Next Article in Journal
Synthesis, Pharmacophore Modeling, and Biological Evaluation of Novel 5H-Thiazolo[3,2-a]pyrimidin-5-one Derivatives as 5-HT2A Receptor Antagonists
Previous Article in Journal
Topological Models for Prediction of Pharmacokinetic Parameters of Cephalosporins using Random Forest, Decision Tree and Moving Average Analysis
Article Menu

Article Versions

Export Article

Open AccessArticle
Sci. Pharm. 2008, 76(3), 395-414; doi:10.3797/scipharm.0805-08 (registering DOI)

Synthesis of Novel 4-Methylcoumarins and Comparative Specificities of Substituted Derivatives for Acetoxy Drug: Protein Transacetylase

1
School of Basic and Applied Sciences, GGSIP University, Kashmere Gate, Delhi-110 403, India
2
Department of Biochemistry, Vallabhbhai Patel Chest Institute, University of Delhi, Delhi-110 007, India
3
School of Biotechnology, GGSIP University, Kashmere Gate, Delhi-110 403, India
*
Author to whom correspondence should be addressed.
Received: 11 May 2008 / Accepted: 11 August 2008 / Published: 12 August 2008
Download PDF [169 KB, uploaded 28 December 2016]

Abstract

Our laboratory has been credited for the discovery of a unique membrane bound enzyme termed Acetoxy Drug: Protein Transacetylase (TAase) catalyzing the transfer of acetyl group from polyphenolic peracetates (PA) to certain functional proteins resulting in the modulation of their catalytic activity. In this report, we have synthesized eight novel 4-methylcoumarins and demonstrated the comparisons of acetoxy derivatives of 4-methylcoumarin with their propoxy and butoxy derivatives for the modulation of some receptor proteins such as cytochrome P-450 (Cyt.P-450), NADPH cytochrome c reductase and cytosolic glutathione S-transferase (GST). The results clearly indicated that acetoxy derivatives have very high efficacy for the modulation of above mentioned functional proteins as compared to their other derivatives. We have also compared the acetoxy derivatives of 4-methylcoumarin with their acid substituted acetoxy derivatives and found that inclusion of carboxylic acid groups on the benzenoid rings of the coumarins system hardly affected TAase mediated catalytic activity.
Keywords: Coumarins; Acetoxy drug: protein transacetylase (TAase); DAMC; Structure Activity Relationship (SAR); Acetyl group Coumarins; Acetoxy drug: protein transacetylase (TAase); DAMC; Structure Activity Relationship (SAR); Acetyl group
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

TYAGI, Y.K.; TYAGI, S.; RAJ, H.G.; GUPTA, R.K. Synthesis of Novel 4-Methylcoumarins and Comparative Specificities of Substituted Derivatives for Acetoxy Drug: Protein Transacetylase. Sci. Pharm. 2008, 76, 395-414.

Show more citation formats Show less citations formats

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Sci. Pharm. EISSN 2218-0532 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top