• English
    • العربية
  • English 
    • English
    • العربية
  • Login
View Item 
  •   DSpace Home
  • AQU Research Network Clusters
  • AQU researchers publications
  • View Item
  •   DSpace Home
  • AQU Research Network Clusters
  • AQU researchers publications
  • View Item
JavaScript is disabled for your browser. Some features of this site may not work without it.

Intramolecular Processes and Their Applications in Prodrugs Approaches- Experimental and Computational Studies

Thumbnail
View/Open
RES_27_JOURNAL_1-s2_0-S1567134816303252-main.pdf (767.3Kb)
Date
2015-11-15
Author
Karaman, Rafik
Jumaa, Salma
Awwadallah, Heba
Salah, Samya
Khawaja, Yahya
Karaman, Donia
Metadata
Show full item record
Abstract
This review supplies the reader with a detailed overview on the utilization of intramolecular processes for a design and synthesis of prodrugs. It is well known that a respected number of drugs suffer from low bioavailability, toxicity, unpleasant taste and presystemic first-pass metabolism which result in drug inactivation. The classical prodrug approach in which the linkage attaching the parent drug to its non-toxic linker and cleaved by in vivo enzyme’s catalyzed reactions has proven its success in solving toxicity and bioavailability related issues. On the other hand, prodrugs based on chemical interconversion in which the prodrug releases the corresponding active parent drug via inter or intramolecular chemical process in the absence of an enzyme is considered as a better alternative approach since the prodrug cleavage is not dependent in the efficiency or quantity of the enzyme catalyzes the interconversion of the prodrug. Examples of successful prodrugs using the chemical approach via intramolecular processes such as cyclization reactions are illustrated as well. In addition, another part of this review is devoted to cover reported studies on enzyme models and their utilization for the design and synthesis of a variety of novel prodrugs. In this approach, computational calculations using DFT and MM methods were exploited and correlations between experimentally determined and computed values of the rate-limiting step in the studied intramolecular processes were utilized in the prodrugs design. Selected examples of the designed prodrugs include aza-nucleosides for the treatment of myelodysplastic syndromes, the anti-Parkinson’s agent dopamine, the anti-viral acyclovir, the anti-malarial atovaquone, and statins for lowering cholesterol levels in the blood, the antihypertensive atenolol, the antibacterial cefuroxime, the anti-bleeding tranexamic acid, the decongestant phenylephrine, and the pain killer paracetamol.
URI
https://dspace.alquds.edu/handle/20.500.12213/860
Collections
  • AQU researchers publications [753]

DSpace software copyright © 2002-2016  DuraSpace
Contact Us | Send Feedback
Theme by 
Atmire NV
 

 

Browse

All of DSpaceCommunities & CollectionsBy Issue DateAuthorsTitlesSubjectsThis CollectionBy Issue DateAuthorsTitlesSubjects

My Account

LoginRegister

DSpace software copyright © 2002-2016  DuraSpace
Contact Us | Send Feedback
Theme by 
Atmire NV