Reference

Structure- and property-based design of factor Xa inhibitors: Pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs

All Rights Reserved.Some chemicals with cas registry numbers like 57260-73-8 and 759454-65-4 are also used. Structure- and property-based design of factor Xa inhibitors: Pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs. Young, Robert J.; Campbell, Matthew; Borthwick, Alan D.; Brown, David; Burns-Kurtis, Cynthia L.; Chan, Chuen; Convery, Maire A.; Crowe, Miriam C.; Dayal, Satish; Diallo, Hawa; Kelly, Henry A.; King, N. Paul; Kleanthous, Savvas; Mason, Andrew M.; Mordaunt, Jackie E.; Patel, Champa; Pateman, Anthony J.; Senger, Stefan; Shah, Gita P.; Smith, Paul W.; Watson, Nigel S.; Weston, Helen E.; Zhou, Ping ( Medicines Research Centre, GlaxoSmithKline, Stevenage, Hertfordshire SG1 2NY, UK). Bioorganic & Medicinal Chemistry Letters, 16(23), 5953-5957 (English) 2006 Elsevier Ltd. CODEN: BMCLE8. ISSN: 0960-894X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 27 Nonracemic 1-alaninyl-3-(6-chloro-2-naphthylsulfonylamino)-2-pyrrolidinones such as I are prepd. as factor Xa inhibitors for use as anticoagulants; the hydrophobicities, anticoagulant activities in rats, and pharmacokinetics of some of the compds. are detd. For example, I inhibits factor Xa with a Ki value of 1 nM and a value of 2.5 mM in the prothrombin time assay. 1-Alaninyl-3-(6-chloro-2-naphthylsulfonylamino)-2-pyrrolidinones have poorer pharmacokinetic profiles than the corresponding morpholine-based analogs, with increased plasma clearance and decreased oral bioavailabilities. The structure of I bound to factor Xa is detd. by X-ray crystallog. .

A selective fluorescent sensor for Cu2+ and its immobilization on CPG beads

All Rights Reserved. A selective fluorescent sensor for Cu2+ and its immobilization on CPG beads. Kovbasyuk, Larisa; Kraemer, Roland ( Anorganisch-Chemisches-Institut, Universitaet Heidelberg, Heidelberg 69120, Germany). 57260-73-8 and 918866-39-4 are also occured in this study. Inorganic Chemistry Communications, 9(6), 586-590 (English) 2006 Elsevier B.V. CODEN: ICCOFP. ISSN: 1387-7003. DOCUMENT TYPE: Journal CA Section: 79 (Inorganic Analytical Chemistry) A new dansyl derived fluorescent sensor for Cu(II) ions (1) was isolated by four-step org. synthesis with a good yield and characterized by NMR- and ESI-MS methods. UV-visible and fluorescent titrns. of 1 with Cu(II), Co(II), Zn(II), Ni(II), Ca(II) and Mg(II) salts were performed. 1 Forms a 1:1 stable complex in soln. (1 ′ 10-6 M) with Cu(II) and does not form such complex with other metals. 1 Was attached to a CPG 1000/100 resin. The fluorescence images of CPG 1000/100 resin with 1 showed strong fluorescence and complete absence of it in the presence of Cu(II) anions. .