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The benzazole scaffolds are present in various therapeutic agents and have been recognized as the essential pharmacophore for diverse biological activities. These have generated interest and necessity to develop efficient synthetic methods of these privileged classes of compounds to generate new therapeutic leads for various diseases. The biological activities of the benzazoles and efforts towards their synthesis have been summarized in a few review articles. In view of these, the aim of this review is to provide an account of the developments that have taken place in the synthesis of biorelevant benzazoles under microwave irradiation as the application of microwave heating has long been recognized as a green chemistry tool for speedy generation of synthetic targets. Attention has been focused to those literature reports wherein the use of microwave irradiation is the key step in the formation of the heterocyclic ring system or in functionalization of the benzazole ring system to generate the essential pharmacophoric feature. The convenient and economic way to synthesize these privileged class of heterocycles through the use of microwave irradiation that would be beneficial for the drug discovery scientist to synthesize biologically active benzazoles and provide access to wide range of reactions for the synthesis of benzazoles constitute the theme of this review. Examples have been drawn wherein the use of microwave heating offers distinct advantage in terms of improved product yields and reduction of reaction time as compared to those observed for the synthesis under conventional heating.
Reduction of nitro compounds - Organic chemistry
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Microwave-assisted Organic Reaction Enhancement (MORE) has emerged as a new ‘lead’ in organic synthesis. During the studies we observed that microwave –assisted organic synthesis requires 2-4 min. of time whereas the conventional ones takes 4-6 hrs and often with poor yields. Hence, with an objective of reducing the reaction time, application of microwave technique has proved to be advantageous in case of synthesis of new benzofuran derivatives. The structures of synthesized derivatives emerged is confirmed by their IR, NMR and Mass spectra. The representative compounds synthesized with this route is further screened for anti-bacterial, analgesic, anti-inflammatory and ulcerogenic studies. In this study we have observed that the benzofuran derivatives are less ulcerogenic compared to phenyl butazone. The structural comparisons have revealed that the chloro substitution will increase the ulcerogenic toxicity.
Further, all the synthesized compounds were ..
ABSTRACT: We have carried out solid supported ,solvent free condition, microwave assisted rapid synthesis of 1- (2,5- substituted diphenyl)-1, 3, 4- oxadiazol -3(2H) - yl) ethanone (3a-3k) by cyclization of N'- (substituted phenyl methylidene) substituted benzohydrazide (2a-2k) in the presence of acetic anhydride and silica gel ( solid support) for 3-4 minutes by microwave irradiation giving excellent yield in short reaction time are notable advantages of this method. The structure elucidations of all the synthesized compounds have been accomplished by elemental analysis, IR, NMR and Mass spectroscopic method. The synthesized compounds (3a-3k) were screened in vitro for their antibacterial activities against S. aureus ( gram positive ) and E. coli ( gram negative ) by cup plate method . Some of the products of series were found to have quite good activities as compared to the standard drug streptomycin. The introduction of -F, -NO2, -Cl (electron withdrawing) group enhancing antibacterial activity