Global ETD Search
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Showing 1 to 10 of 10 for “"β-Carboline"”.
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Hit to Lead Stage Optimization of Orally Efficacious β-Carboline Antimalarials
… develop and synthesize new drugs. Tetrahydro-β-carboline acid (THβC) 1-(2,4-dichlorophenyl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-2-ium-3-carboxylate (MMV008138) has promising antimalarial properties; it was discovered by screening the Malaria Box with the so-called IPP Rescue assay. This …
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Synthesis of the Antimalarial Flindersial Alkaloids
… vinylogous Pictet-Spengler reaction to give a β-carboline, which opens to a 2-enone tryptamine in the presence of base. A BINOL catalyzed enantioselective conjugate addition of a vinyl boronic acid to the 2-enone tryptamine has been achieved. A pyrrolo[a]indole unit could be connected to another …
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Further Exploring the Structure Activity Relationship (SAR) of MMV008138 and MMV1803522
… antimalarial drug candidate MMV1803522. This β-carboline-3-carboxamide shows good in vitro growth inhibition potency of Dd2 strain P. falciparum, operating by a still unknown mechanism. To investigate the pharmacophore of this lead, I first sought to determine whether the pyridine N (i.e. N2) of …
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Exploring the molecular diversity and biomedicinal potential of marine invertebrates and South African actinomycetes for tuberculosis drug discovery
… the isolation of three new natural products, a β-carboline alkaloid (1- (1,2-dihydroxyethyl)-1,2,3,4-tetrahydro-β-carboline-3-carboxylic acid), a peptide (N-(2- phenylacetyl)-serine), and a glycosylated lactone (4-O-(β-glucopyranosyl)-5-(hydroxymethyl)-3- …
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Optimization of Enantiopure tetrahydro-β-carbolines as Potent Antimalarials and Exploration of salicylic acid analogs for combating multidrug-resistant Neisseria gonorrhoeae
… mechanisms of action, identified tetrahydro-β-carboline 2-1 (MMV008138) as an inhibitor of the MEP pathway. Chapter 2 of this work discusses similarity searching of the Novartis portion of the hit set (5K compounds), from the original 20K compound hit set of the Malaria Box, and identifying …
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Novel Antimalarial Compounds from the Optimization of the Malaria Box
… of various substitution on the tetrahydro-β-carboline conformation and D-ring orientation was studied. In the course of preparing the C1-Me analog of MMV008138 featuring 2',4'- dichloro substitution, unexpected ring-expanded azepane products were isolated. Later it was found that the desired …
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Neurodegeneration und Neuroprotektion bei der Parkinson-Krankheit: Untersuchungen von β-Carbolinen und dem Dopaminagonisten Lisurid in der dopaminergen mesencephalen Primärzellkultur des Mausstammes C57Bl/6
β-Carboline sind heterozyklische Indolalkaloide, die ubiquitär in unserer Umwelt und Nahrung vorkommen, aber auch endogen aus Tryptophan gebildet werden können. Aufgrund der strukturellen Verwandtschaft bestimmter β-Carboline zu dem dopaminergen Neurotoxin MPP+ wird ein möglicher Beitrag zur …
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Natural Products Chemistry of Leads Acting on MRSA, HCV, Malaria, and Depression Disorders
… multi-heterocyclic ring system coupled to a β-carboline moiety. Manzamine A shopotent in vitro antimalarial activity against P. falciparum D6 and W2 (0.017-0.020 µM), but its toxicity hindered its development as a drug lead. Malaria, a major tropical infectious disease caused primarily by the …
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1,3-Disubstituted-tetrahydro-β-carbolines: A New Method for Stereochemical Assignment and Synthesis of Potential Antimalarial Agents
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 century were largely successful, the recent rise in resistance to antimalarial treatments resulted in an increasing …