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Synthesis, Characterization, and Antihypertensive Evaluation of Some Novel 2,2,8,8-Tetramethyl-2,3,7,8-Tetrahydro-4,6-Diamino- 3,7-Dihydroxy-6,7-Epoxy-Benzo-[1,2-b:5,4-b']Dipyran Derivatives


Affiliations
1 Department of Pharmaceutical Chemistry, Krupanidhi College of Pharmacy, Bangalore 35, India
2 Department of Pharmaceutical Chemistry, Institute of Pharmacy, Nirma University, Ahmedabad, Gujarat 382481, India
 

A series of 2,2,8,8-tetramethyl-2,3,7,8-tetrahydro-4,6-diamino-3,7-dihydroxy-6,7-epoxy-benzo-[1,2-b:5,4-b']dipyran derivatives 7a-e and 8a-e were synthesized from resorcinol. All the synthesized compounds were characterized by FTIR, mass spectra, and 1H NMR. These compounds were evaluated for antihypertensive activity using Wister Albino Rat model. Direct antihypertensive activity was performed using the instrument BIOPAC System MP-36 Santa Barbara, California, for recording blood pressure response. Among the title compounds, compounds 7b, 7c, and 7d showed potent antihypertensive activity and other compounds were also found to exert low and moderate antihypertensive activity. The relaxant potency in rat aorta and trachea was used for biological characterization of the benzopyrans. Structure-activity relationships study was investigated around position-4 of the benzopyran nucleus.
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  • Synthesis, Characterization, and Antihypertensive Evaluation of Some Novel 2,2,8,8-Tetramethyl-2,3,7,8-Tetrahydro-4,6-Diamino- 3,7-Dihydroxy-6,7-Epoxy-Benzo-[1,2-b:5,4-b']Dipyran Derivatives

Abstract Views: 177  |  PDF Views: 39

Authors

Pankaj Dwivedi
Department of Pharmaceutical Chemistry, Krupanidhi College of Pharmacy, Bangalore 35, India
Kuldipsinh P. Barot
Department of Pharmaceutical Chemistry, Institute of Pharmacy, Nirma University, Ahmedabad, Gujarat 382481, India
Shailesh Jain
Department of Pharmaceutical Chemistry, Institute of Pharmacy, Nirma University, Ahmedabad, Gujarat 382481, India
Manjunath D. Ghate
Department of Pharmaceutical Chemistry, Institute of Pharmacy, Nirma University, Ahmedabad, Gujarat 382481, India

Abstract


A series of 2,2,8,8-tetramethyl-2,3,7,8-tetrahydro-4,6-diamino-3,7-dihydroxy-6,7-epoxy-benzo-[1,2-b:5,4-b']dipyran derivatives 7a-e and 8a-e were synthesized from resorcinol. All the synthesized compounds were characterized by FTIR, mass spectra, and 1H NMR. These compounds were evaluated for antihypertensive activity using Wister Albino Rat model. Direct antihypertensive activity was performed using the instrument BIOPAC System MP-36 Santa Barbara, California, for recording blood pressure response. Among the title compounds, compounds 7b, 7c, and 7d showed potent antihypertensive activity and other compounds were also found to exert low and moderate antihypertensive activity. The relaxant potency in rat aorta and trachea was used for biological characterization of the benzopyrans. Structure-activity relationships study was investigated around position-4 of the benzopyran nucleus.