Klaus Urbahns et al.
Bioorganic & medicinal chemistry letters, 21(11), 3354-3357 (2011-05-03)
We have identified naphthol derivatives as inhibitors of the vanilloid receptor TRPV1 by high throughput screening. The initial lead showed high clearance in rats and has been optimized by enhancing the acidity of the phenol group. Compound 6b has reduced...
Hironobu Maezaki et al.
Bioorganic & medicinal chemistry, 19(15), 4482-4498 (2011-07-12)
Dipeptidyl peptidase IV (DPP-4) inhibition is a validated therapeutic option for type 2 diabetes, exhibiting multiple antidiabetic effects with little or no risk of hypoglycemia. In our studies involving non-covalent DPP-4 inhibitors, a novel series of quinoline-based inhibitors were designed...
Shi, J.; et al.
Chinese Chemical Letters = Zhongguo Hua Xue Kuai Bao, 22, 899-899 (2011)
Salvatore Cananzi et al.
Bioorganic & medicinal chemistry, 19(16), 4971-4984 (2011-07-26)
A novel 5-oxa-6a,8-diazaindeno[2,1-b]phenanthren-7-one scaffold was designed and synthesized as an active analogue of the cytotoxic marine alkaloid Lamellarin D. The design was based on molecular modeling of the site of interaction of Lamellarin D with DNA-topoisomerase I cleavable complex, whereas...
Jhih-Bin Chen et al.
ChemMedChem, 6(8), 1390-1400 (2011-06-22)
A novel compound, N⁶-(4-hydroxybenzyl)adenosine, isolated from Gastrodia elata and which has been shown to be a potential therapeutic agent for preventing and treating neurodegenerative disease, was found to target both the adenosine A(2A) receptor (A(2A) R) and the equilibrative nucleoside...