2020
DOI: 10.1016/j.heliyon.2020.e04916
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Recent evolution on synthesis strategies and anti-leishmanial activity of β-carboline derivatives – An update

Abstract: Leishmaniasis is the most widespread pathogenic disease in several countries. Currently, no effective vaccines are available, and the control of Leishmaniasis primarily relies on decade-old chemotherapy. The treatment for the Leishmaniasis is not up to the mark. Current therapy for Leishmaniasis is ancient and requires hospitalization for the administration. These medications are also highly toxic and resistant. β-carboline, a natural indole containing alkaloid, holds a vital position in the field of medicinal… Show more

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Cited by 16 publications
(9 citation statements)
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“…They can be classified as α-, β-, γ-, and δ-carbolines, depending on the position of the nitrogen atom of the pyridine ring. These naturally occurring compounds are widely known for their anticancer, antifungal, antibacterial, antileishmanial, and anti-inflammatory properties, among many other biological activities . Compound 818 itself is a tetrahydro-γ-carboline similar to tryptoline, another alkaloid known for its neurological action …”
Section: Resultsmentioning
confidence: 99%
“…They can be classified as α-, β-, γ-, and δ-carbolines, depending on the position of the nitrogen atom of the pyridine ring. These naturally occurring compounds are widely known for their anticancer, antifungal, antibacterial, antileishmanial, and anti-inflammatory properties, among many other biological activities . Compound 818 itself is a tetrahydro-γ-carboline similar to tryptoline, another alkaloid known for its neurological action …”
Section: Resultsmentioning
confidence: 99%
“…Five strains of Leishmania donovani were used: (i) the sodium antimony gluconate (SAG)-sensitive (SAG S ) MHOM/IN/1983/ AG83, (ii) the multidrug resistant field isolate MHOM/IN/ 2009/BHU575/0 (BHU-575), 50 (iii) laboratory grown miltefosineresistant (MIL R ) strains, (iv) camptothecin resistant (CPT R ) strain, and (v) Leishmania major were used in the study. Amastigotes obtained from the spleens of infected hamsters were cultured at 22 1C to obtain promastigotes.…”
Section: Parasite Maintenance and Culturementioning
confidence: 99%
“…EC50 and EC 90 values for the effect of P1 and P3 on the Leishmania promastigotes growth obtained by the trypan blue exclusion method…”
mentioning
confidence: 99%
“…Over the past decades, a considerable number of small‐molecule GSK‐3β inhibitors derived from natural products have been designed for anti‐AD treatment. [ 9,23–29 ] Consequently, the structural modifications based on the α‐carboline scaffold are promising for the development of novel GSK‐3β inhibitors, because the NH group and the pyridine N atom of the structure may have high affinity for the hinge residues in the kinase active pocket. Building on these considerations, we aimed to explore the feasibility of developing α‐carboline‐based derivatives as a new class of GSK‐3β inhibitors.…”
Section: Introductionmentioning
confidence: 99%
“…Over the past decades, a considerable number of small-molecule GSK-3β inhibitors derived from natural products have been designed for anti-AD treatment. [9,[23][24][25][26][27][28][29] Consequently, the structural modifications based on…”
mentioning
confidence: 99%