02578nas a2200229   4500008004100000022001400041245019000055210006900245260007300314300001000387490000700397520165500404653002102059653002902080653002002109653002102129653001702150100001702167700001802184700001902202856012702221       2008                        eng d  a0924-857900aBactericidal activity of 2-nitroimidazole against the active replicating stage of mycobacterium bovis BCG and mycobacterium tuberculosis with intracellular efficacy in THP-1 macrophages0 aBactericidal activity of 2nitroimidazole against the active repl  aPO BOX 211, 1000 AE AMSTERDAM, NETHERLANDSbELSEVIER SCIENCE BVcJUL  a40-450 v323 a<p>This study evaluated the antituberculous potential of 2-nitroimidazole under in vitro conditions. Minimal bactericidal concentrations of the compound against actively replicating Mycobacterium bovis BCG and Mycobacterium tuberculosis H37Ra were found to be 0.226 mu g/mL and 0.556 mu g/mL in enriched and minimal medium, respectively. Minimal inhibitory concentrations were &gt; 100 times lower than reported antituberculous nitroimidazoles such as nitrofurantoin and furaltadone, indicating the greater potential of 2-nitroimidazole. No discernible effect of 2-nitroimidazole was seen on saprophytic Mycobacterium smegmatis and the representative bacterial strain Escherichia coli DH5 alpha, indicating the specificity of the molecule against tuberculous mycobacteria. The compound was also found to be effective against M. tuberculosis in the intracellular environment of the human monocytic cell line THP-1, with a reduction in viability of bacilli by 2.5 log after 144 h of incubation at a concentration of 0.113 mu g/mL. A five-fold higher concentration (0.565 mu g/mL) of 2-nitroimidazole sterilised the macrophages of intracellular pathogens within 192 h, without affecting the host. However, 2-nitroimidazole was unable to affect significantly the viability of dormant non-replicating bacilli of M. bovis BCG and M. tuberculosis in Wayne's in vitro model. Overall, the results indicate that 2-nitroimidazole is a potent antituberculous agent active against the organism's active replicating stage, with promising intracellular efficacy as well. (c) 2008 Elsevier B.V. and the International Society of Chemotherapy. All rights reserved.</p>10a2-nitroimidazole10aantimycobacterial agents10anitroimidazoles10aTHP-1 macrophage10atuberculosis1 aKhan, Arshad1 aSarkar, Sampa1 aSarkar, Dhiman  uhttps://library.ncl.res.in/content/bactericidal-activity-2-nitroimidazole-against-active-replicating-stage-mycobacterium-002091nas a2200241   4500008004100000022001400041245016100055210006900216260000900285300001500294490000600309520119300315653002901508653002601537653001901563653003701582653001901619100001801638700001701656700001901673700002501692856013201717       2023                        eng d  a2365-654900aDesign, synthesis, and in vitro biological evaluation of ROS-generating phenanthridin-trione-epoxide conjugates as agents against mycobacterium tuberculosis0 aDesign synthesis and in vitro biological evaluation of ROSgenera  cJUL   ae2023004160 v83 a<p>
	Tuberculosis (TB) is one of the devasting infectious diseases and continues to spread among people despite having several specific drugs. Total eradication of TB is one of the shared interests of both the World Health Organization (WHO) and India globally. A library of antitubercular 6-((1-(aryl/heteroaryl)-1H-1,2,3-triazol-4-yl)methyl)oxireno[2,3-b] phenanthridine-5,7,9(6H,7aH,8aH)-trione (6 a-e) has been prepared in five steps including click chemistry and tested against active and dormant strains of Mycobacterium tuberculosis H37Ra using XRMA protocol. The result showed the inhibitory potential of 6 d IC50 at 0.74 &amp; mu;g/mL concentration against active strain and at 0.9 &amp; mu;g/mL against the dormant strain of Mtb. ROS generating ability of the compounds has been confirmed by luminol, H2O2, and glutathione assays. The molecular docking with the thioredoxin protein of Mtb showed a docking score of -9.6 Kcal/mol. To understand the mechanism with the thioredoxin protein of Mtb, the adduct formation of compounds with cystine was confirmed with HPLC. The involvement of lead molecules with existing drugs can be helpful in the eradication of tuberculosis.</p>
10aantimycobacterial agents10aComputational docking10aCystine adduct10aEpoxy-Phenanthridinone-triazoles10aROS generation1 aMamgain, Ritu1 aSwami, Sagar1 aSarkar, Dhiman1 aSrivastava, Pratibha  uhttps://library.ncl.res.in/content/design-synthesis-and-vitro-biological-evaluation-ros-generating-phenanthridin-trione-epoxide