13669-57-3Relevant articles and documents
Discovery of Inhibitors of the Lipopolysaccharide Transporter MsbA: From a Screening Hit to Potent Wild-Type Gram-Negative Activity
Verma, Vishal A.,Wang, Lan,Labadie, Sharada S.,Liang, Jun,Sellers, Benjamin D.,Wang, Jian,Dong, Liting,Wang, Qiuyue,Zhang, Shuang,Xu, Zhongya,Zhang, Yexia,Niu, Yanan,Wang, Xinxin,Wai, John,Koehler, Michael F. T.,Hu, Huiyong,Alexander, Mary Kate,Nishiyama, Mireille,Miu, Anh,Xu, Yiming,Pang, Jodie,Katakam, Anand K.,Reichelt, Michael,Austin, Cary D.,Ho, Hoangdung,Payandeh, Jian,Koth, Christopher M.
supporting information, p. 4085 - 4120 (2022/03/02)
The dramatic increase in the prevalence of multi-drug resistant Gram-negative bacterial infections and the simultaneous lack of new classes of antibiotics is projected to result in approximately 10 million deaths per year by 2050. We report on efforts to target the Gram-negative ATP-binding cassette (ABC) transporter MsbA, an essential inner membrane protein that transports lipopolysaccharide from the inner leaflet to the periplasmic face of the inner membrane. We demonstrate the improvement of a high throughput screening hit into compounds with on-target single digit micromolar (μM) minimum inhibitory concentrations against wild-type uropathogenic Escherichia coli, Klebsiella pneumoniae, and Enterobacter cloacae. A 2.98 ? resolution X-ray crystal structure of MsbA complexed with an inhibitor revealed a novel mechanism for inhibition of an ABC transporter. The identification of a fully encapsulated membrane binding site in Gram-negative bacteria led to unique physicochemical property requirements for wild-type activity.
2,2,3-Tribromopropanal as a versatile reagent in the skraup-type synthesis of 3-bromoquinolin-6-ols
Lamberth, Clemens,Kessabi, Fiona Murphy,Beaudegnies, Renaud,Quaranta, Laura,Trah, Stephan,Berthon, Guillaume,Cederbaum, Fredrik,Vettiger, Thomas,Prasanna
, p. 858 - 862 (2014/04/17)
2,2,3-Tribromopropanal, a reagent which almost became forgotten in the chemical literature after its first application in the 1950s, is used for the one-step transformation of diversely substituted 4-nitro- and 4-methoxyanilines into 3-bromo-6-nitroquinolines and 3-bromo-6-methoxyquinolines. These intermediates are then converted, in one further step, into 3-bromoquinolin-6- ols, which may carry additional substituents at positions 7 and 8. Georg Thieme Verlag Stuttgart New York.
TRIAZOLOPYRIDINE COMPOUNDS
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Paragraph 0702, (2013/09/26)
The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound o f formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I)
