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Ch. Kantlam ¹, M. Srinivasa Murthy ², Y. Narsimha Reddy ³

Affiliations
1 School of Pharmaceutical Sciences, Jawaharlal Nehru Technological University, Kakinada - 533 003, Andhra Pradesh, IN
2 Department of Pharmaceutical Chemistry, Vignan Institute of Pharmaceutical Sciences, Near Ramoji Film City, Deshmukhi, Nalgonda - 508 284, Telangana State, IN
3 Department of Pharmacology, University College of Pharmaceutical Sciences, Kakatiya University, Warangal - 506 009, Telangana State, IN

Abstract

Purpose: The present research work is aspired to describe the synthesis, characterization and antibacterial activity of novel Mannich derivatives (4a-4f) derived from apocynin.

Methodology/Approach: In the present work, a novel chalcone was prepared by Claisen-Schmidt condensation of apocynin with benzo[b]furan aldehyde. Mannich bases were prepared by reaction of 3- (benzofuran-2-yl)-1-(4-hydroxy-3-methoxyphenyl)prop-2-en-1-one with formaldehyde and 2° amines.

Findings: All the newly synthesized Mannich base derivatives were characterized by their IR, NMR and Mass spectral data. Further all these final compounds were evaluated for their antibacterial activity using norfloxacin as standard reference. It was observed that among the final derivatives (4a-4f), compounds incorporated with morpholino, piperazino and piperidino moieties (4c-4e) exhibited excellent antibacterial activity, while the compound (4f) with pyyrolidino substituent showed similar promising activity and other compounds (4a-4b) possessed moderate activity.

Original Value: The review of literature revealed that conversion of various acyclic conjugated α,β-unsaturated ketones e.g. chalcones, into the corresponding Mannich bases was often accompanied by increased bioactivity both in vitro and in vivo. These facts prompted us to synthesize novel Mannich base derivatives having better biological activity. All the synthesized compounds were screened for their in vitro antibacterial activity.

Conclusion: The study revealed that compounds (4c), (4d) and (4e) derivatives exhibited highest activity against the tested bacteria.

Keywords

Apocynin, Chalcone, Mannich Derivative, Antibacterial Activity.

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H. Parameshwar , G. Krishna Mohan , B. Ravi Kumar , Y. Narsimha Reddy

Abstract

The hepatoprotective activity of methanolic extract of Borreria articularis ( L.F) F.N. W illams: ( Rubiaceae ) at doses of 250 mg/kg and 500 mg/kg were evaluated by carbon tetrachloride (CCl ₄ ) intoxication in rats. The toxic group which received 25% CCl ₄ in olive o il (1 ml/kg ) per oral (p.o), alone exhi bited significant incre ase in serum ALT , AS T , ALP , TB l evels. It also exhibited significant (P<0. 001) decre ase in TP and ALB l evels. The groups received pretreatment of Borreria articularis at a dose of 250 and 500 mg/kg b.w.p.o. had reduced the AST, ALT, ALP and TB levels and the effects were comp ar ed with standard drug (Silymarin 100 mg/kg b .w.p. o).The total protein (TP) and albumin (ALB) levels we re signifi cantly increased in the animals received pretre atment of the extract at the moderate and higher dose l evels and the histop athological studi es also supported the protective effect of the extract.

Keywords

Carbon Tetra Chloride, Silymarin, Borreria articularis, Biochemical Parameters and Histological Study.

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