Author: "Li, Lina" / Journal: bioorganic & medicinal chemistry letters / Topic: oxazoles - Searchworks@Jio Institute Digital Library Search Results

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Start Over Author "Li, Lina" Topic oxazoles Journal bioorganic & medicinal chemistry letters

Author: Pippel, Marna, Allison, Brett D., Phuong, Victor K., Li, Lina, Morton, Magda F., Prendergast, Clodagh, Wu, Xiaodong, Shankley, Nigel P., and Rabinowitz, Michael H.
Subjects: *SULFONAMIDES, *OXAZOLES, *DRUG development, *CHOLECYSTOKININ, *BENZAMIDE, *HORMONE antagonists, *THERAPEUTICS
Abstract: Abstract: A series of CCK2R-selective anthranilic amides is shown to derive CCK1R affinity via selective substitution of the amide side chain. Thus, extending the length of the original benzamide side chain by a single methylene unit imparts CCK1R affinity to the series, and further fine tuning of the affinity results in CCK1R selectivity of greater than 100-fold. [Copyright &y& Elsevier]
Published: 2009
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Author: Pippel, Marna, Boyce, Kristen, Venkatesan, Hariharan, Phuong, Victor K., Yan, Wen, Barrett, Terrance D., Lagaud, Guy, Li, Lina, Morton, Magda F., Prendergast, Clodagh, Wu, Xiaodong, Shankley, Nigel P., and Rabinowitz, Michael H.
Subjects: *SULFONAMIDES, *CHOLECYSTOKININ, *HORMONE antagonists, *OXAZOLES, *PHARMACOKINETICS, *LABORATORY rats, *GASTRIC acid, *AMYLASES, *DRUG efficacy, *THERAPEUTICS
Abstract: Abstract: In the previous article we demonstrated how certain CCK2R-selective anthranilic amides could be structurally modified to afford high-affinity, selective CCK1R activity. We now describe our efforts at modulating and optimizing the CCK1R and CCK2R affinities aimed at producing compounds with good pharmacokinetics properties and in vivo efficacy in rat models of gastric acid and pancreatic amylase secretion. [Copyright &y& Elsevier]
Published: 2009
Full Text: View/download PDF

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