yuexin Li, Westin Morrill, Michael C. Liebman and David H. Peyton
Molecules 2020, 25(9), 2251; https://doi.org/10.3390/molecules25092251 - 10 May 2020
Cited by 11 | Viewed by 3380
Abstract
Quinoline-based scaffolds have been the mainstay of antimalarial drugs, including many artemisinin combination therapies (ACTs), over the history of modern drug development. Although much progress has been made in the search for novel antimalarial scaffolds, it may be that quinolines will remain useful, [...] Read more.
Quinoline-based scaffolds have been the mainstay of antimalarial drugs, including many artemisinin combination therapies (ACTs), over the history of modern drug development. Although much progress has been made in the search for novel antimalarial scaffolds, it may be that quinolines will remain useful, especially if very potent compounds from this class are discovered. We report here the results of a structure-activity relationship (SAR) study assessing potential unsymmetrical bisquinoline antiplasmodial drug candidates using in vitro activity against intact parasites in cell culture. Many unsymmetrical bisquinolines were found to be highly potent against both chloroquine-sensitive and chloroquine-resistant Plasmodium falciparum parasites. Further work to develop such compounds could focus on minimizing toxicities in order to find suitable candidates for clinical evaluation. Full article
(This article belongs to the Special Issue Antimalarial Agents: Design, Synthesis and Biological Evaluation)
Show Figures

Graphical abstract

Review

Jump to: Research

16 pages, 1901 KiB  
Review
Taming the Boys for Global Good: Contraceptive Strategy to Stop Malaria Transmission
by Ryan Choi, Samantha A. Michaels, Emmanuel C. Onu, Matthew A. Hulverson, Aparajita Saha, Morenike E. Coker, Janis C. Weeks, Wesley C. Van Voorhis and Kayode K. Ojo
Molecules 2020, 25(12), 2773; https://doi.org/10.3390/molecules25122773 - 16 Jun 2020
Cited by 4 | Viewed by 3532
Abstract
Transmission of human malaria parasites (Plasmodium spp.) by Anopheles mosquitoes is a continuous process that presents a formidable challenge for effective control of the disease. Infectious gametocytes continue to circulate in humans for up to four weeks after antimalarial drug treatment, permitting [...] Read more.
Transmission of human malaria parasites (Plasmodium spp.) by Anopheles mosquitoes is a continuous process that presents a formidable challenge for effective control of the disease. Infectious gametocytes continue to circulate in humans for up to four weeks after antimalarial drug treatment, permitting prolonged transmission to mosquitoes even after clinical cure. Almost all reported malaria cases are transmitted to humans by mosquitoes, and therefore decreasing the rate of Plasmodium transmission from humans to mosquitoes with novel transmission-blocking remedies would be an important complement to other interventions in reducing malaria incidence. Full article
(This article belongs to the Special Issue Antimalarial Agents: Design, Synthesis and Biological Evaluation)
Show Figures

Figure 1

Back to TopTop