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Novel, Orally Bioavailable γ-Aminoamide CC Chemokine Receptor 2 (CCR2) Antagonists
Through modification of a screening hit we have discovered a structurally distinct new lead, (2S)-N-[3,5-bis(trifluoromethyl)benzyl]-2-(4-fluorophenyl)-4-(4-phenylpiperidin-1-yl)butanamide (11),Expand
2-(3,5-Dimethylphenyl)tryptamine derivatives that bind to the GnRH receptor.
TLDR
The study has helped define structural requirements for GnRH receptor binding for the 2-aryltryptamine GnRH antagonists by evaluating para-substituents on the 4-phenylbutyl side chain attached to the tryptamine nitrogen. Expand
Potent, orally bioavailable somatostatin agonists: good absorption achieved by urea backbone cyclization.
TLDR
Backbone cyclization of urea-based somatostatin agonists resulted in novel, orally bioavailable agonists that were highly potent analogs, selective for receptor subtype 2, and having good oral bioavailability. Expand
Novel, orally bioavailable gamma-aminoamide CC chemokine receptor 2 (CCR2) antagonists.
Through modification of a screening hit we have discovered a structurally distinct new lead, (2S)-N-[3,5-bis(trifluoromethyl)benzyl]-2-(4-fluorophenyl)-4-(4-phenylpiperidin-1-yl)butanamide (11),Expand