63674-47-5Relevant articles and documents
A2Badenosine receptor antagonists: Design, synthesis and biological evaluation of novel xanthine derivatives
Basu, Sujay,Barawkar, Dinesh A.,Ramdas, Vidya,Waman, Yogesh,Patel, Meena,Panmand, Anil,Kumar, Santosh,Thorat, Sachin,Bonagiri, Rajesh,Jadhav, Dilip,Mukhopadhyay, Partha,Prasad, Vandna,Reddy, B. Srinivasa,Goswami, Arnab,Chaturvedi, Sandhya,Menon, Suraj,Quraishi, Azfar,Ghosh, Indraneel,Dusange, Sushant,Paliwal, Shalini,Kulkarni, Abhay,Karande, Vikas,Thakre, Rhishikesh,Bedse, Gaurav,Rouduri, Sreekanth,Gundu, Jayasagar,Palle, Venkata P.,Chugh, Anita,Mookhtiar, Kasim A.
supporting information, p. 986 - 996 (2017/02/12)
A2BAdoR is a low affinity adenosine receptor that functions by Gs mediated elevation of cAMP and subsequent downstream signaling. The receptor has been implicated in lung inflammatory disorders like?COPD and asthma. Several potent and selective
N-Aryl pyrrolidinonyl oxadiazoles as potent mGluR5 positive allosteric modulators
Packiarajan, Mathivanan,Mazza Ferreira, Christine G.,Hong, Sang-Phyo,White, Andrew D.,Chandrasena, Gamini,Pu, Xiaosui,Brodbeck, Robbin M.,Robichaud, Albert J.
scheme or table, p. 5658 - 5662 (2012/09/22)
A novel series of N-aryl pyrrolidinonyl oxadiazoles were identified as mGluR5 positive allosteric modulators (PAMs). Optimization of the initial lead compound 6a led to the identification of the 12c (-) enantiomer as a potent compound with acceptable in vitro clearance, CYP, hERG and PK properties. Para substituted N-aryl pyrrolidinonyl oxadiazoles are mGluR5 PAMs while the meta and ortho substituted N-aryl pyrrolidinonyl oxadiazoles are negative allosteric modulators (NAMs). Para fluoro substitution on the N-aryl group and meta chloro or methyl substituents on the aryl oxadiazole moiety are optimal for mGluR5 PAM efficacy. The existence of an exquisitely sensitive 'PAM to NAM switch' within this chemotype making it challenging for simultaneous optimization of potency and drug-like properties.
