2-Aminomethyl piperidines as novel urotensin-II receptor antagonists

Jin, Jian; Wang, Yonghui; Wang, Feng; Shi, Dongchuan; Erhard, Karl F.; Wu, Zining; Guida, Brian; Lawrence, Sarah K.; Behm, David J.; Disa, Jyoti; Vaidya, Kalindi; Evans, Christopher A.; McMillan, Lynette J.; Rivero, Ralph A.; Neeb, Michael J.; Douglas, Stephen A.

doi:10.1016/j.bmcl.2008.03.078

Cited by 14 publications

(1 citation statement)

References 25 publications

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“…Other 2-aminomethyl piperidine derivatives had moderate hUT binding affinity ( K i = 400 nM) and hUT functional activity (FLIPR IC 50 = 600 nM) [75]. However, these series were correlated to problems such as cytochrome P450 inhibition and low oral bioavailability.…”

Section: Nonpeptide Ligandsmentioning

confidence: 99%

Urotensin-II Ligands: An Overview from Peptide to Nonpeptide Structures

Merlino

Maro

Yousif

et al. 2013

Journal of Amino Acids

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Urotensin-II was originally isolated from the goby urophysis in the 1960s as a vasoactive peptide with a prominent role in cardiovascular homeostasis. The identification of human isoform of urotensin-II and its specific UT receptor by Ames et al. in 1999 led to investigating the putative role of the interaction U-II/UT receptor in multiple pathophysiological effects in humans. Since urotensin-II is widely expressed in several peripheral tissues including cardiovascular system, the design and development of novel urotensin-II analogues can improve knowledge about structure-activity relationships (SAR). In particular, since the modulation of the U-II system offers a great potential for therapeutic strategies related to the treatment of several diseases, like cardiovascular diseases, the research of selective and potent ligands at UT receptor is more fascinating. In this paper, we review the developments of peptide and nonpeptide U-II structures so far developed in order to contribute also to a more rational and detectable design and synthesis of new molecules with high affinity at the UT receptor.

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Section: Nonpeptide Ligandsmentioning

confidence: 99%