Uracils As Potent Antagonists of the Human Gonadotropin-releasing Hormone Receptor Without Atropisomers
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Uracil derivatives were designed and synthesized to avoid atropisomers observed in the 6-methyluracils as antagonists of the human GnRH receptor. Optimization at the 1- and 5-positions of the uracil resulted in potent compounds such as 24 (Ki=0.45 nM).
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