Some Novel Dinuclear phenylboronates of biologically potent β-enaminoesters: Synthesis, Spectroscopic characterization, antimicrobial activity and their antiandrogenic effect

Organoboron derivatives of biologically potent beta-enamino esters of the type [Where R = CH3(1a), C2H5 (1b), C3H7(1c) and C (CH3)(3) (1d)] have been prepared by the reactions of beta-enamino esters and Phenyl boronic acid [PhB (OH)(2)] in 1:2 molar ratio in refluxing tetrahydrofuran (THF). All these derivatives have been characterized by physico-chemical properties, elemental analyses and molecular weight measurements. The structures of these compounds have been proposed on the basis of IR, H-1, C-13, B-11 NMR spectral data and GC-mass spectrometry. Phenyl boronic acid, beta-enamino esters and their respective phenylboronates derivatives have been screened for the antibmicrobial activities against pathogenic bacteria (B. subtilis and E. coli) and fungi (A. niger and P. peniculosum) to access their growth inhibiting potential. In addition to this, antiandrogenic effect of Ligand, (LH2)-H-a and its boron derivative (1a) has also been tested in male albino rats.