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 pyrazolo-pyrimidine carboxamide derivatives were designed synthesized and evaluated for their in vitro potencies towards muscarinic receptors. Most of the compounds showed potent in vitro potency and found to be selective towards M1 receptor sub type. The selected compounds were further evaluated in pharmacokinetic studies to assess their bioavailability; exposures in plasma and brain. Details of design, chemistry, structure activity relationship, in vitro potencies, pharmacokinetic evaluation and in vivo efficacy of pyrazolo-pyrimidine carboxamides will be discussed in this poster presentation.

Novel pyrazolo-pyrimidine carboxamides as muscarinic 1 positive allosteric modulators (M1 PAM) for the potential treatment of Alzheimer’s disease

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.