210992-28-2Relevant articles and documents
Synthesis and antitumor activity of novel pyrimidinyl pyrazole derivatives. III. Synthesis and antitumor activity of 3-phenylpiperazinyl-1-trans-propenes
Naito, Hiroyuki,Ohsuki, Satoru,Atsumi, Ryo,Minami, Megumi,Mochizuki, Mineko,Hirotani, Kenji,Kumazawa, Eiji,Ejima, Akio
, p. 153 - 163 (2007/10/03)
A series of novel 3-[4-phenyl-1-piperazinyl]-1-[5-methyl-1-(2-pyrimidinyl)- 4-pyrazolyl]-1-trans-propenes and related compounds were synthesized and evaluated by their cytotoxic activity against several tumor cell lines in vitro and in vivo antitumor acti
5-FLUORO-, CHLORO- AND CYANO-PYRIDIN-2-YL-TETRAZOLES AS LIGANDS OF THE METABOTROPIC GLUTAMATE RECEPTOR-5
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Page/Page column 22, (2008/06/13)
The present invention relates to new compounds of formula I, wherein Z, Q, X1, X2, R1 and R2, are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
3-[3-Fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine: A highly potent and orally bioavailable metabotropic glutamate subtype 5 (mGlu5) receptor antagonist
Poon, Steve F.,Eastman, Brian W.,Chapman, Deborah F.,Chung, Janice,Cramer, Merryl,Holtz, Gregory,Cosford, Nicholas D.P.,Smith, Nicholas D.
, p. 5477 - 5480 (2007/10/03)
Structure-activity relationship studies performed around 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile for the purposes of developing novel mGlu5 receptor antagonists are described. Synthesis of a series of four-ring tetrazoles led to the discovery of 3-[3-fluoro-5-(5-pyridin-2-yl- 2H-tetrazol-2-yl)phenyl]-4-methylpyridine (26), a highly potent, brain penetrant, tetrazole-based mGlu5 receptor antagonist. Structure-activity relationship studies performed around 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2- yl)benzonitrile for the purpose of developing novel mGlu5 receptor antagonists are described. Synthesis of a series of four-ring tetrazoles led to the discovery of 3-[3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4- methylpyridine, a highly potent, brain penetrant, azole-based mGlu5 receptor antagonist.