Related Experiment Video
Updated: Jul 20, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
N',2-diphenylquinoline-4-carbohydrazide based NK3 receptor antagonists II
Jason M Elliott1, Robert W Carling, Gary G Chicchi
1Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK. jason@elliottj25.fsnet.co.uk
Abstract:
Introduction of selected amine containing side chains into the 3-position of N',2-diphenylquinoline-4-carbohydrazide based NK3 antagonists abolishes unwanted hPXR activation. Introduction of a fluorine at the 8-position is necessary to minimize unwanted hI(Kr) affinity and a piperazine N-tert-butyl group is necessary for metabolic stability. The lead compound (8m) occupies receptors within the CNS following oral dosing (Occ(90) 7 mg/kg po; plasma Occ(90) 0.4 microM) and has good selectivity and excellent PK properties.
More Related Videos
14:11Synthesis of pH Dependent Pyrazole, Imidazole, and Isoindolone Dipyrrinone Fluorophores using a Claisen-Schmidt Condensation Approach
Published on: June 10, 2021
09:39Drug-induced Sensitization of Adenylyl Cyclase: Assay Streamlining and Miniaturization for Small Molecule and siRNA Screening Applications
Published on: January 27, 2014
Related Concept Videos
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists
Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists
Phenothiazines, such as prochlorperazine...
Cholinergic Antagonists: Chemistry and Structure-Activity Relationship
Cholinergic Antagonists: Pharmacokinetics
Indirect-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship
Reversible inhibitors display short to medium durations of action. Short-acting agents include simple alcohols with...
Chemotherapy-Induced Nausea and Vomiting: 5-HT3 Receptor Antagonists