SAR of Dihydropyridines

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Chapter: Medicinal Chemistry : Antianginals

1, 4-Dihydro pyridine ring is essential for activity. Substitution at N or oxidation or reduction of the ring reduces or abolishes the activity.


SAR of Dihydropyridines


  • 1, 4-Dihydro pyridine ring is essential for activity. Substitution at N or oxidation or reduction of the ring reduces or abolishes the activity.

  • A phenyl substitution at the 4th position is optimum for the activity. Substitution at para or unsubstituted phenyl ring reduces the activity.

  •  The 3rd and 5th position ester group optimizes activity. Placement of electron withdrawing substitution results in agonistic activity.

  • When the ester at C3 and C5 are nonidentical, the C4 become chiral and stereo selectivity is observed. S-enantiomers found to be more effective.

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