Synthesis of Novel Cinnoline Fused Mannich Bases: Pharmacological Evaluation of Antibacterial, Analgesic and Anti-Inflammatory Activities

  • Kalyani G Department of Pharmaceutical Chemistry, TKR College of Pharmacy, Hyderabad, India
  • Srinivas Bethi Department of Pharmaceutical Chemistry, Talla Padmavathi College of Pharmacy, Warangal, India.
  • Sastry K V Department of Pharmaceutics, Alliance Institute of Advanced Pharmaceutical and Health Sciences, Hyderabad, India.
  • Vijaya Kuchana Department of Pharmaceutical Chemistry, TKR College of Pharmacy, Hyderabad, India
Keywords: Cinnoline, Mannich condensation, analgesic activity, anti-inflammatory, anti-bacterial.

Abstract

In the present study, we have designed and synthesized a series of novel cinnoline fused Mannich bases by the condensation reaction of 4-methyl-3-acetyl cinnoline with different secondary aromatic and aliphatic amines with and the structures of compounds were characterized by H1-NMR, IR and Mass spectral analysis. The biological potentials of the newly synthesized compounds are evaluated for their antibacterial activity against Staphylococcus aureus (Gram positive), and Eeshricia coli (Gram negative) bacteria, in vivo analgesic and anti-inflammatory activities. Compounds 4 and 3, which are having larger hydrophobic amino substitutions resulted in relatively higher antibacterial against S. aureus and E. coli when compared to streptomycin. Similarly, compound 4 reported higher analgesic activity when compared to diclofenac at 120 mins and 180 mins. From anti-inflammatory evaluations, dose level of 50 mg/kg of test compounds reported significantly higher activity when compared to dose level of 20 mg/kg. Moreover, compound 4 (50 mg/kg) resulted in similar anti-inflammatory activity when compared with celecoxib (20 mg/kg).
Published
2017-07-25