piperidines has been researched along with purine* in 3 studies
3 other study(ies) available for piperidines and purine
| Article | Year |
|---|---|
Peripherally selective diphenyl purine antagonist of the CB1 receptor.
Antagonists of the CB1 receptor can be useful in the treatment of several important disorders. However, to date, the only clinically approved CB1 receptor antagonist, rimonabant, was withdrawn because of adverse central nervous system (CNS)-related side effects. Since rimonabant's withdrawal, several groups are pursuing peripherally selective CB1 antagonists. These compounds are expected to be devoid of undesirable CNS-related effects but maintain efficacy through antagonism of peripherally expressed CB1 receptors. Reported here are our latest results toward the development of a peripherally selective analog of the diphenyl purine CB1 antagonist otenabant 1. Compound 9 (N-{1-[8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl]piperidin-4-yl}pentanamide) is a potent, orally absorbed antagonist of the CB1 receptor that is >50-fold selective for CB1 over CB2, highly selective for the periphery in a rodent model, and without efficacy in a series of in vivo assays designed to evaluate its ability to mitigate the central effects of Δ(9)-tetrahydrocannabinol through the CB1 receptor. Topics: Animals; Area Under Curve; Binding, Competitive; Biphenyl Compounds; Body Temperature; Male; Mice; Mice, Inbred ICR; Molecular Structure; Motor Activity; Piperidines; Purines; Rats; Rats, Sprague-Dawley; Receptor, Cannabinoid, CB1; Receptor, Cannabinoid, CB2 | 2013 |
Design and synthesis of N-benzylpiperidine-purine derivatives as new dual inhibitors of acetyl- and butyrylcholinesterase.
The synthesis and biological evaluation of N-benzyl-(piperidin or pyrrolidin)-purines are described. Compounds derived from N-benzylpiperidine and N-substituted purines showed moderate acetylcholinesterase inhibition. Preliminary structure-activity relationships and a superimposition of the best compound with the active conformation of donepezil have revealed structural features that have been used in the design of more potent N-benzylpiperidine inhibitors bearing an 8-substituted caffeine fragment and a methoxymethyl linker. These new compounds are interesting dual inhibitors of acetylcholinesterase and butyrylcholinesterase and have been chosen for further optimisation. Topics: Acetylcholinesterase; Animals; Butyrylcholinesterase; Cattle; Cholinesterase Inhibitors; Drug Design; Horses; Molecular Structure; Piperidines; Purines; Structure-Activity Relationship | 2005 |
SOME 2-SUBSTITUTED AMINOPURINES AND PURINE ANALOGS.
Topics: 2-Aminopurine; Animals; Antineoplastic Agents; Chemistry, Pharmaceutical; Leukemia; Leukemia, Experimental; Morpholines; Pharmacology; Piperidines; Purines; Pyrimidines; Pyrroles; Research; Sarcoma 180 | 1963 |