Synthesis and evaluation of 4-alkoxy-[1′-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4′-piperidine)] analogues as histamine-3 receptor antagonists
-
Add time:09/24/2019 Source:sciencedirect.com
A novel class of 4-alkoxy-[1′-cyclobutyl-spiro(3,4-dihydrobenzopyran-2,4′-piperidine)] analogues were designed and synthesized as H3R antagonists. Structure–activity relationship identified sulfone 27 with excellent H3R affinities in both humans and rats, and acceptable pharmacokinetic properties. Further, compound 28 achieved single digit nanomolar H3R affinities in both species with minimum hERG activity.
We also recommend Trading Suppliers and Manufacturers of Cyclobutyl chloride (cas 1120-57-6). Pls Click Website Link as below: cas 1120-57-6 suppliers
Prev:Cyclobutyl phenyl sulfoxide and (SR)-cyclobutyl p-tolyl sulfoxide: New reagents for the spiroannelation of cyclopentanone
Next:Stereoselective synthesis of cyclobutyl γ-amino acids leading to branched peptides with a cyclobutane core) - 【Back】【Close 】【Print】【Add to favorite 】
- Related Information
- Synthesis and biological evaluation of anti-1-amino-2-[18F]fluoro-cyclobutyl-1-carboxylic acid (anti-2-[18F]FACBC) in rat 9L gliosarcoma09/30/2019
- Highly stereoselective syntheses of alkenylsilanes and germanes utilizing cyclobutyl ketones09/29/2019
- Synthesis and evaluation of a new series of 1′-cyclobutyl-6-(4-piperidyloxy)spiro[benzopyran-2,4′-piperidine] derivatives as high affinity and selective histamine-3 receptor (H3R) antagonists09/28/2019
- Enantiodivergent synthesis of cyclobutyl-(Z)-α,β-dehydro-α-amino acid derivatives from (−)-cis-pinononic acid10/01/2019
- Cyanuric chloride–dimethylformamide mediated cleavage of cyclopropylcarbinols-synthesis of phenolic antioxidant and construction of a new vinylcyclopropane skeleton09/27/2019
- Cyclobutyl neighboring group effect on the stability of bicyclo-[2.2.2]octyl bridgehead carbenium ions☆09/26/2019
- Stereoselective synthesis of cyclobutyl γ-amino acids leading to branched peptides with a cyclobutane core09/25/2019
- Cyclobutyl phenyl sulfoxide and (SR)-cyclobutyl p-tolyl sulfoxide: New reagents for the spiroannelation of cyclopentanone09/10/2019
- Antitumor platinum(II) complexes of N-cyclobutyl-1R,2R-diaminocyclohexane with dicarboxylates as leaving groups09/09/2019
