178114-22-2Relevant academic research and scientific papers
AMINOPYRAZINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES
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, (2016/12/26)
Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof, wherein: "Z", R1 and R2 are defined herein, which compounds are believed suitable for use in selectively antagonizing th
Benzodiazepine binding activity of some tricyclic heteroatomic systems to define the hydrogen bonding strength of the proton donors of the receptor site
Colotta,Catarzi,Varano,Melani,Filacchioni,Cecchi,Galli,Costagli
, p. 223 - 229 (2007/10/03)
Comparison of the benzodiazepine receptor affinities of some known and newly synthesized tricyclic derivatives of similar size and shape, and bearing the same pharmacophoric descriptors allowed us to suggest the different hydrogen bonding power of the proton donors of the benzodiazepine receptor recognition site. In particular, we propose, according to a previous model, that the lack of the a1 acceptor, which corresponds to a weak hydrogen donor of the receptor site, is not crucial for receptor-ligand interaction but, like the hydrogen donor d, only affects the potency. On the contrary, the presence of a proton acceptor atom in the a2 area is essential for the anchoring of our tricyclic derivatives to the benzodiazepine receptor recognition site.
