- 2-Arylidene Hydrazinecarbodithioates as Potent, Selective Inhibitors of Cystathionine γ-Lyase (CSE)
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Hydrogen sulfide is produced from l-cysteine by the action of both cystathionine γ-lyase (CSE) and cystathionine β-synthase (CBS) and increasingly has been found to play a profound regulatory role in a range of physiological processes. Mounting evidence suggests that upregulation of hydrogen sulfide biosynthesis occurs in several disease states, including rheumatoid arthritis, hypertension, ischemic injury, and sleep-disordered breathing. In addition to being critical tools in our understanding of hydrogen sulfide biology, inhibitors of CSE hold therapeutic potential for the treatment of diseases in which increased levels of this gasotransmitter play a role. We describe the discovery and development of a novel series of potent CSE inhibitors that show increased activity over the benchmark inhibitor and, importantly, display high selectivity for CSE versus CBS.
- Bhattacharjee, Abir,Sinha, Antara,Ratia, Kiira,Yin, Liang,Delgado-Rivera, Loruhama,Petukhov, Pavel A,Thatcher, Gregory R. J.,Wardrop, Duncan J.
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- Copper-catalyzed aerobic carboxygenation and N-arylation of [1,2,3]triazolo[1,5-a]pyridines towards pyridinium triazolinone ylides
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Copper-catalyzed aerobic oxyarylation of [1,2,3]triazolo[1,5-a]pyridines is developed. Notably molecular oxygen was utilized as one of the reagents and the transformation resulted in the formation of novel pyridinium triazolinone ylides. A basic mechanism for the one-pot process is proposed and further functionalization of the ylidic products were also presented.
- Pankajakshan, Sreekumar,Chng, Zhi Guang,Ganguly, Rakesh,Loh, Teck Peng
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supporting information
p. 5929 - 5931
(2015/03/30)
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- Triazolopyridines. Part 6. Ring Opening Reactions of Triazolopyridines
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The triazole ring in 1,2,3-triazolo-pyridines and -quinolines, and in 1,2,3-triazoloisoquinolines can be opened with loss of nitrogen.The reagents described are bromine, aqueous sulphuric acid, glacial acetic acid, and selenium dioxide; the products from the triazolopyridines are dibromomethyl, hydroxymethyl, acetoxymethyl, and acyl derivatives of pyridine.The generality of the reactions is discussed.The first reported reaction in which the six-membered ring of a 1,2,3-triazolopyridine is opened, by hydride reduction, gives a triazolylbutadiene.
- Jones, Gurnos,Mouat, Deborah J.,Tonkinson, Daryl J.
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p. 2719 - 2724
(2007/10/02)
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