42548-08-3Relevant academic research and scientific papers
AMIDE BOND ISOSTERES: IMIDAZOLINES IN PSEUDOPEPTIDE CHEMISTRY
Jones, Raymond C.F.,Ward, Gary J.
, p. 3853 - 3856 (2007/10/02)
The 2-imidazole ring has been incorporated as an amide bond replacement into pseudodipeptides, a pseudotripeptide, and pseudopentapeptide enkephalin analogues.
Specific Covalent Fixation of Chelating Agents on Peptides
Sergheraert, Christian,Maes, Pierrette,Tartar, Andre
, p. 1061 - 1064 (2007/10/02)
The synthesis of two selectively protected bifunctional analogues of ethylenediaminetetra-acetic acid (EDTA) is described.In these analogues the four carboxy groups involved in chelation are protected as benzyl or t-butyl esters, while the fifth one, whic
Tissue Distribution Properties of Technetium-99m-Diamide-Dimercaptide Complexes and Potential Use as Renal Radiopharmaceuticals
Kasina, Sudhakar,Fritzberg, Alan R.,Johnson, Dennis L.,Eshima, Dennis
, p. 1933 - 1940 (2007/10/02)
A series of new ligands and the corresponding technetium-99m chelates based on diamide dimercaptide donor groups were synthesized as derivatives of technetium-99m 1,2-bis(2-thioacetamido)ethane, a complex shown to be excreted by renal tubular secretion. Chelation with 99mTc resulted in single radiochemical products or the expected numbers of stereoisomers. They were purified by high-performance liquid chromatography (HPLC) and evaluated in mice as potential renal tubular function agents. The in vivo properties were sensitive to the presence of functional groups, the positional isomerism of the carboxylate group functionality, and the chelate ring stereochemistry of the ligand. The presence of methyl groups slowed renal transit and decreased renal specificity. Cyclohexyl rings fused to the ethylene bridge of the center chelate ring decreased renal excretion while aromatic rings essentially abolished renal excretion. Slow hepatobiliary clearance was observed as an alternate mode of excretion. Polar groups, such as hydroxyl, carboxylate, and carboxamide, increased renal excretion rates and specificity in a stereochemically dependent manner. 99mTc chelates of 1,3-bis(2-thioacetamido)-2-hydroxypropane, 3,4-bis(2-thioacetamido)butanoate and 1,8-dimercapto-2,7-dioxo-3,6-diazanonanoate were identified as promising new renal radiopharmaceuticals.
AMINOACID DERIVATIVES AS ANTIHYPERTENSIVES
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, (2008/06/13)
The invention relates to new carboxyalkyl dipeptide derivatives and related compounds which are useful as antihypertensives.
