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Volume 76
Issue 3
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Article

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

by
Yogesh Kumar TYAGI
1,
Shvetambari TYAGI
2,
Hanumantharao Guru RAJ
2 and
Rajinder Kumar GUPTA
3,*
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.
Sci. Pharm. 2008, 76(3), 395-414; https://doi.org/10.3797/scipharm.0805-08
Submission received: 11 May 2008 / Accepted: 11 August 2008 / Published: 12 August 2008
Versions Notes

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

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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. https://doi.org/10.3797/scipharm.0805-08

AMA Style

TYAGI YK, TYAGI S, RAJ HG, GUPTA RK. Synthesis of Novel 4-Methylcoumarins and Comparative Specificities of Substituted Derivatives for Acetoxy Drug: Protein Transacetylase. Scientia Pharmaceutica. 2008; 76(3):395-414. https://doi.org/10.3797/scipharm.0805-08

Chicago/Turabian Style

TYAGI, Yogesh Kumar, Shvetambari TYAGI, Hanumantharao Guru RAJ, and Rajinder Kumar GUPTA. 2008. "Synthesis of Novel 4-Methylcoumarins and Comparative Specificities of Substituted Derivatives for Acetoxy Drug: Protein Transacetylase" Scientia Pharmaceutica 76, no. 3: 395-414. https://doi.org/10.3797/scipharm.0805-08

APA Style

TYAGI, Y. K., TYAGI, S., RAJ, H. G., & GUPTA, R. K. (2008). Synthesis of Novel 4-Methylcoumarins and Comparative Specificities of Substituted Derivatives for Acetoxy Drug: Protein Transacetylase. Scientia Pharmaceutica, 76(3), 395-414. https://doi.org/10.3797/scipharm.0805-08

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