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SAR

NOT Open Access | Design, Synthesis, and Structural Analysis of Cladosporin-Based Inhibitors of Malaria Parasites

April 13, 2021 - 13:26 -- NOT Open Access
Author(s): 
Babbar P, Das P, Manickam Y, Mankad Y, Yadav S, Parvez S, Sharma A, Reddy DS
Reference: 
ACS Infect Dis. 2021 Apr 12

Here we have described a systematic structure activity relationship (SAR) of a set of compounds inspired from cladosporin, a tool compound that targets parasite (Plasmodium falciparum) lysyl tRNA synthetase (KRS). Four sets of analogues, synthesized based on point changes in the chemical scaffold of cladosporin and other logical modifications and hybridizations, were assessed using high throughput enzymatic and parasitic assays along with in vitro pharmacokinetics.

NOT Open Access | Discovery of Potent and Fast-Acting Antimalarial Bis-1,2,4-triazines

March 26, 2021 - 16:11 -- NOT Open Access
Author(s): 
Priebbenow DL, Mathiew M, Baell JB, et al.
Reference: 
J Med Chem. 2021 Mar 24

Novel 3,3'-disubstituted-5,5'-bi(1,2,4-triazine) compounds with potent in vitro activity against Plasmodium falciparum parasites were recently discovered. To improve the pharmacokinetic properties of the triazine derivatives, a new structure-activity relationship (SAR) investigation was initiated with a focus on enhancing the metabolic stability of lead compounds.

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