Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists was written by Kaila, Neelu;Janz, Kristin;DeBernardo, Silvano;Bedard, Patricia W.;Camphausen, Raymond T.;Tam, Steve;Tsao, Desiree H. H.;Keith, James C. Jr.;Nickerson-Nutter, Cheryl;Shilling, Adam;Young-Sciame, Ruth;Wang, Qin. And the article was included in Journal of Medicinal Chemistry in 2007.Application of 150560-58-0 This article mentions the following:
Leukocyte recruitment of sites of inflammation and tissue injury involves leukocyte rolling along the endothelial wall, followed by firm adherence of the leukocyte, and finally transmigration of the leukocyte across cell junctions into the underlying tissue. The initial rolling step is mediated by the interaction of leukocyte glycoproteins containing active moieties such as sialyl Lewisx (sLex) with P-selectin expressed on endothelial cells. Consequently, inhibition of this interaction by means of a small mol. P-selectin antagonist is an attractive strategy for the treatment of inflammatory diseases such as arthritis. High-throughput screening of the Wyeth chem. library identified the quinoline salicylic acid class of compounds as antagonists of P-selectin, with potency in in vitro and cell-based assays far superior to that of sLex. Through iterative medicinal chem., it was identified analogs with improved P-selectin activity, decreased inhibition of dihydrooratate dehydrogenase, and acceptable CYP profiles. Lead compound , I, was efficacious in the rat AIA model of rheumatoid arthritis. In the experiment, the researchers used many compounds, for example, 5-Isopropylindoline-2,3-dione (cas: 150560-58-0Application of 150560-58-0).
5-Isopropylindoline-2,3-dione (cas: 150560-58-0) belongs to indole derivatives. In addition to tryptophan, indigo, and indoleacetic acid, numerous compounds obtainable from plant or animal sources contain the indole molecular structure. More than 200 indole derivatives have already been marketed as drugs or are under advanced stages of clinical trials.Application of 150560-58-0
Referemce:
Indole alkaloid derivatives as building blocks of natural products from闂佽壈浜崹淇沜illus thuringiensis闂佽壈浜粋鍧闂佽壈浜崹淇沜illus velezensis闂佽壈浜粋鍧 their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles