Design, synthesis, and biological activity of novel factor Xa inhibitors: Improving metabolic stability by S1 and S4 ligand modification was written by Komoriya, Satoshi;Kobayashi, Shozo;Osanai, Ken;Yoshino, Toshiharu;Nagata, Tsutomu;Haginoya, Noriyasu;Nakamoto, Yumi;Mochizuki, Akiyoshi;Nagahara, Takayasu;Suzuki, Makoto;Shimada, Takashi;Watanabe, Kengo;Isobe, Yumiko;Furugoori, Taketoshi. And the article was included in Bioorganic & Medicinal Chemistry in 2006.Category: piperazines The following contents are mentioned in the article:
Serine protease factor Xa (fXa) inhibitor I showed good ex vivo anti-fXa activity upon oral administration in rats. However, it has been revealed that I had low metabolic stability against human liver microsomes. To improve the metabolic stability, we attempted to modify the S1 and S4 ligands of I. These modifications resulted in a compound which exhibited selective anti-fXa activity and excellent anti-coagulation activity. This study involved multiple reactions and reactants, such as Methyl 2-(1,4-dibenzylpiperazin-2-yl)acetate (cas: 183742-32-7Category: piperazines).
Methyl 2-(1,4-dibenzylpiperazin-2-yl)acetate (cas: 183742-32-7) belongs to piperazine derivatives. Piperazine belongs to the family of medicines called anthelmintics. Although many piperazine derivatives occur naturally, piperazine itself can be synthesized by reacting alcoholic ammonia with 1,2-dichloroethane, by the action of sodium and ethylene glycol on ethylene diamine hydrochloride, or by reduction of pyrazine with sodium in ethanol.Category: piperazines
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics