Comprehensive Coverage on Anti‐mycobacterial Endeavour Reported in 2021

Abstract

Tuberculosis (TB) has been the highly contagious airborne disease caused by Mycobacterium tuberculosis and the major leading infectious disease with the higher upsurge of morbidity and mortality. Owing to problems in the current regimen for TB and emergence of drug resistance strains, there is a strong necessity for development of new anti-TB drugs with better efficacy, reduced duration of action, along with improved patient compliance. Towards this, the scaffolds reported in 2021 with anti-tubercular activity such as benzofuran, benzothiazinone, benzimidazoles, indole, piperidine, piperazine, pyrazole, pyridine, pyrimidine, pyrrolidine, quinoxaline, triazole, etc. have been critically reviewed along with their structureactivity relationships, mode of actions with anticipations of intuitions to design the newer anti-mycobacterial scaffolds.The present work provide the organized coverage of diversified scaffolds with anti-tubercular profile reported in 2021 along with the insightful discussion on their merits and demerits. The mode of anti-tubercular action against Mycobacterium tuberculosis strains have been presented keeping in mind the novel drug candidates against drug resistant strains [a] Dr.

In‐silico Computational Investigations of AntiViral Lignan Derivatives as Potent Inhibitors of SARS CoV‐2

“…Several heterocycles have been reported as anti‐infectious agents against pathogemic microorganisms[ 55 , 56 , 57 , 58 , 59 ] with their greener synthesis. [ 60 , 61 , 62 , 63 ] Following this, heterocyclic ligands such as savinin and cleistantoxin showed the inhibition of papain‐like protease (PDB ID: 6W6Y) with docking scores of −8.05 and −7.66, respectively, which are superior to the remdesivir (docking score of −7.37).…”

Synthesis of Nitrogen- and Oxygen-Containing Heterocycles Catalysed by Metal Nanoparticles Reported in 2022

“…42 Several three-to seven-membered heterocyclic ring systems have been synthesised using MNPs as catalysts, as evident from the published literature from the scientific community. 43 As part of the on-going research endeavour from this laboratory for the synthesis of such heterocyclic scaffolds [44][45][46][47][48][49][50][51] with biological importance, [52][53][54][55] we provided a decennary report on MNP-catalysed synthesis of heterocycles published during 2010-2019, 49 and kept updating the same for 2020 50 and 2021. 45 Herein, we have provided further updates of the review on the metal nanoparticle-catalysed synthesis of aza-and oxa-heterocycles, with a primary focus on the mechanistic insights into MNPs and synthetic approaches to heterocyclic scaffolds, together with their elaborated understandings, reported during the calendar year 2022 (Table 1).…”

“…Laffafchi and colleagues published the one-pot, threecomponent, regioselective synthesis of 1,2,3-triazoles (55) via click reaction of substituted alkynes (25), aryl halides (53), and sodium azide (54) with sodium ascorbate in the presence of Fe 3 O 4 @Creatine@Cu catalysts under mild conditions at 60 °C (Scheme 13). 67 The Fe 3 O 4 NPs prepared from ferrous and ferric salts were sequentially functionalised with creatinine and 2-(2-hydroxyethoxy)benzaldehyde followed by complexation using Cu salts to get the final MNPs.…”

Thiazole Heterocycle: An Incredible and Potential Scaffold in Drug Discovery and Development of Antitubercular Agents

“…In the present scenario, many heterocyclic compounds have been proven to be potent against different strains of M.tb., [25,27] which has attracted medicinal chemists all across the globe to search for various efficient novel compounds with the heterocyclic nucleus as their main core and have been evident to show a high rate of inhibition (Figure 2). [28,29]…”