- 2-Aryl benzazole derived new class of anti-tubercular compounds: Endowed to eradicate mycobacterium tuberculosis in replicating and non-replicating forms
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The high mortality rate and the increasing prevalence of Mtb resistance are the major concerns for the Tuberculosis (TB) treatment in this century. To counteract the prevalence of Mtb resistance, we have synthesized 2-aryl benzazole based dual targeted molecules. Compound 9m and 9n were found to be equally active against replicating and non-replicating form of Mtb (MIC(MABA) 1.98 and 1.66 μg/ml; MIC(LORA) 2.06 and 1.59 μg/ml respectively). They arrested the cell division (replicating Mtb) by inhibiting the GTPase activity of FtsZ with IC50 values 45 and 64 μM respectively. They were also capable of kill Mtb in non-replicating form by inhibiting the biosynthesis of menaquinone which was substantiated by the MenG inhibition (IC50 = 11.62 and 7.49 μM respectively) followed by the Vit-K2 rescue study and ATP production assay.
- Datta, Dhrubajyoti,Debnath, Joy,Franzblau, Scott G.,Ghosh, Kalyan Sundar,Hari, Natarajan,Ma, Rui,Rana, Shiwani,Velappan, Anand Babu
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- Studies on the alkylation of phenolate in an organofluorine solvent and its application to the synthesis of myrsinoic acids A and E
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Among the distinct features of organofluorines, solubility properties to molecules often enable unique applications. More importantly, organofluorines can be compatible with chemical reactions in general, even under harsh conditions. In this context, a study on the alkylation of phenolate using an organofluorine solvent were performed for the preparation of ortho-alkyl phenols. Herewith, the study on the alkylation of phenolate in an organofluorine solvent as well as its application to the synthesis of bioactive terpenylated phenolic natural products, myrsinoic acids A and E, will be reported. Our study suggested that organofluorine solvents could be better alternatives to the conventional nondissociating solvents as organic reaction media to suppress the nondesirable and nonselective side reactions such as in the ortho-alkylation of phenolate.
- Ryu, Miseon,Kim, Minjun,Jeong, Minseon,Jang, Jaebong,Lee, Minyoung,Jin, Hyo-Eon,Jung, Jong-Wha
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p. 818 - 824
(2017/04/06)
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- Applications of the Stereochemically-Controlled Horner-Wittig Reaction: Synthesis of Feniculin, (E)-Non-6-en-1-ol, a Pheromone of the Mediterranean Fruit Fly, (E)- and (Z)-Dec-5-en-1-ol, Tri-substituted Alkenes, and (Z)-α-Bisabolene
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Stereoselective reduction of the appropriate α-diphenylphosphinoyl ketone or addition of the lithium derivative of an alkyl diphenylphospine oxide to an aldehyde or a ketone gives Horner-Wittig intermediates and hence the title compounds.
- Buss, Antony D.,Greeves, Nicholas,Mason, Ralph,Warren, Stuart
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p. 2569 - 2578
(2007/10/02)
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- TRANS ALKENES BY STEREOSELECTIVE REDUCTION OF α-Ph2PO KETONES: E-ISOSAFFROLE, E-ANETHOLE, AND FENICULIN
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Conditions are described for the stereoselective reduction of α-Ph2PO ketones and stereospecific elimination from the resulting threo Horner-Witting intermediates to give pure E-alkenes such as the title compounds.
- Buss, Antony D.,Mason, Ralph,Warren, Stuart
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p. 5293 - 5296
(2007/10/02)
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- Alkynyloxy-phenyl derivatives
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Alkynyl, benzyl or phenyl, ethers and esters which are ring substituted with an oxy or a thio aliphatic chain. These ethers and esters are useful in killing and preventing the proliferation of insects by upsetting their hormonal balance.
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