179089-84-0Relevant articles and documents
Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists
Peng, Hairuo,Kumaravel, Gnanasambandam,Yao, Gang,Sha, Li,Wang, Joy,Van Vlijmen, Herman,Bohnert, Tonika,Huang, Carol,Vu, Chi B.,Ensinger, Carol L.,Chang, Hexi,Engber, Thomas M.,Whalley, Eric T.,Petter, Russell C.
, p. 6218 - 6229 (2004)
A series of bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines was synthesized. Some of these analogues show high affinity and excellent selectivity for adenosine A2a receptor versus the adenosine A1 receptor. Structure-activity-relationship (SAR) studies based on octahydropyrrolo[1,2-a]pyrazine and octahydropyrido[1,2-a]pyrazine with various capping groups are reported. Among these analogues, the most potent and selective A2a antagonist 26h has a Ki value of 0.2 nM and is 16 500-fold selective with respect to the A1 receptor. Among a number of compounds tested, compounds 21a and 21c exhibited significantly improved metabolic stability. Compounds 21a, 21c, and 18a showed good oral efficacy in rodent catalepsy models of Parkinson's disease.
A2A ADENOSINE RECEPTOR ANTAGONISTS
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Page 27, (2008/06/13)
The invention is based on the discovery that compounds of formula (I) possess unexpectedly high affinity for the A2a adenosine receptor, and can be useful as antagonists thereof for preventing and/or treating numerous diseases, including Parkin
Synthesis, SAR and pharmacology of CP-293,019: A potent, selective dopamine D4 receptor antagonist
Sanner, Mark A.,Chappie, Thomas A.,Dunaiskis, Audrey R.,Fliri, Anton F.,Desai, Kishor A.,Zorn, Stevin H.,Jackson, Elisa R.,Johnson, Celeste G.,Morrone, Jean M.,Seymour, Patricia A.,Majchrzak, Mark J.,Faraci, W. Stephen,Collins, Judith L.,Duignan, David B.,Di Prete, Cecilia C.,Lee, Jae S.,Trozzi, Angela
, p. 725 - 730 (2007/10/03)
A series of novel, potent and selective pyrido[1,2-a]pyrazine dopamine D4 receptor antagonists are reported including CP-293,019 (D4 K(i) = 3.4 nM, D2 K(i) > 3,310 nM), which also inhibits apomorphine-induced hyperlocomotion in rats after oral dosing.
