Aminoquinazolines as TRPV1 antagonists: Modulation of drug-like properties through the exploration of 2-position substitution
Graphical abstract
Section snippets
Acknowledgments
The authors gratefully acknowledge the electrophysiology work of John Dessaint and Gina Borrelli. The authors also thank Lauren Danner (cell culture) and Du-Shieng Chien (pharmacokinetics).
References and notes (15)
- et al.
Bioorg. Med. Chem. Lett.
(2006)(b)Zheng, X.; Blum, C. A.; Hodgetts, K. J.; Brielmann, H.; Hutchison, A.; Chenard, B. L.; Burkamp, F.; Jones, A. B.;... - (a)DeSimone, R. W.; Hodgetts, K.; Krause, J. E.; White, G. PCT WO...(b)Bakthavatchalam, R.; Hutchison, A.; DeSimone, R. W.; Hodgetts, K.; Krause, J. E.; White, G. U.S. Patent 6,723,730,...
- et al.
J. Med. Chem.
(2005)
There are more references available in the full text version of this article.
Cited by (18)
1,2-Diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d] azepines as TRPV1 antagonists with improved properties
2010, Bioorganic and Medicinal Chemistry LettersPyrido[2,3-b]pyrazines, discovery of TRPV1 antagonists with reduced potential for the formation of reactive metabolites
2010, Bioorganic and Medicinal Chemistry LettersThe T1R2/T1R3 sweet receptor and TRPM5 ion channel: Taste targets with therapeutic potential
2010, Progress in Molecular Biology and Translational ScienceCitation Excerpt :However, the basic principles of our approach can be exemplified by using a related target, the TRPV1 ion channel. Figure 11 lists a panel of 17 TRPV1 ligands.204–208 Thirteen are the results of pharmaceutical research while the remaining six are natural products (capsacin analogs) responsible for the burning sensation associated with the pepper plant (genus Capsicum).
Analgesic potential of TRPV1 antagonists
2009, Biochemical PharmacologySpiro-piperidine azetidinones as potent TRPV1 antagonists
2009, Bioorganic and Medicinal Chemistry LettersA Highly Efficient Copper-Catalyzed Three-Component Synthesis of 4-Aminoquinazolines
2017, Synthesis (Germany)
- †
Present address: Boehringer Ingelheim Pharmaceuticals Inc., Ridgefield, CT, USA.
Copyright © 2008 Elsevier Ltd. All rights reserved.