Vol 64 No 3 (2019): Journal of the Chilean Chemical Society
Original Research Papers
ZIDOVUDINE: STRUCTURAL MODIFICATIONS AND THEIR IMPACT ON BIOLOGICAL ACTIVITIES AND PHARMACOKINETIC PROPERTIES
Published
October 30, 2019
Keywords
- Human Immunodeficiency Virus (HIV),
- Hybrids,
- Phosphate and phosphonate,
- Polymers,
- Prodrugs
How to Cite
Ul Amin Mohsin, N., Ahmed, M., & Irfan, M. (2019). ZIDOVUDINE: STRUCTURAL MODIFICATIONS AND THEIR IMPACT ON BIOLOGICAL ACTIVITIES AND PHARMACOKINETIC PROPERTIES. Journal of the Chilean Chemical Society, 64(3), 4523-4530. Retrieved from https://jcchems.com/index.php/JCCHEMS/article/view/1314
Abstract
Zidovudine was the first drug approved for the treatment of Acquired Immuno Deficiency Syndrome (AIDS). Its chemical name is azidothymidine (AZT). AZT
use is associated with bone marrow toxicity. Shorter half-life and inability to penetrate the blood-brain barrier are the pharmacokinetic problems of this important
drug molecule. Various modifications have been carried out in the structure of AZT. These include modification of hydroxyl and azido group, thymidine ring,
preparation of phosphate and phosphonate derivatives, attachment of polymers and synthesis of hybrid molecules. Some of these changes produced compounds with
significantly increased activity and less toxicity. This review highlights the various structural modifications of AZT and their influence on biological activities and
pharmacokinetic properties.
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