Facile microwave-assisted synthesis and antitubercular evaluation of novel aziridine derivatives

Sarojini, Perumal; Jeyachandran, M.; Sriram, Dharmarajan; Ranganathan, Palraj; Gandhimathi, S.

doi:10.1016/j.molstruc.2021.130038

Cited by 4 publications

(3 citation statements)

References 28 publications

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“…Among them a large variety of compounds are active against various types of oncological diseases. 97 However, several molecules displayed inhibitory activity towards other biological targets such proving to be good glucocerebrosidase (GBA), 98 cysteine proteases, 99 tuberculosis, 100 microbial, 101 and Leishmania 102 inhibitors (Fig. 1).…”

Section: Biological Activities Of Aziridinesmentioning

confidence: 99%

Recent advances in the accessibility, synthetic utility, and biological applications of aziridines

Dank

Ielo

2023

Org. Biomol. Chem.

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Section: Biological Activities Of Aziridinesmentioning

confidence: 99%

Recent advances in the accessibility, synthetic utility, and biological applications of aziridines

Dank

Ielo

2023

Org. Biomol. Chem.

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“…[62] Jeyachandran et al have reported 2-(aryloxy methyl)aziridines ( 35) and 2-((3-aryl-1phenylallyloxy)methyl)aziridine (36) with MIC of 0.5 μg/mL having three-fold activity than standard drugs like ciprofloxacin and ethambutol as compared to ethambutol (MIC of 0.5 μg/ mL). [63] Chakravarty et al have reported anthracenyl phosphonate and π-conjugated acid cocrystals (37) with MIC of 1.56 μg/ mL, as active as ethambutol. These cocrystals have shown better anti-tubercular activity as compared to individual compounds due to hydrogen bonding interactions ( 31 P/ 1 H NMR) enhancing the hydrophobicity to penetrate the mycobacterial cell wall.…”

Section: Othersmentioning

confidence: 99%

“…Jeyachandran et al . have reported 2‐(aryloxy methyl)aziridines ( 35 ) and 2‐((3‐aryl‐1‐phenylallyloxy)methyl)aziridine ( 36 ) with MIC of 0.5 μg/mL having three‐fold activity than standard drugs like ciprofloxacin and ethambutol as compared to ethambutol (MIC of 0.5 μg/mL) [63] . Chakravarty et al .…”

Section: Introductionmentioning

confidence: 99%

Comprehensive Coverage on Anti‐mycobacterial Endeavour Reported in 2021

et al. 2022

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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.

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Green Synthesis of Molecules for the Treatment of Neglected Diseases

Schumacher

Baroni

Alves

et al. 2023

CTMC

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Neglected tropical diseases (NTDs) affect mainly poor and marginalized populations of tropical and subtropical areas in 150 countries. Many of the chemical processes involved in the synthesis of active pharmaceutical ingredients (APIs) are highly polluting and inefficient, both in terms of materials and energy-consuming. In this review, we present the green protocols developed in the last 10 years to access new small molecules with potential applications in the treatment of leishmania, tuberculosis, malaria, and Chagas disease. The use of alternative and efficient energy sources, like microwaves and ultrasound, as well as reactions using green solvents and solvent-free protocols, are discussed in this review.

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Facile microwave-assisted synthesis and antitubercular evaluation of novel aziridine derivatives

Cited by 4 publications

References 28 publications

Recent advances in the accessibility, synthetic utility, and biological applications of aziridines

Recent advances in the accessibility, synthetic utility, and biological applications of aziridines

Comprehensive Coverage on Anti‐mycobacterial Endeavour Reported in 2021

Green Synthesis of Molecules for the Treatment of Neglected Diseases

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