Quercetin-pivaloxymethyl conjugate (Q-POM) potentiated the activity of ampicillin, cefepime, and vancomycin against S. aureus and Enterococcus (including highly resistant strains such as hVISA, VISA, and VRE), by decreasing the MICs of these antibiotics by 4-128 folds. Q-POM was found to be partially synergistic with ampicillin and cefepime against S. aureus and Enterococcus, while it was strongly synergistic with vancomycin. Q-POM at 5 mg/L inhibited the formation of biofilms of S. aureus by 24-83% and VRE by 70%. Additionally, Q-POM inhibited the hemolytic activity of S. aureus in a dose-dependent manner.
Metal carbenoid species are known to insert into a C−H bond, C=X double bonds (X = C, N, O), and Y−H bonds (Y = N, O, Si, P, S, etc), however, a carbenoid insertion into a urea C−N bond has not yet been reported. In the article, the first urea insertion reaction of carbenoid species is described. The urea insertion reaction proceeded smoothly using Rh2(NHPiv)4, a rhodium catalyst previously designed by the authors’ group, to produce highly functionalized bridged molecules with three adjacent stereocenters.
Primary drying conditions for the commercial manufacturing were designed based on the vial heat transfer coefficient of the production lyophilizer and the drying resistance (Rp) calculated from manufacture with the pilot lyophilizer under dust-free condition. The production scale-verification study confirmed that the Rp obtained using pilot lyophilizer under dust-free condition could be available for the production lyophilizer. This scale-up theory, which bridges the gap between the laboratory scale and the production scale, is useful for the development of an efficient and robust process at production scale.
New Cannabinoid-Like Chromane and Chromene Derivatives from Rhododendron anthopogonoides
Released: November 01, 2011 | Volume 59 Issue 11 Pages 1409-1412
Naoki Iwata, Susumu Kitanaka
Synthesis and Biological Evaluation of FTY720 (Fingolimod) Derivatives with Aromatic Head Group as Anticancer Agents
Released: October 01, 2018 | Volume 66 Issue 10 Pages 1015-1018
Taeho Lee, Hong Seop Moon, Seon Woong Kim, Jitendra Shrestha, Sang Mi Shin, Joo-Youn Lee, Sanghee Kim, Eun-Young Park, Dong Jae Baek