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Aminoquinazolines as TRPV1 antagonists: Modulation of drug-like properties through the exploration of 2-position substitution BIOORGANIC & MEDICINAL CHEMISTRY LETTERS Blum, C. A., Zheng, X., Brielmann, H., Hodgetts, K. J., Bakthavatchalam, R., Chandrasekhar, J., Krause, J. E., Cortright, D., Matson, D., Crandall, M., Ngo, C. K., Fung, L., Day, M., Kershaw, M., De Lombaert, S., Chenard, B. L. 2008; 18 (16): 4573-4577
Abstract
A focused SAR exploration of the lead 4-aminoquinazoline TRPV1 antagonist 2 led to the discovery of compound 18. In rats, compound 18 is readily absorbed following oral dosing and demonstrates excellent in vivo potency and efficacy in an acute inflammatory pain model.
View details for DOI 10.1016/j.bmcl.2008.07.036
View details for Web of Science ID 000258769200027
View details for PubMedID 18662872