Structure activity relationship in β-carboline derived anti-malarial agents

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ID: 271215
2021
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Abstract
Malaria, even though an avoidable and treatable disease, can be fatal if ignored. Artemisinin Combination Therapy (ACT) and RTS, S/AS01 vaccine (Mosquirix™) are the only modest means available with humans to overcome malaria, a lethal affliction wreaking havoc across the globe. Employment of ACT is associated with problems such as "Artemisinin Resistance" and the "Hypnozoite conundrum" that hinder the complete eradication of malaria. In this view, the natural products specifically comprising β-carboline scaffold have shown good antiplasmodial responses against different strains of malaria. Taking these observations forward, researchers have performed structure-activity relationship (SAR) studies around three different β-carboline skeletons (tetrahydro β-carbolines, dihydro β-carbolines, β-carbolines) to design new β-carboline derived heterocyclic structures or modified naturally occurring derivatives. In addition, different approaches such as dimerization and linkage to other moieties have also been adopted to enhance the antimalarial activity. The present review describes a comprehensive SAR study encapsulating various natural and synthetic β-carbolines to elaborate upon the utility of these skeletons in designing drugs to subdue this deadly disease.
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a2021europeanstructure Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Kamboj A;Sihag B;Brar DS;Kaur A;Salunke DB;;
Journal European journal of medicinal chemistry
Year 2021
DOI
DOI not found
URL
http://www.ncbi.nlm.nih.gov/pubmed/34058709
Keywords
National Center for Biotechnology Information NCBI NLM MEDLINE review humans pubmed abstract nih national institutes of health national library of medicine molecular structure antimalarials / therapeutic use* malaria / drug therapy* pmid:34058709 doi:10.1016/j.ejmech.2021.113536 aarzoo kamboj binita sihag deepak b salunke antimalarials / chemical synthesis antimalarials / chemistry carbolines / chemical synthesis carbolines / chemistry carbolines / therapeutic use*

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