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
Medicinal Chemistry
Title: Prediction of Theoretical Physicochemical Properties and One-Pot Synthesis of Bis-Azetidinones by [2+2] Ketene – Imine Cycloaddition in the Presence of Montmorillonite
Volume: 7 Issue: 4
Author(s): Ramakanth Pagadala, Jyotsna S. Meshram, Himani N. Chopde, Venkateshwarlu Jetti, Uppalaiah Kusampally and V. Udayini
Affiliation:
Keywords: Azomethine, microwave irradiation, zeolite, bis-azetidinone, antibacterial, antifungal activity, Lipinski, structure and activity relationship, antibacterial pharmacophores, Antimicrobial, Theoretical, Physicochemical
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.
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Pagadala Ramakanth, S. Meshram Jyotsna, N. Chopde Himani, Jetti Venkateshwarlu, Kusampally Uppalaiah and Udayini V., Prediction of Theoretical Physicochemical Properties and One-Pot Synthesis of Bis-Azetidinones by [2+2] Ketene – Imine Cycloaddition in the Presence of Montmorillonite, Medicinal Chemistry 2011; 7 (4) . https://dx.doi.org/10.2174/157340611796150897
DOI https://dx.doi.org/10.2174/157340611796150897 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
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Scope of the Thematic Issue: Correlation between structure and function is one of the important aspects of the success of anti-cancer compounds associated with their structure-activity interactions, physiology, biochemical, molecular, and genetic processes. Overcoming these obstacles is key to obtaining further insights into developments in rational drug design, bioorganic chemistry, ...read more
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