Synthesis and Pharmacological Properties of 1,3-Bis[(S)Phenylethyl]Imidazolidine-2-Thione

Enantiomerically and diastereomerically pure thiourea derivative (compound I) has been synthesized in two steps starting from (S)-1-phenylethanamine and 1,2-dibromoethane. Compound I was screened for various biochemical parameters including blood glucose level, serum total cholesterol level, serum bilirubin and triglyceride levels, serum glutamate pyruvate transaminase (SGPT) and alkaline phosphatase (ALP) activity in New Zealand White (NZW) rabbits. Compound I was also screened for brine shrimp cytotoxicity, antileishmanial and antioxidant activity. Acute toxicity tests in NZW rabbits were performed and the results showed that compound I was safe up to 2 mg/mL/kg rabbit body weight. For the blood parameters, it was found that compound I caused slightly reduced blood glucose level, increased blood serum bilirubin, ALP and SGPT levels, and caused no changes in cholesterol and triglyceride levels. Thus, results show that compound I possesses good cytotoxic, poor antileishmanial activity, and no prominent antioxidant activity.

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Acknowledgments

The authors are grateful to the University of Malakand (Chakdara, Dir Lower KPK, Pakistan) for making the resources available to carry out the research work.

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Correspondence to Mohammad Shoaib.

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Umar, M.N., Shoaib, M., Sadiq, M. et al. Synthesis and Pharmacological Properties of 1,3-Bis[(S)Phenylethyl]Imidazolidine-2-Thione. Pharm Chem J 50, 382–387 (2016). https://doi.org/10.1007/s11094-016-1456-4

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Keywords

  • antileishmanial activity
  • antioxidant
  • brine shrimp cytotoxicity
  • blood parameters
  • cytotoxicity
  • thiourea derivative