4846-84-8Relevant articles and documents
Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARδ-selective agonists
Fujieda, Hiroki,Usui, Shinya,Suzuki, Takayoshi,Nakagawa, Hidehiko,Ogura, Michitaka,Makishima, Makoto,Miyata, Naoki
, p. 4351 - 4357 (2008/02/12)
To find novel PPARδ-selective agonists, we designed and synthesized phenylpropanoic acid derivatives bearing 6-substituted benzothiazoles. Optimization of this series led to the identification of a potent and selective PPARδ agonist 17. Molecular modeling suggested that compound 17 occupies the Y-shaped pocket of PPARδ appropriately.
Comparison of phosphonate transition state analogs for inducing catalytic antibodies and evaluation of key structural factors by an ab initio study
Kakinuma, Hiroyuki,Shimazaki, Kazuko,Takahashi, Naoko,Takahashi, Kyoko,Niihata, Shigeo,Aoki, Yoshiko,Hamada, Katsumi,Matsushita, Hajime,Nishi, Yoshisuke
, p. 2559 - 2572 (2007/10/03)
The relation between the structure of haptens and the esterolytic activities of antibodies was investigated. We synthesized two phenylalanine analogs, the negatively charged phosphonate derivative 1 and the neutral phosphonamidate derivative 2. Seventeen out of 41 monoclonal antibodies generated against the hapten 1 hydrolyzed the relevant phenylalanine ester R- 12. On the contrary, none of 27 monoclonal antibodies generated against the hapten 2 had catalytic activity. An ab initio study of the structural and electronic properties of the modeled haptens showed that the value of the negative electrostatic potential around the phosphonyl oxygen was an important factor affecting the induction of esterolytic antibodies.
