ABSTRACT

Design, Synthesis and Evaluation of 2-amino-4-aryl-3-carbethoxy-

4H-1-benzopyran derivatives as potential antihypertensive agents.

ABSTRACT

Hypertension is the major health problem worldwide. Globally 7 million people die and
1.5 billion suffer every year because of high blood pressure levels. There is consistant
demand to develop new molecules for hypertension therapy. In present work various
derivatives of 4H-1-benzopyran scaffolds were designed by indirect type of molecular
modeling using Nifedipine. It shows very less RMSD value. On the basis of this we
planned to synthesize derivatives of 4H-1-benzopyarn derivatives for antihypertensive
activity.

R= H, 2-NO 2, 3-NO2,4-NO2, 2,3-diChloro

Title compounds were synthesized by literature procedure. Enantioselective synthesis of

some compound was also performed and the obtained product was found to have (S)-
configuration. Docking analysis was also carried out and all the compounds show good
binding score. All the compounds were screened for in-vivo antihypertensive activity
and they exhibited promising antihypertensive activity with siginificant recovery time.
The compound Ethyl - 2 - amino - 4 - (2-nitrophenyl) - 7, 7 - dimethyl - 5 - oxo - 5 , 6 ,
7,8-tetrahydro 4H-1-benzopyran 3-carboxylate (61b) and Ethyl -2-amino-4-(2,3-
dichloro)l-7-hydroxy-4H-1-benzopyran 3-carboxylate (72e) were found to be potent
compound as comprared to standard Nifedipine. The new 4H-1-benzopyarn derivatives
represent a potential strategy for the treatment of arterial hypertension.

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