Literature DB >> 34171661

Recent advancements in anti-leishmanial research: Synthetic strategies and structural activity relationships.

Ojasvi Gupta1, Tathagata Pradhan1, Rohit Bhatia2, Vikramdeep Monga3.   

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.
Copyright © 2021 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Chalcone; DHFR; Leishmaniasis; Quinolone; ROS; Triazole

Year:  2021        PMID: 34171661     DOI: 10.1016/j.ejmech.2021.113606

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  3 in total

1.  Antimicrobial Activity and DFT Studies of a Novel Set of Spiropyrrolidines Tethered with Thiochroman-4-one/Chroman-4-one Scaffolds.

Authors:  Nourhène Chouchène; Amani Toumi; Sarra Boudriga; Hayet Edziri; Mansour Sobeh; Mohamed A O Abdelfattah; Moheddine Askri; Michael Knorr; Carsten Strohmann; Lukas Brieger; Armand Soldera
Journal:  Molecules       Date:  2022-01-18       Impact factor: 4.411

2.  New quinoline-based triazole hybrid analogs as effective inhibitors of α-amylase and α-glucosidase: Preparation, in vitro evaluation, and molecular docking along with in silico studies.

Authors:  Yousaf Khan; Shahid Iqbal; Mazloom Shah; Aneela Maalik; Rafaqat Hussain; Shoaib Khan; Imran Khan; Rami Adel Pashameah; Eman Alzahrani; Abd-ElAziem Farouk; Mohammed Issa Alahmdi; Hisham S M Abd-Rabboh
Journal:  Front Chem       Date:  2022-09-15       Impact factor: 5.545

3.  Total Synthesis of the Natural Chalcone Lophirone E, Synthetic Studies toward Benzofuran and Indole-Based Analogues, and Investigation of Anti-Leishmanial Activity.

Authors:  Luca Pozzetti; Roberta Ibba; Sara Rossi; Orazio Taglialatela-Scafati; Donatella Taramelli; Nicoletta Basilico; Sarah D'Alessandro; Silvia Parapini; Stefania Butini; Giuseppe Campiani; Sandra Gemma
Journal:  Molecules       Date:  2022-01-11       Impact factor: 4.411

  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.