Submission Details

EDJ-MED-edeb0d3a
Molecule(s):
COc1ccc(Cl)cc1OCCN(C)C(=O)c1cc(=O)[nH]c2ccccc12

EDJ-MED-edeb0d3a-1
Duplicate of:
BEN-DND-b89db3f2-5

COc1ccc(Cl)cc1OCCN(C)C(=O)c1cc(=O)[nH]c2ccccc12

Duplicate quinolones Check Availability on Manifold View
COc1ccc(Cl)cc1OCCNC(=O)c1cc(=O)[nH]c2cccc(OC)c12

EDJ-MED-edeb0d3a-2
Duplicate of:
MAT-POS-3b536971-1

COc1ccc(Cl)cc1OCCNC(=O)c1cc(=O)[nH]c2cccc(OC)c12

Duplicate quinolones Assayed Check Availability on Manifold View
COc1ccc(Cl)cc1OCCN(C)C(=O)c1cc(=O)[nH]c2cccc(OC)c12

EDJ-MED-edeb0d3a-3

COc1ccc(Cl)cc1OCCN(C)C(=O)c1cc(=O)[nH]c2cccc(OC)c12

Design Rationale:

Improve ALP-POS-05819dc4, 400nM permeability and potency. 5 position OMe adds ~ 3 fold potency, Me on chain amide to improve permeability. Makes matched square of compounds.

Inspired By:
Discussion:

Contributor: Ed J Griffen, MedChemica Ltd - Tue, 08 Dec 2020 11:44:29 +0000