ZIDOVUDINE: STRUCTURAL MODIFICATIONS AND THEIR IMPACT ON BIOLOGICAL ACTIVITIES AND PHARMACOKINETIC PROPERTIES

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 pr...

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Autores principales:	Mohsin,Noor Ul Amin, Ahmed,Matloob, Irfan,Muhammad
Lenguaje:	English
Publicado:	Sociedad Chilena de Química 2019
Materias:	Human Immunodeficiency Virus (HIV) Hybrids Phosphate and phosphonate Polymers Prodrugs
Acceso en línea:	http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072019000304523
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spelling	oai:scielo:S0717-970720190003045232019-11-06ZIDOVUDINE: STRUCTURAL MODIFICATIONS AND THEIR IMPACT ON BIOLOGICAL ACTIVITIES AND PHARMACOKINETIC PROPERTIESMohsin,Noor Ul AminAhmed,MatloobIrfan,Muhammad Human Immunodeficiency Virus (HIV) Hybrids Phosphate and phosphonate Polymers Prodrugs 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.info:eu-repo/semantics/openAccessSociedad Chilena de QuímicaJournal of the Chilean Chemical Society v.64 n.3 20192019-09-01text/htmlhttp://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072019000304523en10.4067/S0717-97072019000304523
institution	Scielo Chile
collection	Scielo Chile
language	English
topic	Human Immunodeficiency Virus (HIV) Hybrids Phosphate and phosphonate Polymers Prodrugs
spellingShingle	Human Immunodeficiency Virus (HIV) Hybrids Phosphate and phosphonate Polymers Prodrugs Mohsin,Noor Ul Amin Ahmed,Matloob Irfan,Muhammad ZIDOVUDINE: STRUCTURAL MODIFICATIONS AND THEIR IMPACT ON BIOLOGICAL ACTIVITIES AND PHARMACOKINETIC PROPERTIES
description	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.
author	Mohsin,Noor Ul Amin Ahmed,Matloob Irfan,Muhammad
author_facet	Mohsin,Noor Ul Amin Ahmed,Matloob Irfan,Muhammad
author_sort	Mohsin,Noor Ul Amin
title	ZIDOVUDINE: STRUCTURAL MODIFICATIONS AND THEIR IMPACT ON BIOLOGICAL ACTIVITIES AND PHARMACOKINETIC PROPERTIES
title_short	ZIDOVUDINE: STRUCTURAL MODIFICATIONS AND THEIR IMPACT ON BIOLOGICAL ACTIVITIES AND PHARMACOKINETIC PROPERTIES
title_full	ZIDOVUDINE: STRUCTURAL MODIFICATIONS AND THEIR IMPACT ON BIOLOGICAL ACTIVITIES AND PHARMACOKINETIC PROPERTIES
title_fullStr	ZIDOVUDINE: STRUCTURAL MODIFICATIONS AND THEIR IMPACT ON BIOLOGICAL ACTIVITIES AND PHARMACOKINETIC PROPERTIES
title_full_unstemmed	ZIDOVUDINE: STRUCTURAL MODIFICATIONS AND THEIR IMPACT ON BIOLOGICAL ACTIVITIES AND PHARMACOKINETIC PROPERTIES
title_sort	zidovudine: structural modifications and their impact on biological activities and pharmacokinetic properties
publisher	Sociedad Chilena de Química
publishDate	2019
url	http://www.scielo.cl/scielo.php?script=sci_arttext&pid=S0717-97072019000304523
work_keys_str_mv	AT mohsinnoorulamin zidovudinestructuralmodificationsandtheirimpactonbiologicalactivitiesandpharmacokineticproperties AT ahmedmatloob zidovudinestructuralmodificationsandtheirimpactonbiologicalactivitiesandpharmacokineticproperties AT irfanmuhammad zidovudinestructuralmodificationsandtheirimpactonbiologicalactivitiesandpharmacokineticproperties
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ZIDOVUDINE: STRUCTURAL MODIFICATIONS AND THEIR IMPACT ON BIOLOGICAL ACTIVITIES AND PHARMACOKINETIC PROPERTIES

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