61006-27-7Relevant academic research and scientific papers
Synthesis and pharmacological activity of N-(2,2-dimethyl-3,4-dihydro-2H-1- benzopyran-4-yl)-4H-1,2,4-benzothiadiazine-3-carboxamides 1,1-dioxides on rat uterus, rat aorta and rat pancreatic β-cells
Khelili, Smail,Kihal, Nadjib,Yekhlef, Mohamed,De Tullio, Pascal,Lebrun, Philippe,Pirotte, Bernard
scheme or table, p. 873 - 878 (2012/09/10)
N-(2,2-Dimethyl-3,4-dihydro-2H-1-benzopyran-4-yl)-4H-1,2, 4-benzothiadiazine-3-carboxamides 1,1-dioxides were prepared and evaluated on rat uterus, rat aortic rings and rat pancreatic β-cells. Pharmacological studies conducted on rat uterus indicated that several of these original hybrid compounds displayed a strong myorelaxant activity. The most active compounds hold a bromine atom at the 6-position of the dihydrobenzopyran ring. Moreover, the compounds failed to display a marked inhibitory effect on insulin secretion and vascular myogenic activity. These features suggest that the 6-bromo compounds could be relatively selective towards the uterine smooth muscle.
Design, synthesis, and SAR of cis-1,2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part II: Exploration of 6-6 fused rings as alternative S1 moieties
Yoshikawa, Kenji,Kobayashi, Shozo,Nakamoto, Yumi,Haginoya, Noriyasu,Komoriya, Satoshi,Yoshino, Toshiharu,Nagata, Tsutomu,Mochizuki, Akiyoshi,Watanabe, Kengo,Suzuki, Makoto,Kanno, Hideyuki,Ohta, Toshiharu
experimental part, p. 8221 - 8233 (2010/03/25)
A series of cis-1,2-diaminocyclohexane derivatives possessing a 6-6 fused ring for the S1 moiety were synthesized as novel factor Xa (fXa) inhibitors. The synthesis, structure-activity relationship (SAR), and physicochemical properties are reported herein, together with the discovery of compound 45c, which has potent anti-fXa activity, good physicochemical properties and pharmacokinetic (PK) profiles, including a reduced negative food effect.
