1, 3-Disubstituted-tetrahydro-β-carbolines: A New Method for Stereochemical Assignment and Synthesis of Potential Antimalarial Agents

K Cagasova - 2021 - vtechworks.lib.vt.edu
Malaria is a serious mosquito-borne disease affecting the majority of Earth's southern
hemisphere. While consistent efforts to curb malaria spread throughout 20th and early 21st …

Malaria Box-Inspired Discovery of N-Aminoalkyl-β-carboline-3-carboxamides, a Novel Orally Active Class of Antimalarials

J Mathew, S Ding, KA Kunz, EE Stacy… - ACS Medicinal …, 2022 - ACS Publications
Virtual ligand screening of a publicly available database of antimalarial hits using a
pharmacophore derived from antimalarial MMV008138 identified TCMDC-140230, a …

Enantiopure Benzofuran-2-carboxamides of 1-Aryltetrahydro-β-carbolines Are Potent Antimalarials In Vitro

H Almolhim, S Ding, JH Butler… - ACS Medicinal …, 2022 - ACS Publications
The tetrahydro-β-carboline scaffold has proven fertile ground for the discovery of
antimalarial agents (eg, MMV008138 (1) and cipargamin (2)). Similarity searching of a …

[PDF][PDF] Hit to Lead Stage Optimization of Orally Efficacious β-Carboline Antimalarials

J Mathew - 2022 - vtechworks.lib.vt.edu
Malaria, a disease caused by the parasite Plasmodium, continues to be one of the deadliest
diseases worldwide. The WHO reported over 627,000 deaths in 2020, and over 1 billion …

Synthesis and Evaluation of 1‐Amino‐6‐halo‐β‐carbolines as Antimalarial and Antiprion Agents

MJ Thompson, JC Louth, SM Little… - …, 2012 - Wiley Online Library
Malaria is one of the world's most devastating parasitic diseases, causing almost one million
deaths each year. Growing resistance to classical antimalarial drugs, such as chloroquine …

Probing the B-& C-rings of the antimalarial tetrahydro-β-carboline MMV008138 for steric and conformational constraints

S Ding, M Ghavami, JH Butler, EF Merino… - Bioorganic & medicinal …, 2020 - Elsevier
The antimalarial candidate MMV008138 (1a) is of particular interest because its target
enzyme (IspD) is absent in human. To achieve higher potency, and to probe for steric …

Cyclopropyl carboxamides: a new oral antimalarial series derived from the Tres Cantos anti-malarial set (TCAMS)

L Rueda, I Castellote, J Castro-Pichel… - ACS Medicinal …, 2011 - ACS Publications
Rapid triaging of three series of related hits selected from the Tres Cantos Anti-Malarial Set
(TCAMS) are described. A triazolopyrimidine series was deprioritized due to delayed …

Current development of β-carboline derived potential antimalarial scaffolds

P Kushwaha, V Kumar, B Saha - European Journal of Medicinal Chemistry, 2023 - Elsevier
Abstract β-Carboline alkaloids are an eminent class of nitrogen-based natural alkaloids and
therapeutic molecules which exert various pharmacological activities through diverse …

New antimalarials identified by a cell-based phenotypic approach: structure–activity relationships of 2, 3, 4, 9-tetrahydro-1H-β-carboline derivatives possessing a 2 …

N Cho, K Kikuzato, Y Futamura, T Shimizu… - Bioorganic & Medicinal …, 2022 - Elsevier
The identification, structure–activity relationships (SARs), and biological effects of new
antimalarials consisting of a 2, 3, 4, 9-tetrahydro-1H-β-carboline core, a coumarin ring, and …

3, 5-Bis (benzylidene)-4-piperidones and related N-acyl analogs: A novel cluster of antimalarials targeting the liver stage of Plasmodium falciparum

U Das, RSP Singh, J Alcorn, MR Hickman… - Bioorganic & medicinal …, 2013 - Elsevier
Drug resistance is a major challenge in antimalarial chemotherapy. In addition, a complete
cure of malaria requires intervention at various stages in the development of the parasite …