Synthesis, Chemical Stability and Comparative Anti-Hypertensive Activity of Indolizine Derivatives of Propranolol

International E-publication: Publish Projects, Dissertation, Theses, Books, Souvenir, Conference Proceeding with ISBN. International E-Bulletin: Information/News regarding: Academics and Research

Synthesis, Chemical Stability and Comparative Anti-Hypertensive Activity of Indolizine Derivatives of Propranolol

Author Affiliations

¹Department of Pharmaceutical Chemistry, Sri Indu Institute of Pharmacy, Sheriguda, Ibrahimpatnam, Telangana, India
²Department of Pharmaceutical Chemistry, Acharya and B M Reddy College of Pharmacy, Bangalore, Karnataka, India
³Department of Pharmaceutical Chemistry, Acharya and B M Reddy College of Pharmacy, Bangalore, Karnataka, India
⁴Department of Pharmaceutical Chemistry, Acharya and B M Reddy College of Pharmacy, Bangalore, Karnataka, India

Res. J. Recent Sci., Volume 5, Issue (6), Pages 34-39, June,2 (2016)

Abstract

Prodrugs are chemically modified versions of a pharmacologically active agent, which undergo transformation in vivo to release the active drug. Prodrugs of Propranolol have been designed with an aim to achieve improved therapeutic and biopharmaceutical properties and also to reduce the extent of first pass metabolism. All the synthesized derivatives 9a-cwere subjected to drug release study and further evaluated for in vivo anti-hypertensive activity using fructose induced noninvasive tail cuff method. Among all the synthesized derivatives, 9chas shown significant anti-hypertensive activity and prolonged duration of action when compared to the standard drug Propranolol.

References

Karaman R. (2012)., The future of prodrugs designed by computational chemistry., Drug Des., 1(1),1-3.
Google Scholar
Han H.K. and Amidon G.L. (2000)., Targeted prodrug design to optimize drug delivery., AAPS Pharma. Sci., 2(1), 1-2.
Google Scholar
Prakash Rao H.S. (2003)., Capping Drugs: Development of prodrugs., Resonance, 8(2), 19-27.
Google Scholar
Kuei-Meng Wu. (2009)., A New Classification of prodrugs: Regulatory Perspectives., Pharmaceuticals, 2, 77-81. doi:10.3390/ph2030077.
Google Scholar
Rathnakar C.H. and Das A.K. (2011)., Synthesis, Hydrolysis Kinetics and Comparative anti-tubercular activity of indolizine derivatives of Isoniazid / Pyrazinamide / Ethionamide., Int. J. Pharm. Sci. Rev and Res., 6(2), 128-131.
Denny G. and Das A.K. (2005)., Synthesis and evaluation of central nervous system depressant activity of some indolizine derivatives., [M. Pharm Thesis]. Rajiv Gandhi University of Health Sciences, Bangalore, India.
Google Scholar
Mayukh B. and Das A.K. (2004)., Synthesis and pharmacological screening of some indolizinamidoglutamidoglutamine derivatives., Ind. J. Heterocycl. Chem., 14(9), 81-82.

[ref1] Karaman R. (2012)., The future of prodrugs designed by computational chemistry., Drug Des., 1(1),1-3.
Google Scholar

[ref2] Han H.K. and Amidon G.L. (2000)., Targeted prodrug design to optimize drug delivery., AAPS Pharma. Sci., 2(1), 1-2.
Google Scholar

[ref3] Prakash Rao H.S. (2003)., Capping Drugs: Development of prodrugs., Resonance, 8(2), 19-27.
Google Scholar

[ref4] Kuei-Meng Wu. (2009)., A New Classification of prodrugs: Regulatory Perspectives., Pharmaceuticals, 2, 77-81. doi:10.3390/ph2030077.
Google Scholar

[ref5] Rathnakar C.H. and Das A.K. (2011)., Synthesis, Hydrolysis Kinetics and Comparative anti-tubercular activity of indolizine derivatives of Isoniazid / Pyrazinamide / Ethionamide., Int. J. Pharm. Sci. Rev and Res., 6(2), 128-131.

[ref6] Denny G. and Das A.K. (2005)., Synthesis and evaluation of central nervous system depressant activity of some indolizine derivatives., [M. Pharm Thesis]. Rajiv Gandhi University of Health Sciences, Bangalore, India.
Google Scholar

[ref7] Mayukh B. and Das A.K. (2004)., Synthesis and pharmacological screening of some indolizinamidoglutamidoglutamine derivatives., Ind. J. Heterocycl. Chem., 14(9), 81-82.