54752-10-2Relevant articles and documents
A novel bifunctional chelating agent based on bis(hydroxamamide) for 99mTc labeling of polypeptides
Ono, Masahiro,Ohgami, Masatsugu,Haratake, Mamoru,Saji, Hideo,Nakayama, Morio
experimental part, p. 71 - 79 (2012/06/30)
This paper describes the synthesis and biological evaluation of a novel bifunctional chelating agent (BCA) based on bis(hydroxamamide) for 99mTc labeling of polypeptides. We successfully designed and synthesized C3(BHam)2·COOH as a new BCA. C 3(BHam)2·COOH formed a stable 99mTc complex and enabled us to prepare 99mTc-labeled polypeptides by using a 2,3,5,6-tetrafluorophenol (TFP) active ester of C3(BHam) 2·COOH. 99mTc-C3(BHam) 2·HSA prepared with C3(BHam)2·TFP was stable in both murine plasma and an excess of l-cysteine without any dissociation of 99mTc from polypeptides. Furthermore, the blood clearance of 99mTc-C3(BHam)2·HSA in mice was similar to that of 125I-HSA, suggesting that C 3(BHam)2·COOH retained stable binding between 99mTc and the polypeptides in vivo. When 99mTc-C 3(BHam)2·NGA was injected into mice, the radioactivity showed high hepatic uptake early on and a rapid clearance from the liver, indicating that C3(BHam)2·COOH did not affect the pharmacokinetics of polypeptides in vivo and gave radiometabolites, which displayed a rapid elimination from the liver. Such characteristics would render C3(BHam)2·COOH attractive as a new BCA for 99mTc labeling of polypeptides. Copyright
Heterocycles from Nitrile Oxides. 3. 1,2,4-Oxadiazol-5(4H)-ones
Hussein, Ahmad Q.
, p. 127 - 128 (2007/10/02)
The reaction of nitrile oxides with potassium cyanate gives 3-aryl-1,2,4-oxadiazol-5(4H)-ones (5).These heterocycles are also obtained by cyclization of the corresponding O-carbethoxyamidoximes (7) with sodium ethoxide.
