900297-43-0Relevant articles and documents
PYRAZOLO[1,5-A]PYRIMIDINES AS ANTIVIRAL COMPOUNDS
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, (2016/11/17)
A compound of formula (I) or a pharmaceutically acceptable salt thereof, useful in therapy, in particular in the treatment of a viral infection.
Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility
Chen, Chen,Wilcoxen, Keith M.,Huang, Charles Q.,McCarthy, James R.,Chen, Takung,Grigoriadis, Dimitri E.
, p. 3669 - 3673 (2007/10/03)
In our efforts to identify potent CRF1 antagonists with proper physicochemical properties, a series of 3-phenylpyrazolo[1,5-a]pyrimidines bearing polar groups, such as amino, hydroxyl, methoxy, sulfoxide, were designed and synthesized. Several positions of the core structure were identified, where a polar group was tolerated with slight reduction in receptor binding. NBI 30545 (18n) was found to have good binding affinity and potent antagonistic activity at the human CRF1 receptor. Moreover, this compound had proper lipophilicity (logD=2.78) and good solubility in water (>10mg/mL), and exhibited good plasma and brain exposure when given orally.