13301-04-7Relevant articles and documents
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.
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.
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.
