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Synthesis and Biocompatibility Studies of New Iminodiacetic Acid Derivatives

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Laboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul. Muszyńskiego1, 90-151 Lodz, Poland
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Students Research Group, Laboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul. Muszyńskiego 1, 90-151 Lodz, Poland
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Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul. Muszyńskiego 1, 90-151 Lodz, Poland
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Author to whom correspondence should be addressed.
Molecules 2017, 22(12), 2265; https://doi.org/10.3390/molecules22122265
Received: 12 November 2017 / Revised: 6 December 2017 / Accepted: 12 December 2017 / Published: 18 December 2017
(This article belongs to the Section Medicinal Chemistry)
Background: Iminodiacetic acid (IDA) derivatives can be used as ligands to form complexes with technetium, with potential application as hepatobiliary diagnostic agents. The aim of this study was to synthesize five novel IDA derivatives and to compare their effects on plasma haemostasis with clinically approved ligands for technetium complexation. Methods: The influence of synthesized IDA derivatives on plasma haemostasis was evaluated spectrophotometrically by clot formation and lysis test (CL-test), coagulation assay, Prothrombin Time and Activated Partial Tromboplastin Time. The effects of the tested compounds on erythrocytes were assessed using haemolysis assays, microscopy and flow cytometry studies. Results: Despite their significant influence on the kinetic parameters of the process of clot formation and fibrinolysis, the tested ligands, at potential diagnostic concentrations, did not alter the overall potential of clot formation and lysis (CLAUC). At potential diagnostic concentrations (0.4 μmol/mL) all the tested compounds showed no adverse effects on the membranes of RBCs (Red Blood Cells). Conclusion: IDA derivatives with methoxy substituents in aromatic ring, exert multidirectional effects on plasma haemostasis and should be considered safe as their significant impacts were mostly observed at 4 μmol/mL, which is about 10-fold higher than the theoretical plasma concentrations of these compounds. View Full-Text
Keywords: iminodiacetic acid; radiopharmaceuticals; biocompatibility; haemostasis iminodiacetic acid; radiopharmaceuticals; biocompatibility; haemostasis
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Markowicz-Piasecka, M.; Dębski, P.; Mikiciuk-Olasik, E.; Sikora, J. Synthesis and Biocompatibility Studies of New Iminodiacetic Acid Derivatives. Molecules 2017, 22, 2265.

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