1192015-16-9Relevant academic research and scientific papers
IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS HISTONE DEMETHYLASE INHIBITORS
-
Paragraph 0134, (2018/01/15)
This disclosure relates, inter alia, to compounds that inhibit histone demethylase activity. In particular, the disclosure relates to compounds that inhibit histone lysine demethylase KDM5B, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions disclosed herein.
5-(2-Pyrimidinyl)-imidazo[1,2-a]pyridines are antibacterial agents targeting the ATPase domains of DNA gyrase and topoisomerase IV
Starr, Jeremy T.,Sciotti, Richard J.,Hanna, Debra L.,Huband, Michael D.,Mullins, Lisa M.,Cai, Hongliang,Gage, Jeffrey W.,Lockard, Mandy,Rauckhorst, Mark R.,Owen, Robert M.,Lall, Manjinder S.,Tomilo, Mark,Chen, Huifen,McCurdy, Sandra P.,Barbachyn, Michael R.
experimental part, p. 5302 - 5306 (2010/05/02)
Dual inhibitors of bacterial gyrB and parE based on a 5-(2-pyrimidinyl)-imidazo[1,2-a]pyridine template exhibited MICs (μg/mL) of 0.06-64 (Sau), 0.25-64 (MRSA), 0.06-64 (Spy), 0.06-64 (Spn), and 0.03-64 (FQR Spn). Selected examples were efficacious in mouse sepsis and lung infection models at 50 mg/kg (PO dosing).
