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antimalarial drug

MalDA, Accelerating Malaria Drug Discovery

March 4, 2021 - 11:12 -- Open Access
Author(s): 
Yang T, Ottilie S, Winzeler EA, et al.
Reference: 
Trends Parasitol. 2021 Feb 26:S1471-4922(21)00012-X

The Malaria Drug Accelerator (MalDA) is a consortium of 15 leading scientific laboratories. The aim of MalDA is to improve and accelerate the early antimalarial drug discovery process by identifying new, essential, druggable targets.

NOT Open Access | Quinoline carboxamide core moiety-based compounds inhibit P. falciparumfalcipain-2: Design, synthesis and antimalarial efficacy studies

March 2, 2021 - 15:34 -- NOT Open Access
Author(s): 
Singh A, Kalamuddin M, Maqbool M, Mohmmed A, Malhotra P, Hoda N
Reference: 
Bioorg Chem. 2021 Mar;108:104514

Targeting Falcipain-2 (FP2) for the development of antimalarials is a promising and established concept in antimalarial drug discovery and development. FP2, a member of papain-family cysteine protease of the malaria parasite Plasmodium falciparum holds an important role in hemoglobin degradation pathway. A new series of quinoline carboxamide-based compounds was designed, synthesized and evaluated for antimalarial activity.

Quest for a potent antimalarial drug lead: Synthesis and evaluation of 6,7-dimethoxyquinazoline-2,4-diamines

March 2, 2021 - 11:25 -- Open Access
Author(s): 
Mizukawa Y, Ikegami-Kawai M, Itoh I, et al.
Reference: 
Bioorg Med Chem. 2021 Mar 1;33:116018

Quinazolines have long been known to exert varied pharmacologic activities that make them suitable for use in treating hypertension, viral infections, tumors, and malaria. Since 2014, we have synthesized approximately 150 different 6,7-dimethoxyquinazoline-2,4-diamines and evaluated their antimalarial activity via structure-activity relationship studies.

NOT Open Access | A Novel Hybrid of Chloroquine and Primaquine Linked by Gold(I): Multitarget and Multiphase Antiplasmodial Agent

February 25, 2021 - 08:21 -- NOT Open Access
Author(s): 
de Souza Pereira C, Costa Quadros H, Navarro M, et al.
Reference: 
ChemMedChem. 2021 Feb 17;16(4):662-678

Plasmodium parasites kill 435 000 people around the world every year due to unavailable vaccines, a limited arsenal of antimalarial drugs, delayed treatment, and the reduced clinical effectiveness of current practices caused by drug resistance. Therefore, there is an urgent need to discover and develop new antiplasmodial candidates. In this work, we present a novel strategy to develop a multitarget metallic hybrid antimalarial agent with possible dual efficacy in both sexual and asexual erythrocytic stages.

NOT Open Access | Inhibition Mechanism of Antimalarial Drugs Targeting the Cytochrome bc1 Complex

February 23, 2021 - 13:16 -- NOT Open Access
Author(s): 
Jacobsen L, Husen P, Solov'yov IA
Reference: 
J Chem Inf Model. 2021 Feb 22

Plasmodium falciparum (P. falciparum) is the main parasite known to cause malaria in humans. The antimalarial drug atovaquone is known to inhibit the Qo-site of the cytochrome bc1 complex of P. falciparum, which ultimately blocks ATP synthesis, leading to cell death. Through the years, mutations of the P. falciparum cytochrome bc1 complex, causing resistance to atovaquone, have emerged.

Diversity-oriented synthesis derived indole based spiro and fused small molecules kills artemisinin-resistant Plasmodium falciparum

February 20, 2021 - 08:37 -- Open Access
Author(s): 
Akshaykumar Nayak, Himani Saxena, Chandramohan Bathula, Tarkeshwar Kumar, Souvik Bhattacharjee, Subhabrata Sen and Ashish Gupta
Reference: 
Malaria Journal 2021 20:100, 17 February 2021

Despite numerous efforts to eradicate the disease, malaria continues to remain one of the most dangerous infectious diseases plaguing the world. In the absence of any effective vaccines and with emerging drug resistance in the parasite against the majority of anti-malarial drugs, the search for new drugs is urgently needed for effective malaria treatment.

NOT Open Access | A tablet derived from Andrographis paniculata complements dihydroartemisinin-piperaquine treatment of malaria in pregnant mice

February 15, 2021 - 15:15 -- NOT Open Access
Author(s): 
Bastiana, Widyawaruyanti A, Ilmi H, Tumewu L, Prasetyo B, Hafid AF, Aryati
Reference: 
J Basic Clin Physiol Pharmacol. 2021 Feb 11

The use of standard antimalarial drugs, such as dihydroartemisinin-piperaquine (DHP) for the treatment of malaria during pregnancy is limited due to the risk of teratogenicity. The alternative is therefore required although few exist. Here we show a phytopharmaceutical drug derived from Andrographis paniculata (AS201-01), which is effective as herbal antimalarial both in vitro and in vivo and may be a suitable alternative when used in complementary treatment with DHP.

NOT Open Access | A novel antiplasmodial compound: integration of in silico and in vitro assays

February 10, 2021 - 09:51 -- NOT Open Access
Author(s): 
Costa Júnior DB, Araújo JSC, Oliveira LM, Neri FSM, Moreira POL, Taranto AG, Fonseca AL, Varotti FP, Leite FHA
Reference: 
J Biomol Struct Dyn. 2021 Feb 8:1-13

Malaria is a disease caused by Plasmodium genus. which P. falciparum is responsible for the most severe form of the disease, cerebral malaria. In 2018, 405,000 people died of malaria. Antimalarial drugs have serious adverse effects and limited efficacy due to multidrug-resistant strains. One way to overcome these limitations is the use of computational approaches for prioritizing candidates to phenotypic assays and/or in vitro assays against validated targets. Plasmodium falciparum Enoyl-ACP reductase (PfENR) is noteworthy because it catalyzes the rate-limiting step of the biosynthetic pathway of fatty acid.

NOT Open Access | Metalloaminopeptidases of the Protozoan Parasite Plasmodium falciparum as Targets for the Discovery of Novel Antimalarial Drugs

February 6, 2021 - 10:50 -- NOT Open Access
Author(s): 
Mills B, Isaac RE, Foster R
Reference: 
J Med Chem. 2021 Feb 3

Malaria poses a significant threat to approximately half of the world's population with an annual death toll close to half a million. The emergence of resistance to front-line antimalarials in the most lethal human parasite species, Plasmodium falciparum (Pf), threatens progress made in malaria control. The prospect of losing the efficacy of antimalarial drugs is driving the search for small molecules with new modes of action.

Parasite-host dynamics throughout antimalarial drug development stages complicate the translation of parasite clearance

February 2, 2021 - 16:29 -- Open Access
Author(s): 
Burgert L, Zaloumis S, Dini S, Marquart L, Cao P, Cherkaoui M, Gobeau N, McCarthy J, Simpson JA, Möhrle JJ, Penny MA
Reference: 
Antimicrob Agents Chemother. 2021 Feb 1:AAC.01539-20

Ensuring continued success against malaria depends on a pipeline of new antimalarials. Antimalarial drug development utilizes pre-clinical murine and experimental human malaria infection studies to evaluate drug efficacy. A sequential approach is typically adapted, with results from each stage, informing the design of the next stage of development. The validity of this approach depends on confidence that results from murine malarial studies predict the outcome of clinical trials in humans. Parasite clearance rates following treatment are key parameters of drug efficacy.

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