196809-22-0Relevant academic research and scientific papers
Substituted 4-hydroxy-phenylalcanoic acid derivatives with agonist activity to PPAR-gamma
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, (2008/06/13)
A compound having formula (I), wherein A is selected from the group consisting of: (i) phenyl, wherein said phenyl is optionally substituted by one or more halogen atoms, C1-6alkyl, C1-3alkoxy, C1-3fluoroalkoxy, nitrile, or —NR7R8where R7and R8are independently hydrogen or C1-3alkyl; (ii) a 5- or 6-membered hetrocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur; and (iii) a fused bicyclic ring (a), wherein ring C represents a heterocyclic group as defined in point (ii) above, which bicyclic ring is attached to group B via a ring atom of ring C; B is selected from the group consisting of: (iv) C1-6alkylene; (v) —MC1-6alkylene or C1-6alkyleneMC1-6alkylene, wherein M is O, S, or —NR2wherein R2represents hydrogen or C1-3alkyl; (vi) a 5- or 6-membered heterocyclic group containing at least one nitrogen heteroatom and optionally at least one further heteroatom selected from oxygen, nitrogen and sulfur and optionally substituted by C1-3alkyl; and (vii) Het-C1-6alkylene, wherein Het represents a heterocyclic group as defined in point (vi) above; Alk represents C1-3alkylene; R1represents hydrogen or C1-3alkyl; Z is selected from the group consisting of: (viii) —(C1-3alkylene) phenyl, which phenyl is optionally substituted by one or more halogen atoms; and (ix) —NR3R4, wherein R3represents hydrogen or C1-3alkyl, and R4represents —Y—(C═O)—T—R5, or —Y—(CH(OH))—T—R5.
N-(2-benzoylphenyl)-L-tyrosine PPARγ agonists. 3. Structure-activity relationship and optimization of the N-aryl substituent
Cobb, Jeff E.,Blanchard, Steven G.,Boswell, Evan G.,Brown, Kathleen K.,Charifson, Paul S.,Cooper, Joel P.,Collins, Jon L.,Dezube, Milana,Henke, Brad R.,Hull-Ryde, Emily A.,Lake, Debra H.,Lenhard, James M.,Oliver Jr., William,Oplinger, Jeffery,Pentti, Mila,Parks, Derek J.,Plunket, Kelli D.,Tong, Wei-Qin
, p. 5055 - 5069 (2007/10/03)
3-{4-[2-(Benzoxazol-2-ylmethylamino)ethoxy]phenyl}-(2S)-((2- benzoylphenyl)amino)propionic acid (1) and (2S)-((2-benzoylphenyl)amino)-3- {4-[2-(5-methyl-2-phenyloxazol-4-yl)ethoxy]phenyl}propionic acid (2) are peroxisome proliferator-activated receptor γ
