92852-66-9Relevant academic research and scientific papers
Design and Synthesis of 5-Oxoimidazolidine Derivatives in Search of Potent Antitubercular and Antifungal agents
Singirisetty, Triveni,Chilamakuru, Naresh Babu,Peraman, Ramalingam,Mallela, Vijaya Jyothi,Sana, Maheswari P.,Begum, Inthiyaz
, p. 441 - 451 (2021/02/02)
5-Oxoimidazolidines are significant outfits because of their impending biological activity and also because of their resourcefulness as synthons in organic revolutions. The designed library was docked against the crystal structure of Mycobacterium tuberculosis enoyl reductase (2B35) and crystal structure of flavohemoglobin (3OZU) to know the best fit molecule. The ADMET parameters revealed that the compounds have synthetic acceptability and leadlikeness. Accordingly, the selected 5-oxoimidazolidines (S1-8 and A1-8) were synthesized from carbohydrazides (1a-h) and characterized by spectral data. Further, these compounds were screened against M. tuberculosis H37RV by microplate Alamar Blue assay method. The compound S3 showed minimum inhibitory concentration at 6.25 μg/mL, while the antifungal screening demonstrated S1 as a promising lead with the corresponding zone of inhibitions of 22 mm and 18 mm against Aspergillus niger and Candida albicans.
Isonicotinic acid hydrazide derivatives: Synthesis, antimicrobial activity, and QSAR studies
Judge, Vikramjeet,Narasimhan, Balasubramanian,Ahuja, Munish,Sriram, Dharmarajan,Yogeeswari, Perumal,De Clercq, Erik,Pannecouque, Christophe,Balzarini, Jan
, p. 1451 - 1470 (2012/09/22)
A series of isonicotinic acid hydrazide derivatives (1-19) was synthesized and tested in vitro for antimycobacterial activity against Mycobacterium tuberculosis and antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Candida albicans, and Aspergillus niger and the results indicated that the compounds with OH, SCH3, and OCH 3 groups were found to be active against the tested strains. None of the test compounds were active against a broad variety of RNA and DNA viruses at subtoxic concentrations, except 8, that showed some selective anti-reovirus-1 activity. The multi-target QSAR models were found to be effective in predicting the antimicrobial activity of the isoniazid derivatives and indicated the importance of nuclear repulsion energy (Nu.E) in explaining the antimicrobial activity of isoniazid derivatives. The developed QSAR models were validated using the external test set of synthesized derivatives. Springer Science+Business Media, LLC 2011.
