13301-04-7Relevant academic research and scientific papers
Aminopyrazinamides: Novel and specific GyrB inhibitors that kill replicating and nonreplicating mycobacterium tuberculosis
Shirude, Pravin S.,Madhavapeddi, Prashanti,Tucker, Julie A.,Murugan, Kannan,Patil, Vikas,Basavarajappa, Halesha,Raichurkar, Anandkumar V.,Humnabadkar, Vaishali,Hussein, Syeed,Sharma, Sreevalli,Ramya,Narayan, Chandan B.,Balganesh, Tanjore S.,Sambandamurthy, Vasan K.
, p. 519 - 523 (2013)
Aminopyrazinamides originated from a high throughput screen targeting the Mycobacterium smegmatis (Msm) GyrB ATPase. This series displays chemical tractability, robust structure-activity relationship, and potent antitubercular activity. The crystal structure of Msm GyrB in complex with one of the aminopyrazinamides revealed promising attributes of specificity against other broad spectrum pathogens and selectivity against eukaryotic kinases due to novel interactions at hydrophobic pocket, unlike other known GyrB inhibitors. The aminopyrazinamides display excellent mycobacterial kill under in vitro, intracellular, and hypoxic conditions.
JAK kinase inhibitor, preparation method thereof, and application in the field of medicines
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Paragraph 0230; 0233-0235, (2019/04/10)
The application relates to a JAK kinase inhibitor, a preparation method thereof, and an application in the field of medicines and belongs to the field of medical chemistry. In the application, a series of novel small-molecular JAK inhibitors are provided and are represented as the general formula (II). The compounds have better effects and higher safety in prevention or treatment on JAK-related adaptation diseases.
BCR-ABL kinase inhibitor and its application (by machine translation)
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, (2017/03/28)
The present invention relates to the field of chemical medicines, in particular to compounds as represented by formula I having BCR-ABL kinase inhibitory activity, or pharmaceutically acceptable salt, isomer, solvate, crystal or prodrug thereof, and pharmaceutical composition containing the compounds, and application of the compounds or compositions in drug preparation. The compounds of the present invention have strong inhibitory effect on BCR-ABL kinase, and can be used to treat diseases such as tumors.
Discovery of a series of imidazopyrazine small molecule inhibitors of the kinase MAPKAPK5, that show activity using in vitro and in vivo models of rheumatoid arthritis
Andrews, Martin J.I.,Andrew Clase,Bar, Gregory,Tricarico, Giovanni,Edwards, Paul J.,Brys, Reginald,Chambers, Mark,Schmidt, Wolfgang,MacLeod, Angus,Hirst, Kim,Allen, Vivienne,Birault, Veronique,Le, Joelle,Harris, John,Self, Andrew,Nash, Kevin,Dixon, Graham
, p. 2266 - 2270 (2012/05/04)
MAPKAPK5 has been proposed to play a role in regulation of matrix metalloprotease expression and so to be a potential target for intervention in rheumatoid arthritis. We present here the identification of a series of compounds against this target which are effective in both biochemical and cell assays. The expansion of the series is described, along with early SAR and pharmacokinetics for some representative compounds.
INHIBITORS OF JAK
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, (2011/04/18)
The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R′, X, X′, Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.
Efficient three-step one-pot synthesis of a novel 2,3,5-substituted pyrazine library
Delvare, Christian,Harris, Craig S.,Hennequin, Laurent,Koza, Patrice,Lambert-Van Der Brempt, Christine,Pelleter, Jacques,Willerval, Olivier
, p. 449 - 452 (2011/11/29)
The partnership between rational synthesis design and mass-triggered preparative LCMS is a powerful one, capable of furnishing very large libraries in a selective manner in a very short space of time. Herein, we communicate one example of possibly a perfect marriage between the synthetic chemistry and the subsequent purification method employed, affording a ~1000-member library supplying 50 mg on average of final compound in less than a month.
