Novel Malonamide Derivatives as .ALPHA.v.BETA.3 Antagonists. Syntheses and Evaluation of 3-(3-Indolin-1-yl-3-Oxopropanoyl)aminopropanoic Acids on Vitronectin Interaction with .ALPHA.v.BETA.3.

Biological and molecular properties of a new αvβ3/αvβ5 integrin antagonist

“…Primary cultures of bovine microvascular endothelial cells were obtained from bovine adrenal glands as described (27) and maintained in DMEM supplemented with 20% Solid-Phase Receptor-Binding Assay The receptor-binding assays were done as described previously (24,28,29 Each data point is the result of the average of triplicate wells and was analyzed by nonlinear regression analysis with Allfit program.…”

Synthesis, radiolabeling and evaluation of novel amine guanidine derivatives as potential positron emission tomography tracers for the ion channel of the N-methyl-d-aspartate receptor

“…After methylation of the cyanamide moiety and reduction of the nitro moiety, 17 was obtained in 72% overall yield. Subsequent monoprotection of the amine moiety with a trifluoroacetic acid group [33] gave 18 in 86% yield and the subsequent methylation gave 19 in quantitative yield. Compound 17 was dimethylated to obtain 20 in 51% yield.…”

“…The organic layer was collected, dried over anhydrous magnesium sulfate, filtered and evaporated to dryness under reduced pressure. The crude product was purified over silica (ethyl acetate/hexanes/Et 3 N, 33 …”

Asymmetric organocatalytic Michael addition of Meldrum’s acid to nitroalkenes: probing the mechanism of bifunctional thiourea organocatalysts

“…7 The methylated aniline 18 was easily prepared from the commercially available 3,5-bis(trifluoromethyl)aniline via trifluoroacetylation, methylation and hydrolysis, giving a practically pure product in excellent yield. 19 The condensation step was found to be somewhat problematic, since 18 is an extremely electron-poor nucleophile. Catalyst 13 was obtained by deprotonating 18 with n-BuLi at -78 °C and then adding the isothiocyanate dissolved in DMF.…”

“…There are other reports probing the activity of bifunctional thiourea catalysts by adding, blocking or removing additional hydrogen bond donor sites. Wang reported that catalyst activity in nitro-Michael addition is significantly boosted by addition of H-bond donor sites (19,20), giving improved yields and enantioselectivities. 20 Conversely, the enantioselectivity is significantly eroded when the additional coordination sites around the thiourea moiety are blocked or removed.…”