Search Results - "SOLINSKY, M. G"

Analogs of sub-nanomolar hMC1R agonist LK-184 [Ph(CH 2) 3CO-His- d-Phe-Arg-Trp-NH 2]. An additional binding site within the human melanocortin receptor 1? by Koikov, L.N, Ebetino, F.H, Solinsky, M.G, Cross-Doersen, D, Knittel, J.J

“…Of the 29 analogs of LK-184 ( 1) tested at the human MC1, MC3, and MC4 receptors (R), only LK-312 ( 3), partially mimicking the π-system of 1, had an EC 50 of…”
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Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH2 by KOIKOV, L. N, EBETINO, F. H, SOLINSKY, M. G, CROSS-DOERSEN, D, KNITTEL, J. J

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C6 Modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption by Isaacs, Richard C.A., Cutrona, Kellie J., Newton, Christina L., Sanderson, Philip E.J., Solinsky, Mark G., Baskin, Elizabeth P., Chen, I-Wu, Cooper, Carolyn M., Cook, Jacquelynn J., Gardell, Stephen J., Lewis, S.Dale, Lucas, Robert J., Lyle, Elizabeth A., Lynch, Joseph J., Naylor-Olsen, Adel M., Stranieri, Maria T., Vastag, Kari, Vacca, Joseph P.

“…1 (L-374,087) is a potent, selective, efficacious, and orally bioavailable thrombin inhibitor that contains a core 3-amino-2-pyridinone moiety. Replacement of…”
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Sub-nanomolar hMC1R agonists by end-capping of the melanocortin tetrapeptide His-D-Phe-Arg-Trp-NH(2) by Koikov, L N, Ebetino, F H, Solinsky, M G, Cross-Doersen, D, Knittel, J J

“…Twenty three derivatives of the core fragment His(6)-D-Phe(7)-Arg(8)-Trp(9)-NH(2) end-capped with carboxylic and sulfonic acids were synthesized and evaluated…”
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Structure-based design of novel groups for use in the P1 position of thrombin inhibitor scaffolds. Part 1: Weakly basic azoles by Isaacs, Richard C.A., Solinsky, Mark G., Cutrona, Kellie J., Newton, Christina L., Naylor-Olsen, Adel M., Krueger, Julie A., Lewis, S. Dale, Lucas, Bobby J.

“…Imidazoles and aminothiazoles, in spite of their weak basicity, have been optimized to function as potent P1 ligands in both a peptide series and a nonpeptide…”
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Synthesis of Tic-d-Phe Ψ[CH2–CH2] isostere and its use in the development of melanocortin receptor agonists by Tian, Xinrong, Chen, Xuemei, Gan, Lixian, Hayes, Jeffery C., Switzer, Adrian G., Solinsky, Mark G., Ebetino, Frank H., Wos, John A., Pinney, Beth B., Farmer, Julie A., Crossdoersen, Doreen, Sheldon, Russell J.

“…The first synthesis of Tic-d-Phe Ψ[CH2–CH2] isostere is described, which features diastereoselective alkylation of the tricyclic lactam 14. The use of this…”
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