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3.
Scheme 1

Scheme 1. From: Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor.

Synthesis of APJ antagonists, conditions: (a) neat SOCl2 (17 equiv); (b) R1SH (1 equiv), NaOMe (1 equiv), MeCN; (c) R2COCl (1.4 equiv), Cs2CO3 (1 equiv), MeCN.

Patrick R. Maloney, et al. Bioorg Med Chem Lett. ;22(21):6656-6660.
4.
Figure 2

Figure 2. From: Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor.

Representative dose response curve for ML221. The compound antagonized Ap13-mediated activation of APJ in a concentration-dependent manner in both a cAMP assay (■), and a β-arrestin recruitment assay (●). Data plotted are the mean ± SEM% inhibition of Ap13. Curves represent the best fit of a four parameter logistic generated using GraphPad Prism5.

Patrick R. Maloney, et al. Bioorg Med Chem Lett. ;22(21):6656-6660.

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