Synthesis, Antimicrobial Activity and Docking Study of Some N3, N6‑diphenylpyridazine‑3,6‑diamine Derivatives as Dihydrofolate Reductase Inhibitors

  • Athar Javed Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Shoolini University, Solan, Himachal Pradesh, India.
  • Sameer Sapra Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Shoolini University, Solan, Himachal Pradesh, India.
  • Afroze Alam Department of Pharmaceutical Chemistry, Narayan Institute of Pharmacy, Gopal Narayan Singh University, Sasaram, Bihar, India.
Keywords: Antimicrobial activity, Biphenyl, Dihydrofolate reductase inhibitors, Docking study, Pyridazine analogs

Abstract

Objective: The present study focussed on the synthesis of pyridazine analogs to explore broad‑spectrum antimicrobial study. Since pyridazine analogs are not conventionally found in nature, and hence, its analogs are studied later. Materials and Methods: All the synthesized compounds were characterized by spectroscopic techniques, namely, UV, IR, 1HNMR, and mass spectrometry. Antimicrobial activity was screened by serial dilution method and absorbance was recorded using ELISA reader, subsequently minimum inhibitory concentrations were determined. Docking study was done into the active site of dihydrofolate reductase using Auto Dock 4.2. Results: The present investigation about synthesis, characterization, and biological studies of some new pyridazine analogs were carried out to obtain potent and pharmacologically active compounds. The free energy of binding was in the range of −5.12 to −8.97 kcal/mole. In silico study report was in good tune with laboratory experiments. Conclusions: Most of the compounds were moderate‑to‑good toward the antimicrobial activity. Compound AJ27 was found to be most active. Results of anti‑microbial activity establishes the importance of N3, N6‑diphenylpyridazine‑3,6‑diamine as the basic skeleton required for the antimicrobial activity.

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General synthetic scheme
Published
2019-02-01
How to Cite
1.
Javed A, Sapra S, Alam A. Synthesis, Antimicrobial Activity and Docking Study of Some N3, N6‑diphenylpyridazine‑3,6‑diamine Derivatives as Dihydrofolate Reductase Inhibitors. ijpi [Internet]. 1Feb.2019 [cited 29Feb.2020];8(3):138-44. Available from: http://jpionline.org/index.php/ijpi/article/view/267