43218-50-4Relevant articles and documents
The [(Cp)M(CO)3] (M=Re, 99mTc) building block for imaging agents and bioinorganic probes: Perspectives and limitations
Can, Daniel,Peindy N'Dongo, Harmel W.,Spingler, Bernhard,Schmutz, Paul,Alberto, Roger,Raposinho, Paula,Santos, Isabel
, p. 1849 - 1866,18 (2020/08/24)
Starting from asymmetric Thiele's acid derivatives, two different imaging probes [99mTc(CO)3(CpR)] (R=potential targeting vector) are generated simultaneously in one-pot and from one substrate. This extends the previously introduced
Studies directed at the use of a parallel synthesis matrix to increase throughput in an in vivo assay
Leone-Bay,Freeman,O'Toole,Rosario-Gray,Salo-Kostmayer,Tai,Mercogliano,Baughman
, p. 3573 - 3576 (2007/10/03)
Heparin is the anticoagulant of choice for hospitalized patients, but it is dosed only by injection because it is not absorbed following oral administration. We have discovered and prepared compounds (delivery agents) that facilitate the gastrointestinal absorption of heparin in rats, monkeys, and humans when given orally. We are currently developing a parallel synthesis approach to increase our delivery agent screening throughput in vivo. This approach has been used to produce micromolar quantities of compounds for testing in rats in a 5 x 5 parallel synthesis array. Using an amine benzoylation reaction sequence, 10 mixtures were prepared. These mixtures contained equal weight quantities of five N-substituted, non-α, amino acid delivery agents. Each of these mixtures was orally administered to rats in combination with heparin, and plasma clotting times (APTT) were measured to determine activity. Deconvolution of the data accurately identified the most active individual components. Independent synthesis of these compounds verified their activity. This parallel synthesis approach is an effective tool for the screening of oral heparin delivery agents and has increased screening throughput significantly.
Composition containing a penem or carbapenem antibiotic and the use of the same
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, (2008/06/13)
Administration of an N-acylated amino acid in association with a penem or carbapenem antibiotic relieves or eliminates the renal problems associated with administration of the antibiotic alone. The amino acid derivative and antibiotic may be formulated together as a composition or administered separately, either simultaneously or sequentially.