Positive allosteric modulation (PAM) of the muscarinic acetylcholine receptor subtype 1 (M1) has drawn the attention of the researchers across the world as novel therapeutic approach for the treatment of cognitive deficits associated with Alzheimer’s disease (AD). Moreover, selective M1 PAMs also showed disease modifying potential, in addition to symptomatic cognition enhancing properties. A series of pyrimidine carboxamide derivatives were designed synthesized and evaluated for their in-vitro potencies towards muscarinic receptors. Most of the compounds showed potent in vitro potencies towards M1 receptor and found to be selective against other sub types M2 to M5. The selected compounds were further evaluated in pharmacokinetic studies to assess their exposures in plasma and brain. Details of design, chemistry, structure activity relationship, in vitro potencies and pharmacokinetic studies of pyrimidine carboxamide derivatives will be disclosed in this poster presentation.

Pyrimidine carboxamide derivatives as muscarinic acetylcholine subtype 1 positive allosteric modulators (M1 PAM) for the treatment of cognitive deficits in Alzheimer’s disease

254th National Meeting (2017)

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