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Abstract: A novel synthesis of 2,3-dihydro-4-pyridinones via the reaction of bisdemethoxycurcumin and primary amines or amine acetates is demonstrated. The structures of the products were established by elemental analysis and from mass, 1H and 13C NMR spectra. [Copyright &y& Elsevier]

Abstract: Dihydropyridones were prepared by microwave-assisted reaction between curcumin and primary amines or their acetates in the presence of Montmorillonite (K-10) as a catalyst. The reaction was complete within a few minutes and the yield depends on the amine used. [Copyright &y& Elsevier]

Abstract: Two series of five membered heterocyclic bis(1,3,4-oxadiazole) derivatives 2(a–h) and 3,5-bis(substituted)pyrazoles, isoxazoles 3(a,b,d–i), 4(a–c) were synthesized via oxidative cyclization of some diaroylhydrazones using chloramine-T and cyclocondensation reaction with hydrazine hydrate and hydroxylamine hydrochloride, respectively. The newly synthesized compounds were screened for antioxidant and anti-microbial activities. Compounds 2(b), 3(b), and 4(a) showed higher antioxidant activity at 10μg/ml while compounds 2(a), 3(a), 3(f), and 4(a) exhibited better anti-microbial activity at 100μg/ml compared with standard vitamin C and ciprofloxacin, respectively. Structures of newly synthesized compounds were confirmed by elemental analysis and spectral IR, 1H NMR, and 13C NMR data. [Copyright &y& Elsevier]

The Gaussian visible Continuous-wave (CW) laser beam propagation in three curcuminoids compounds has led to diffraction ring patterns. These patterns believed to be originated due to self-phase modulation. The study focuses on the effect of input power on the diffraction ring patterns. As a result of increasing input power each circular ring pattern flattened in the upper part due to the convection. These results are reproduced numerically using the Fresnel-Kirchhoff integral. It appears that each ring pattern evolve with time from circular to flattened ones. The thermal nonlinear refractive indexes of the curcuminoids are calculated based on diffraction ring patterns and the Z-scan technique. [ABSTRACT FROM AUTHOR]

A new class of steroids is being synthesized for its ability to prevent intratumoral androgen production by inhibiting the activity of CYP17 hydroxylase enzyme. The scheme involved the synthesis of chalcone derivative of pregnenolone 5 which was further modified to the corresponding biaryl-chalcone pregnenolone analogs 16 – 25 using Suzuki–Miyaura cross-coupling reaction. The synthesized compounds were tested for activity using human CYP17α hydroxylase expressed in Escherichia coli . Compounds 21 was the most active inhibitor in this series, with IC 50 values of 0.61 μM and selectivity profile of 88.7% inhibition of hydroxylase enzyme. Molecular docking study of 21 was performed and showed the hydrogen bonds and hydrophobic interaction with the amino acid residues of the active site of CYP17. [ABSTRACT FROM AUTHOR]

A new series of 17-( N -(arylimino)-5-pregnen-3β-ol derivatives 19–32 as well as carboxylate and acrylate analogues of pregnenolone 37–40 were synthesized and evaluated for their inhibitory activity against human CYP17 hydroxylase expressed in Escherichia coli . Compounds 32 and 37 were the most potent analogues in this series, showing inhibition activity with IC 50 = 2.11 and 1.29 μM, respectively. However, the analogue 37 revealed a better selectivity profile (83.21% inhibition of hydroxylase), which is a leading candidate for further development. Molecular docking study of 37 showed binding with the amino acid residues of CYP17 through hydrogen bonds and hydrophobic interaction. [ABSTRACT FROM AUTHOR]