50289-13-9Relevant academic research and scientific papers
Anesthetic compounds and related methods of use
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Page/Page column 69, (2015/11/09)
Provided herein are compounds according to formula (I): Provided herein is also a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and a method for providing anesthesia in a subject by administering such a pharmaceutical composition.
Bradykinin B1 receptor antagonists: An α-hydroxy amide with an improved metabolism profile
Kuduk, Scott D.,Chang, Ronald K.,DiPardo, Robert M.,Di Marco, Christina N.,Murphy, Kathy L.,Ransom, Richard W.,Reiss, Duane R.,Tang, Cuyue,Prueksaritanont, Thomayant,Pettibone, Douglas J.,Bock, Mark G.
scheme or table, p. 5107 - 5110 (2009/05/26)
A series of carbo- and heterocyclic α-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl α-hydroxy amide was incorporated along with a 2-methyl tetrazole in lieu of an oxadiazole to afford a suitable compound with good pharmacokinetic properties, CNS penetration, and clearance by multiple metabolic pathways.
Oxazolones as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1
Sutin, Lori,Andersson, Soeren,Bergquist, Lars,Castro, Victor M.,Danielsson, Eva,James, Stephen,Henriksson, Martin,Johansson, Lars,Kaiser, Christina,Flyren, Katarina,Williams, Meredith
, p. 4837 - 4840 (2008/02/11)
2,5,5-Trisubstituted oxazolones were identified as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The synthesis, structure-activity relationship and metabolic stability of these compounds are presented.
Inhibitors of leukotriene B4. Synthesis and SAR of new β-enaminoester open-chain analogues of Zeneca ZD2138
Bird,Olivier
, p. 515 - 520 (2007/10/03)
A series of methoxy tetrahydropyranyl β-enaminoester has been discovered as inhibitors of LTB4 production. These are unusual open chain analogues of Zeneca ZD2138, the highly potent orally active 5-LO inhibitor under development for the treatment of asthma and rheumatoid arthritis. In vitro, compound 1a inhibited LTB4 formation in human whole blood with an IC50 of 0.04 μM. In inflamed exudate in the rat 1a inhibited formation of LTB4 with an oral ED50 3h after dosing of 3.0 mg/kg.
