On October 12, 2000, Link, James; Liu, Gang; Pei, Zhonghua; Von Geldern, Thomas W.; Winn, Martin; Xin, Zhili; Wang, Sheldon; Boyd, Steven A.; Zhu, Gui-Dong; Freeman, Jennifer C.; Gunawardana, Indrani W.; Staeger, Michael A.; Jae, Hwan-soo; Lynch, John K. published a patent.Category: alcohols-buliding-blocks The title of the patent was Preparation of 2- or 4-(phenylthio)cinnamides as cell adhesion-inhibiting antiinflammatory and immune-suppressive compounds. And the patent contained the following:
The title compounds (I) [wherein R1-R5 = independently H, halo, (halo)alkyl, alkoxy, cyano, NO2, CHO, and least one of R1 or R3 is an (un)substituted cis- or trans-cinnamide; Ar = (un)substituted (hetero)aryl] were prepared as cell adhesion inhibitors for the treatment of inflammatory and immune diseases. Examples include syntheses for 443 invention compounds and data for 3 bioassays. For instance, a mixture of 2-[(2,4-dichlorophenyl)thio]benzaldehyde (preparation given), malonic acid, piperidine in anhydrous pyridine was heated at 110° for 2 h and then treated with aqueous HCl to give trans-2-[(2,4-dichlorophenyl)thio]cinnamic acid (91%). Conversion to the acid chloride followed by amidation with 6-amino-1-hexanol gave (E)-II (90%). In an integrin LFA-1/ICAM-1 biochem. interaction assay, I demonstrated inhibition at 4 μM. In cell-based adhesion assays which measure the ability of test compounds to block adherence of JY-8 cells (a human EBV-transformed B cell line expressing LFA-1 on its surface) to immobilized ICAM-1 or ICAM-3, I exhibited blocking activity at 4 μM and 0.6 μM, resp. The experimental process involved the reaction of (6-Bromo-2,3-dihydrobenzo[b][1,4]dioxin-2-yl)methanol(cas: 280752-78-5).Category: alcohols-buliding-blocks
The Article related to phenylthio cinnamide preparation cell adhesion inhibitor, aminocarbonylethenylphenyl phenyl sulfide preparation antiinflammatory, sulfide aminocarbonylethenylphenyl phenyl preparation immunosuppressant and other aspects.Category: alcohols-buliding-blocks
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