Electric Literature of 123-06-8, Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. 123-06-8, Name is Ethoxymethylenemalononitrile, SMILES is N#C/C(C#N)=C/OCC, belongs to nitriles-buliding-blocks compound. In a article, author is Zhang, Gang, introduce new discover of the category.
8-cyanobenzothiazinone analogs with potent antitubercular activity
8-Nitrobenzothiazinones (BTZs) exemplified by macozinone are a new class of antitubercular agents with exceptionally potent activity. The aryl nitro group has been considered indispensable for activity since this is bioactivated within mycobacteria by the flavoenzyme DprE1 to a reactive nitroso metabolite that covalently labels Cys387. However, the aryl nitro group is a potential liability with regards to safety, stability, and resistance. In this paper, we introduced a nitrile as a bioisosteric replacement of the nitro group, which we hypothesize can maintain a similar covalent mechanism of inhibition, but mitigate against the aforementioned concerns. 8-cyanobenzothiazinone 1d displayed potent antitubercular activity with an MIC of 130 nM and had an improved volume of distribution in mice that increased the intrinsic half-life by twofold compared to macozinone. Analysis of the C-2 substituent of 1d revealed similar structure-activity relationships as observed for macozinone. Overall, the results confirm the 8-nitro group of benzothiazinones can be successfully replaced with a nitrile to retain useful activity and favorable pharmacokinetic properties. [GRAPHICS] .
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