One-pot Synthesis Of Novel Derivatives Research Articles

Synthesis of bis chalcones and transformation into bis heterocyclic compounds with expected antimicrobial activity

One-pot synthesis of novel derivatives of bis-chalcones has been achieved by condensation of 1,4-diacetylbenzene with different aldehydes in basic media. The reaction of chalcone derivatives 3a,b with thioglycolic acid gives compounds 4a,b. This, when reacted with ethyl cyanoacetate in presence of ammonium acetate gives the corresponding cyanopyridine derivatives 5a,b. Furthermore, bis-chalcone 3a,b has been cyclized to pyrazole analogs by using 2,4-dinitrophenylhydrazine to give compounds 7a,b in good yields. All products have been characterized by IR, 1H and 13C NMR, and elemental analysis. The newly synthesised compounds have been screened for anti-bacterial activity.

Unsaturated carboxylic acids in the one-pot synthesis of novel derivatives of 3,4-dihydro-2H-thiopyran

Unsaturated carboxylic acids in the one-pot synthesis of novel derivatives of 3,4-dihydro-2H-thiopyran

A One-pot Synthesis of Novel Derivatives of Oxadiazine-4-thione, and its Antibacterial Activity, and Molecular Modeling Studies.

The synthesis of a novel series of oxadiazine-4-thione biological molecules was executed through the incorporation of the ortho-, meta-, and para-benzoyl isocyanates to the tetrabromophthalimide nucleus. A one-pot multicomponent methodology in a solvent-free microwave irradiation environment was employed to afford this series of oxadiazine-4-thione, deriving a comparison with the conventional method. Subsequently, the yielded derivatives were subjected to further biological assessment. The acquired results denoted that the one-pot procedure, which delivered products in a 2-4 min. interval, was more efficient in evaluation against the classical method, which consumed a 1-2:30 hr. interval. The application of the antibacterial analyses was subjected to all the compounds, resulting in molecules 6a and 6c demonstrating the highest activity regarding Aspergillus Favus; molecules 5b and 5c exhibiting an equivalent level of activity towards E-coli and Fusarium Moniliform; and molecules 4b, 4c, 5b, and 5c presenting an identical level of activity to the aforementioned derivatives involving Staphylococcus. Concluison: Molecular modeling studies by the MOE, the preceding antibacterial behavior was conducted to advocate the newly prepared compounds. Moreover, the spectroscopic approaches were exploited to verify and establish the structures and mechanisms of the synthesized derivatives' reactions.