SYNTHESIS AND EVALUATION OF SOME SUBSTITUTED INDOLE DERIVATIVES FOR CARDIOVASCULAR ACTIVITY
Abstract
In the present study, a series of Indole containing the oxadiazole and thiazolidinones side chain at 3- position, is discussed. The synthesized Indole derivatives 4 (a-e), 5 (a-e) were evaluated for cardiovascular activities. Compound 3-[5’-(3”-indolomethylene)-1’,3’,4’-oxadiazol-2’-yl]-2-(p-methoxy phenyl)-4-thiazolidinone 5b, was found to be the most potent compound of the present study which showed cardiovascular activity of varying degree at dose 2.5 mg/Kg. The structures of these compounds were elucidated by IR, 1H NMR, mass spectroscopy and elemental analysis.
Keywords:
Indole derivatives, oxadiazole, thiazolidinone, antihypertensive, cardiovascular activityDOI
https://doi.org/10.25004/IJPSDR.2013.050102References
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3. Pandey VK, Mukesh, Kumar A, Trivedi Noopur. An investigation leading to preparation of tetra hydro- quinazoline derivatives involving ureidoalkylation and α- amidoalkylation reactions. Indian J.Chem. 2008; 47 B: 1910-1914.
4. Oliveira CSD, Lira BF, Filho JMB, Lorenzo JGF, Filho PFDA. Synthetic Approaches and Pharmacological Activity of 1, 3, 4-Oxadiazoles: A Review of the Literature from 2000-2012. Molecules. 2012; 17: 10192-10231; doi: 10.3390 / molecules 170910192.
5. Saini MS, Singh R, Dwivedi J, Kumar A. Synthesis and Biological Activity of some N- Benzylidene Derivatives of 2-Aryl-5- Hydroxy-7- Methyl-1, 2, 4- Triazolo-[1, 5-A]-Pyrimidines. Inter. J. Scie. Nature. 2012; 3(4): 925-927.
6. Kumar A, Gurtu S, Agrawal JC, Sinha JN, Bhargava KP, Shanker K. Synthesis and cardiovascular activity of substituted 4- azetidinones. J. Ind. Chem. Soc. 1983; LX: 608-609.
7. Arya, David PJ, Grewal RS, Kaul CL, Mizoni RH, Rajappa S, Shenoy SJ. Synthesis and Central Nervous system depressant Activity of some 2,3-disubstituted Indole. Ind. J. Chem. 1977; 15 B: 473-477.
8. Biswal S, Sahoo U, Sethy S, Kumar HKS, Banerjee M. Indole: The Molecule of Diverse Biological Activities. Asian J. Phar. Clin. Res. 2012; 5:1.
9. Kumar L, Bala S, Jeet K. The Diverse Pharmacological Importance of Indole Derivatives: A Review. Inter.J. Res. Phar. Sci. 2012; 2(2):23-33.
10. Sharma K, Jain R. Synthesis, reactions and anthelmintic activity of 1- [benzimidazol-2-yl-4-formyl- 3-[2’- (substituted phenyl) indol-3-yl] pyrazoles. Ind. J. Chem.2012. 51B: 1462-1469.
11. Mogilaiah K, Rao RB. Synthesis and antibacterial activity of some novel spiro [indole-pyrazolines], spiro [indole- pyrimidines] and spiro [indole-1, 5-benzodiazepine] containing 1, 8- napthyridine moiety. Indian J. Chem. 1998;37: 139-144.
12. Panwar H, Chaudhary N, Singh S. Synthesis, Characterization and Biological Activity of some Substituted Pyrazolyl and Pyrazolinyl- 1, 3, 4-Thiadiazino (6,5-b) Indoles. Rasayan J. Chem. 2011; 4(2): 371- 380.
13. Kumar A, Agarwal JC, Nath C, Gurtu S, Sinha JN, Bhargava KP, Shanker K. Synthesis and biological activity of 2-substituted – 3 – ethyl – N –alkyl / arylindoles. J. Hetro. Chem. 1981; 18(6): 1269-1271.
14. Grasso S, Molica C, Monforte AM, Monforte P, Zappala M, Monforte MT, Trovato A. Synthesis and antihypertensive activity evaluation of indole derivatives N-acetamido substituted. Farmaco. 1995; 50(2):113-117.
15. Smith QE. Pharmacological Screening tests progress in Medicinal Chemistry, 1, Butteworths, London.1960.
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01-09-2018
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“SYNTHESIS AND EVALUATION OF SOME SUBSTITUTED INDOLE DERIVATIVES FOR CARDIOVASCULAR ACTIVITY”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 5, no. 1, Sept. 2018, pp. 14-17, https://doi.org/10.25004/IJPSDR.2013.050102.
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How to Cite
“SYNTHESIS AND EVALUATION OF SOME SUBSTITUTED INDOLE DERIVATIVES FOR CARDIOVASCULAR ACTIVITY”. International Journal of Pharmaceutical Sciences and Drug Research, vol. 5, no. 1, Sept. 2018, pp. 14-17, https://doi.org/10.25004/IJPSDR.2013.050102.
