Submission Details

RAL-THA-5e0a6f1a
Molecule(s):
CN(C)C(=O)CN1CC(C(=O)Nc2cncc3ccccc23)c2cc(Cl)ccc2C1=O

RAL-THA-5e0a6f1a-1

CN(C)C(=O)CN1CC(C(=O)Nc2cncc3ccccc23)c2cc(Cl)ccc2C1=O

3-aminopyridine-like Assayed Check Availability on Manifold View
Design Rationale:

The corresponding compound without the lactam carbonyl loses significant potency with the introduction of a tertiary amide. This compound will test whether or not that SAR translates to the lactam series, which generally enjoys greater metabolic stability. Removal of an H-bond donor and a slight increase in logP are expected to improve permeability.

Discussion:

Contributor: Ralph Robinson, Thames Pharma Partners LLC - Thu, 26 Aug 2021 15:31:33 +0000