Bioorganic and Medicinal Chemistry Letters p. 4146 - 4149 (2011)
Update date:2022-08-05
Topics: Purification Structure-Activity Relationship (SAR) Analysis Chemical Synthesis In vitro Testing Clinical Trials In Vivo Testing Lead Optimization Regulatory Approval Design and Synthesis Pharmacokinetic and Toxicity Studies
Wang, Haixia
Robl, Jeffrey A.
Hamann, Lawrence G.
Simpkins, Ligaya
Golla, Rajasree
Li, Yi-Xin
Seethala, Ramakrishna
Zvyaga, Tatyana
Gordon, David A.
Li, James J.
A series of pyridyl amide/sulfonamide inhibitors of 11β-HSD-1 were modified to incorporate a novel 1,2,4-triazolopyridine scaffold. Optimization of substituents at the 3 and 8 position of the TZP core, with a special focus on enhancing metabolic stability, resulted in the identification of compound 38 as a potent and metabolically stable inhibitor of the enzyme.
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Doi:10.1016/S0040-4039(00)71225-1
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