Structure-activity studies of a novel series of 5,6-fused heteroaromatic ureas as TRPV1 antagonists.
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Summary
It was found that 4-aminoindoles and indazoles are the preferential cores for the attachment of ureas and Bulky electron-withdrawing groups in the para-position of the aromatic ring of the urea substituents imparted the best in vitro potency at TRPV1.
- Type
- article
- Published
- 2006-07-15
- Cited by
- 25
- References
- 16
- OpenAlex
- https://openalex.org/W16621571
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:41754275
Keywords
Geography
References
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Cited by
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- In silico research to assist the investigation of carboxamide derivatives as potent TRPV1 antagonists.
- Acid Solution Is a Suitable Medium for Introducing QX-314 into Nociceptors through TRPV1 Channels to Produce Sensory-Specific Analgesic Effects
- ThermoTRP Channels in Nociceptors: Taking a Lead from Capsaicin Receptor TRPV1
- Thermoregulatory Phenotype of the Trpv1 Knockout Mouse: Thermoeffector Dysbalance with Hyperkinesis
- Investigation of TRPV1 loss-of-function phenotypes in transgenic shRNA expressing and knockout mice.
- Effects of the transient receptor potential vanilloid 1 antagonist A-425619 on body temperature and thermoregulation in the rat.
- Molecular Mechanisms Underlying the Analgesic Property of Intrathecal Dexmedetomidine and Its Neurotoxicity Evaluation: An In Vivo and In Vitro Experimental Study
- Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists.
- 13C and 15N NMR spectra of aminobenzimidazoles in solution and in the solid state
- Spiro-piperidine azetidinones as potent TRPV1 antagonists.
- QSAR Approach to Correlate TRPV1 Antagonist Activity for a Series of Heteroaromatic Urea
- Advances in the development of novel analgesics
- Hemodynamic effects of potent and selective JNK inhibitors in anesthetized rats: implication for targeting protein kinases in metabolic diseases.
- Discovery of TRPV1 antagonist ABT-116.
- Indazole: a medicinally important heterocyclic moiety
- Identification of (R)-1-(5-tert-butyl-2,3-dihydro-1H-inden-1-yl)-3-(1H-indazol-4-yl)urea (ABT-102) as a potent TRPV1 antagonist for pain management.
- Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
- A structural view of ligand-dependent activation in thermoTRP channels
- Coapplication of Lidocaine and Membrane-Impermeable Lidocaine Derivative QX-222 Produces Divergent Effects on Evoked and Spontaneous Nociceptive Behaviors in Mice
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