A simple, practical, and efficient approach to synthesize new series of 2-(3-(2,4-dichlorophenoxy)-2-(4-(dimethylamino)phenyl)-4-oxoazetidin-1-ylamino)-N-arylacetamide by Staudinger [2 + 2] cycloaddition reaction. The titled compounds were evaluated for their antibacterial and antifungal activity against eight microorganisms. All the newly synthesized compounds are characterized by IR, 1 H-NMR, and mass spectroscopic data.

magnified imageN‐Benzylidene‐4‐(phenyldiazenyl)aniline (Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ii, Ij) has been prepared from p‐aminoazobenzene with different aromatic aldehydes under microwave irradiation, which on further treatment with chloro acetic acid and POCl3 in the presence of triethyl amine gave the title compounds. The structure of the compounds has been confirmed by spectroscopic techniques (IR and 1H NMR) and elemental analysis. These azetidinones analogues were screened for their antimicrobial activities against strains of different microorganisms. Some of the compounds displayed the promising antibacterial activities against some bacterial strains. J. Heterocyclic Chem., (2010).

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.

With the aim of synthesizing new heterocyclic compounds and exploring biological potency, new series of chalcones, that is, 3-(2-hydroxy-5-(aryl-diazenyl)phenyl)-1-(aryl)prop-2-en-1-one and their pyrimidine derivatives, that is, 4-(2-hydroxy-5-(aryl-diazenyl)phenyl)-6-(aryl)pyrimidin-2-ols were synthesized using different aromatic amines and salicylaldehyde as starting moieties. The structures of newly synthesized compounds were confirmed using different spectroscopic techniques such as IR, 1H-NMR, 13C-NMR, and mass spectral analysis, and elemental analysis. The newly synthesized pyrimidines derivatives were screened for their in vitro antibacterial and antifungal activities. It was observed that some of the newly synthesized compounds had shown promising activity against several bacterial and fungal stains. Anti-bacterial activity and anti-fungal activity studies revealed that pyrimidine derivatives consisting of nitro group in their molecular structure possess better activity than their corresponding chalcones.

Abstract:In the present communication, we herein report the synthesis of some novel derivatives of coumarin i.e. 3-((2E)-(3-(2-hydroxy-5-((aryl)diazenyl)phenyl)acryloyl)-2H-chromen-2-one (2a-2g). Various aromatic amines and salicylaldehyde in the presence of sodium nitrite and conc. HCl yielded 2-hydroxy-5-((aryl)diazenyl)benzaldehyde (1a-1g). A series of 3-((2E)-(3-(2-hydroxy-5-((aryl)diazenyl) phenyl)acryloyl)-2H-chromen-2-one were synthesized by the reaction of 2-hydroxy-5-((aryl)diazenyl) benzaldehyde and coumarin in presence of ethanol and piperidine. Different analytical techniques such as elemental analysis, IR spectra, 1 H NMR spectra and mass spectra were used to elucidate the structures of all newly synthesized compounds (1a-1g and 2a-2g). The anti-bacterial and anti-fungal activity of newly synthesized chalcone derivatives (2a-2g) were evaluated against different bacterial and fungal stains. Some of these compounds showed promising activity against different stains.