Synthesis and antimicrobial screening of new 9, 10-dihydro Anthracene-9, 10-endo-α, B-succinimides bearing pharmacologically active components

Abstract EN

This operation five early cyclic imides bearing biologically an effect components were Syntheside.

9,10-dihydro anthracene-9,10-endo-α,β-Succinicanhydride was synthesized then used in the synthesis of target imides.

Two nitrogen containing hetero cycles namely pyridine and quinazoline are selected as biologically active components to be used in this work beside two β-lactam antibiotics namely Ampicillin and Cefotaxime in addition to active folic acid.

The new cyclic imides were synthesized by two steps in the first one 9,10-dihyro anthracene-9,10-endo-α,β-Succinic anhydride was introduced in reaction with 4-amino pyridine,1-amino-quinazoline-2-one, Ampicillin and Cefotaxime producing the corresponding N-(drug) or N-(heterocycle)-9,10-dihydro anthracene-9,10-endo-(α,β)-Succinamic acid with acetic anhydride which in turn were dehydrated.

In the second step via reaction involving ,acetic anhydride and sodium acetate,anhydrous below reflux conditions producing the target N-(drug) or N-(heterocycle) ,10-dihyro anthracene-(9,10)-endo-α,β-Succinimides.

N-(folic acid )-9,10-dihyro (anthracene-9,10-endo-α,β)-Succinimide was synthesized via direct reaction between folic acid and 9,10-dihydro anthracene-9,10-endo-α,β-Succinic anhydride in glacial acetic acid under reflux.

Results ofantimicrobial activity evaluation of the newly synthesized imides showed that the new imides exhibit very high antimicrobial activity against the tested bacteria and fungi.