Synthesis and benzodiazepine binding activity of a series of novel [1, 2, 4] triazolo [1, 5-c] quinazolin-5 (6H)-ones

…, BS Barbaz, PS Bernard, RA Lovell…

Index: Francis, John E.; Cash, William D.; Barbaz, Beverly S.; Bernard, Patrick S.; Lovell, Richard A.; et al. Journal of Medicinal Chemistry, 1991 , vol. 34, # 1 p. 281 - 290

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Citation Number: 63

Abstract

Investigation of tricyclic heterocycles related to the 2-arylpyrazolo [4, 3-c] quinolin-3 (5H)- ones, structures with high affiiity for the benzodiazepine (BZ) receptor, led to the synthesis of 2-phenyl-[1, 2, 4] triazolo [1, 5-c] quinazolin-5 (6H)-one, a compound with 4 nM binding affinity to the BZ receptor. Analogues were prepared to assess the importance of the 2- substituent and ring substitution in modifying activity. Several novel synthetic routes were ...