Recent advancements in anti-leishmanial research: Synthetic strategies and structural activity relationships
Ojasvi Gupta1, Tathagata Pradhan1, Rohit Bhatia1
1Department of Pharmaceutical Chemistry, ISF College of Pharmacy, GT Road, Ghal Kalan, Moga, 142001, Punjab, India.
Abstract:
Leishmaniasis is a parasitic neglected tropical disease caused by various species of Leishmania parasite. Despite tremendous advancements in the therapeutic sector and drug development strategies, still the existing anti-leishmanial agents are associated with some clinical issues like drug resistance, toxicity and selectivity. Therefore, several research groups are continuously working towards the development of new therapeutic candidates to overcome these issues. Many potential heterocyclic moieties have been explored for this purpose including triazoles, chalcones, chromone, thiazoles, thiosemicarbazones, indole, quinolines, etc. It is evident from the literature that the majority of anti-leishmanial agents act by interacting with key regulators including PTR-I, DHFR, LdMetAP1, MAPK, 14 α-demethylase and pteridine reductase-I, etc. Also, these tend to induce the production of ROS which causes damage to parasites. In the present compilation, authors have summarized various significant synthetic procedures for anti-leishmanial agents reported in recent years. A brief description of the pharmacological potentials of synthesized compounds along with important aspects related to structural activity relationship has been provided. Important docking outcomes highlighting the possible mode of interaction for the reported compounds have also been included. This review would be helpful to the scientific community to design newer strategies and also to develop novel therapeutic candidates against leishmaniasis.
More Related Videos
08:48Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
Published on: January 26, 2016
10:29Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Related Concept Videos
Structure-Activity Relationships and Drug Design
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
Drug Discovery: Overview
Local Anesthetics: Chemistry and Structure-Activity Relationship
Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
The direct-acting...
Ligand Binding Sites
Protein-ligand interactions are quite specific; even though numerous potential ligands surround a cellular protein at any given time, only a particular ligand can bind to that protein. Moreover, a ligand binds only to a dedicated area on the surface of the protein, known as the...
