02684nas a2200301   4500008004100000022001400041245015500055210006900210260000800279300002100287490000700308520162000315653001601935653003001951653001601981653002301997653002002020653002202040653002102062100002402083700002202107700002002129700002202149700003102171700001902202700003002221856013102251       2018                        eng d  a1420-304900aUltrasound assisted synthesis of 4-(Benzyloxy)-N-(3-chloro-2-(substitutedphenyl)-4-oxoazetidin-1-yl) benzamide as challenging anti-tubercular scaffold0 aUltrasound assisted synthesis of 4BenzyloxyN3chloro2substitutedp  cAUG  aArticle No: 19450 v233 a<p>A series of ten novel derivatives of 4-(benzyloxy)-N-(3-chloro-2-(substituted phenyl)-4-oxoazetidin-1-yl) benzamide 6a-j were synthesized in good yield from the key compound 4-(benzyloxy)-N-(substituted benzylidene) benzo hydrazide, called Schiff `s bases 5a-j, by Staudinger reaction ([2 + 2] ketene-imine cycloaddition reaction) with chloro acetyl chloride in the presence of catalyst tri ethylamine and solvent dimethyl formamide (DMF), by using ultra-sonication as one of the green chemistry tools. All the synthesised compounds were evaluated for in vitro anti-tubercular activity against Mycobacterium tuberculosis (MTB) and most of them showed promising activity with an IC50 value of less than 1 mu g/mL. To establish the safety, all the synthesized compounds were further tested for cytotoxicity against the human cancer cell line HeLa and all 6a-j compounds were found to be non-cytotoxic in nature. The molecular docking study was carried out with essential enzyme InhA (FabI/ENR) of Mycobacterium responsible for cell wall synthesis which suggests that 6a and 6e are the most active derivatives of the series. The theoretical evaluation of cell permeability based on Lipinski's rule of five has helped to rationalize the biological results and hence the synthesized azetidinone derivatives 6a-j were also analyzed for physicochemical evaluation that is, absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties and the results showed that all the derivatives could comply with essential features required for a potential lead in the anti-tubercular drug discovery process.</p>10aADMET study10aanti-tubercular screening10aazetidinone10acytotoxicity study10agreen chemistry10aMolecular docking10aultra-sonication1 aNimbalkar, Urja, D.1 aSeijas, Julio, A.1 aBorkute, Rachna1 aDamale, Manoj, G.1 aSangshetti, Jaiprakash, N.1 aSarkar, Dhiman1 aNikalje, Anna, Pratima G.  uhttps://library.ncl.res.in/content/ultrasound-assisted-synthesis-4-benzyloxy-n-3-chloro-2-substitutedphenyl-4-oxoazetidin-1-yl02012nas a2200181   4500008004100000022001400041245013800055210006900193260000800262300001300270490000700283520133400290100001701624700002001641700001901661700001901680856013101699       2019                        eng d  a1932-620300aUsing diphenyleneiodonium to induce a viable but non-culturable phenotype in Mycobacterium tuberculosis and its metabolomics analysis0 aUsing diphenyleneiodonium to induce a viable but nonculturable p  cAUG  ae02206280 v143 a<p>Depletion of oxygen levels is a well-accepted model for induction of non-replicating, persistent states in mycobacteria. Increasing the stress levels in mycobacterium bacilli facilitates their entry into a non-cultivable, dormant state. In this study, it was shown that diphenyleneiodonium, an inhibitor of NADH oxidase, induced a viable, but non-culturable state in mycobacteria, having similar features to dormant bacilli, like loss of acid-fastness, upregulation of stress-regulated genes and decreased superoxide levels as compared to actively growing bacilli. Comprehensive, untargeted metabolic profiling also confirmed a decrease in biogenesis of amino acids, NAD, unsaturated fatty acids and nucleotides. Additionally, an increase in the level of lactate, fumarate, succinate and pentose phosphate pathways along with increased mycothiol and sulfate metabolites, similar to dormant bacilli, was observed in the granuloma. These non-cultivable bacilli were resuscitated by supplementation of fetal bovine serum, regaining their culturability in liquid as well as on agar medium. This study focused on the effect of diphenyleneiodonium treatment in causing mycobacteria to rapidly transition from an active state into a viable, but non-cultivable state, and comparing their characteristics with dormant phenotypes.</p>
1 aYeware, Amar1 aGample, Suwarna1 aAgrawal, Sonia1 aSarkar, Dhiman  uhttps://library.ncl.res.in/content/using-diphenyleneiodonium-induce-viable-non-culturable-phenotype-mycobacterium-tuberculosis