1Synthesis and QSAR analysis of 5-substituted (arylmethylene) pyridin-2-amine derivatives as potential antibacterials

Choudhari P.B.¹, Mulani A.K.², Bhatia M.S.³*, Ingale K.B.⁴, Bhatia N.M.^5
1Department of Pharmaceutical Chemistry, Bharati Vidyapeeth College of pharmacy,Near chitranagri, Kolhapur.416013
²Department of Pharmaceutical Chemistry, Bharati Vidyapeeth College of pharmacy,Near chitranagri, Kolhapur.416013
³Department of Pharmaceutical Chemistry, Bharati Vidyapeeth College of pharmacy,Near chitranagri, Kolhapur.416013
⁴Department of Pharmaceutical Chemistry, Bharati Vidyapeeth College of pharmacy,Near chitranagri, Kolhapur.416013
⁵Department of Pharmaceutical Chemistry, Bharati Vidyapeeth College of pharmacy,Near chitranagri, Kolhapur.416013
* Corresponding Author : manish_bhatia13@yahoo.co.in

Received : -     Accepted : -     Published : 15-06-2009
Volume : 1     Issue : 1       Pages : 1 - 9
Int J Drug Discov 1.1 (2009):1-9
DOI : http://dx.doi.org/10.9735/0975-4423.1.1.1-9

Keywords : QSAR, antibacterial, pyridin-2-amine, imines
Conflict of Interest : None declared

A series of 5-substituted (arylmethylene) pyridin-2-amine were synthesized by condensing various 5-substituted pyridyl-2-amines with various aromatic aldehydes. The structures of newly synthesized compounds were characterized by spectral and elemental analysis. All the compounds were screened for their antibacterial activities. The QSAR studies of were performed on MOE 2006.08 software. QSAR equation reveled that selected electronic, steric and liphophillic parameters have correlation with antibacterial activity. Best equations were selected on basis of correlation coefficient (r2) and predicitivity of equation. The frequent appearance of Log P and SMR terms in the QSAR equations is indicative of lipophilic and steric parameters are the prerequisites for molecules to exhibit activity against bacteria.

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