36361-64-5Relevant academic research and scientific papers
Synthesis and spectral properties of 2-methyl-5-aryl-1,3,4-oxadiazoles
Popova,Krasovitskii,Pivnenko,Surov
, p. 712 - 717 (1997)
By heterocyclization of 1-acyl-2-aroylhydrazines under the influence of strong dehydrating substances, a series of 2-methyl-5-aryl-1,3,4-oxadiazoles has been synthesized and their UV, IR, and PMR spectra have been investigated. Through analysis of data on
Synthesis and biological evaluation of 3-biphenyl-4-yl-4-phenyl-4 h -1,2,4-triazoles as novel glycine transporter 1 inhibitors
Sugane, Takashi,Tobe, Takahiko,Hamaguchi, Wataru,Shimada, Itsuro,Maeno, Kyoichi,Miyata, Junji,Suzuki, Takeshi,Kimizuka, Tetsuya,Kohara, Atsuyuki,Morita, Takuma,Doihara, Hitoshi,Saita, Kyouko,Aota, Masaki,Furutani, Masako,Shimada, Yoshiaki,Hamada, Noritaka,Sakamoto, Shuichi,Tsukamoto, Shin-Ichi
supporting information; experimental part, p. 387 - 391 (2011/03/18)
We describe the preparation and evaluation of a novel series of glycine transporter 1 (GlyT1) inhibitors derived from a high-throughput screening hit. The SAR studies resulted in the discovery of 3-biphenyl-4-yl-4-(2-fluorophenyl)- 5-isopropyl-4H-1,2,4-tr
Discovery of 4,5-diphenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human V(1A) receptor.
Kakefuda, Akio,Suzuki, Takeshi,Tobe, Takahiko,Tahara, Atsuo,Sakamoto, Shuichi,Tsukamoto, Shin ichi
, p. 1905 - 1912 (2007/10/03)
In the search for a novel class of selective antagonists for the human V(1A) receptor, high-throughput screening (HTS) of the Yamanouchi chemical library using CHO cells expressing the cloned human V(1A) (hV(1A)) receptor led to the discovery of 5-(4-biphenyl)-4-(2-methoxyphenyl)-3-methyl-1,2,4-triazole (3) which possessed the novel 4,5-diphenyl-1,2,4-triazole structure. Subsequent structure-activity relationships studies on a series of the 4,5-diphenyl-1,2,4-triazole derivatives related to 3 revealed that the 4,5-diphenyl-1,2,4-triazole structure played an essential role in exerting high affinity for the hV(1A) receptor and that introduction of a basic amine moiety to the methoxy part of the 4-phenyl ring was effective in the improvement of both affinity for the hV(1A) receptor and selectivity versus the hV(2) receptor. Compound 3 and the 2-(morphorino)ethoxy derivative (11b) were shown to be antagonists for the hV(1A) receptor, from their effects on AVP-induced [Ca(2+)](i) response in CHO cells expressing the hV(1A) receptor.
