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 …
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
Virtual ligand screening of a publicly available database of antimalarial hits using a
pharmacophore derived from antimalarial MMV008138 identified TCMDC-140230, 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 …
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 …
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 …
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
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 …
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)
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 …
(TCAMS) are described. A triazolopyrimidine series was deprioritized due to delayed …
Current development of β-carboline derived potential antimalarial scaffolds
Abstract β-Carboline alkaloids are an eminent class of nitrogen-based natural alkaloids and
therapeutic molecules which exert various pharmacological activities through diverse …
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 …
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
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 …
cure of malaria requires intervention at various stages in the development of the parasite …