Apelt, J.; Grassmann, S.; Ligneau, X.; Pertz, H. H.; Ganellin, C. R.; Arrang, J.-M.; Schwartz, J.-C.; Schunack, W.; Stark, H. published the artcile< Search for histamine H3 receptor antagonists with combined inhibitory potency at Nτ-methyltransferase: ether derivatives>, Product Details of C11H16O2, the main research area is histamine receptor antagonist methyltransferase inhibitor aryl piperidinopropyl ether preparation.
Several compounds containing an ether moiety derived from 4-(3-piperidinopropoxy)phenylaminoquinoline derivatives, such as FUB 836, were synthesized and tested for their affinity at cloned human histamine H3 (hH3) receptors and on the inhibition of rat histamine Nτ-methyltransferase (HMT). Besides different heterocycles, e.g. nitro- or amino-substituted pyridines, quinolines, benzothiazole or pyrroline, three classes of compounds were produced: heteroaromatic 3-piperidinopropyl ethers, keto- or imino-substituted 4-(3-piperidinopropyl)phenyl ethers and 4-(3-piperidinopropyl)phenyl ethers with substituted (alkyl)aminopyridines. Whereas the (3-piperidinopropoxy)heterocycles showed only moderate activities on both test models, the 4-(3-piperidinopropoxy)phenyl derivatives were identified as potent histamine H3 receptor ligands and/or HMT inhibitors. Ki values ≤ 0.42 nM were found for the affinity to the hH3 receptor. HMT inhibitory potency was identified with IC50 values about 0.3 μM for the most potent compounds in this series. Comparison of the pyridine-containing derivatives to recently published quinoline analogs showed a decrease in potencies for the pyridines. The dual activity, H3 receptor affinity and HMT inhibition, was moderate to good. For all compounds affinities at hH3 receptors were higher than their inhibitory HMT potencies.
Pharmazie published new progress about Histamine H3 receptor antagonists. 52244-70-9 belongs to class ethers-buliding-blocks, and the molecular formula is C11H16O2, Product Details of C11H16O2.
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Ether – Wikipedia,
Ether | (C2H5)2O – PubChem