Basic Nitrogen (BaN) is a key property of antimalarial chemical space

H Valluri, A Bhanot, S Shah, N Bhandaru… - Journal of Medicinal …, 2023 - ACS Publications
Most antimalarials are based on basic N-heterocycles and possess amine functionalities.
Despite this, the role of basic nitrogen (BaN) in antimalarial drug design has not been …

Towards next-generation treatment options to combat Plasmodium falciparum malaria

J Okombo, DA Fidock - Nature Reviews Microbiology, 2024 - nature.com
Malaria, which is caused by infection of red blood cells with Plasmodium parasites, can be
fatal in non-immune individuals if left untreated. The recent approval of the pre-erythrocytic …

Benzimidazole Derivatives Are Potent against Multiple Life Cycle Stages of Plasmodium falciparum Malaria Parasites

M Leshabane, GA Dziwornu, D Coertzen… - ACS Infectious …, 2021 - ACS Publications
The continued emergence of resistance to front-line antimalarial treatments is of great
concern. Therefore, new compounds that potentially have a novel target in various …

Antimalarial benzimidazole derivatives incorporating phenolic mannich base side chains inhibit microtubule and hemozoin formation: structure–activity relationship …

GA Dziwornu, D Coertzen, M Leshabane… - Journal of medicinal …, 2021 - ACS Publications
A novel series of antimalarial benzimidazole derivatives incorporating phenolic Mannich
base side chains at the C2 position, which possess dual asexual blood and sexual stage …

Antiplasmodial activity, structure–activity relationship and studies on the action of novel benzimidazole derivatives

N Escala, LM Pineda, MG Ng, LM Coronado… - Scientific Reports, 2023 - nature.com
Malaria cases and deaths keep being excessively high every year. Some inroads gained in
the last two decades have been eroded especially due to the surge of resistance to most …

Novel 3-Trifluoromethyl-1,2,4-oxadiazole Analogues of Astemizole with Multi-stage Antiplasmodium Activity and In Vivo Efficacy in a Plasmodium berghei Mouse …

D Mambwe, CM Korkor, A Mabhula… - Journal of medicinal …, 2022 - ACS Publications
Iterative medicinal chemistry optimization of an ester-containing astemizole (AST) analogue
1 with an associated metabolic instability liability led to the identification of a highly potent 3 …

[HTML][HTML] Current status of antihistamine drugs repurposing for infectious diseases

BL Travi - Medicine in Drug Discovery, 2022 - Elsevier
Objectives The principal objectives of this review were to gather information on the potential
role of antihistamines as anti-infective agents and to identify the gaps in research that have …

Targeting virulence factors as an antimicrobial approach: pigment inhibitors

S Ni, B Li, Y Xu, F Mao, X Li, L Lan… - Medicinal Research …, 2020 - Wiley Online Library
The fascinating and dangerous colored pathogens contain unique chemically pigmented
molecules, which give varied and efficient assistance as virulence factors to the crucial …

Metal-Free Synthesis of Heteroaryl Amines or Their Hydrochlorides via an External-Base-Free and Solvent-Free C–N Coupling Protocol

GG Fan, BW Jiang, W Sang, H Cheng… - The Journal of …, 2021 - ACS Publications
Herein, a metal-free and solvent-free protocol was developed for the C–N coupling of
heteroaryl halides and amines, which afforded numerous heteroaryl amines or their …

Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in Plasmodium falciparum

A Lawong, S Gahalawat, J Okombo… - Journal of medicinal …, 2021 - ACS Publications
Malaria control programs continue to be threatened by drug resistance. To identify new
antimalarials, we conducted a phenotypic screen and identified a novel tetrazole-based …