Wolkenberg S.E.,Sumneytown Pike |
Zhao Z.,Sumneytown Pike |
Thut C.,Sumneytown Pike |
Maxwell J.W.,Sumneytown Pike |
And 5 more authors.
Journal of Medicinal Chemistry | Year: 2011
Agonists of somatostatin receptor subtype 2 (sst2) have been proposed as therapeutics for the treatment of proliferative diabetic retinopathy and exudative age-related macular degeneration. An HTS screen identified 2-quinolones as weak agonists of sst2, and these were optimized to provide small molecules with sst2 binding and functional potency comparable to peptide agonists. Agonist 21 was shown to inhibit rat growth hormone secretion following systemic administration and to inhibit ocular neovascular lesion formation after local administration. © 2011 American Chemical Society.
Kuduk S.D.,Sumneytown Pike |
Di Marco C.N.,Sumneytown Pike |
Saffold J.R.,Sumneytown Pike |
Ray W.J.,Sumneytown Pike |
And 7 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2014
A series of methoxynaphthalene amides were prepared and evaluated as alternatives to quinolizidinone amide M1 positive allosteric modulators. A methoxy group was optimal for M1 activity and addressed key P-gp issues present in the aforementioned quinolizidinone amide series. © 2014 Elsevier Ltd. All rights reserved.