Prediction of Theoretical Physicochemical Properties and One-Pot Synthesis of Bis-Azetidinones by [2+2] Ketene – Imine Cycloaddition in the Presence of Montmorillonite

Author(s): Ramakanth Pagadala, Jyotsna S. Meshram, Himani N. Chopde, Venkateshwarlu Jetti, Uppalaiah Kusampally, V. Udayini.

Journal Name: Medicinal Chemistry

Volume 7 , Issue 4 , 2011

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Abstract:

A simple, highly efficient and environmentally friendly microwave accelerated one-pot synthesis of a series of differently substituted bis-azetidinones have been synthesized expeditiously in good yields from 1,2-diaminoethane and aromatic aldehydes in the presence of zeolite. The structures of the newly synthesized compounds were confirmed by IR, NMR, and mass spectra. The design and calculated molecular properties of all the reported compounds are on the basis of hypothetical antibacterial pharmacophores, which were formulated to interact with microorganisms. A correlation of structure and activity relationship of these compounds with respect to Lipinski rules and drug likeness properties of drugs are described and verified experimentally.

Keywords: Azomethine, microwave irradiation, zeolite, bis-azetidinone, antibacterial, antifungal activity, Lipinski, structure and activity relationship, antibacterial pharmacophores, Antimicrobial, Theoretical, Physicochemical

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Article Details

VOLUME: 7
ISSUE: 4
Year: 2011
Page: [325 - 332]
Pages: 8
DOI: 10.2174/157340611796150897
Price: $58

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