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Development of novel EDG3 antagonists using a 3D database search and their structure-activity relationships.
Because precise structural information on EDG receptors is not yet available, pharmacophore models were generated based on structural information for S1P using the rational drug design software Catalyst, and more potent antagonists, 2-alkylthiazolidine-4-carboxylic acid, were developed.
Synthesis and antibacterial activity of acylides (3-O-acyl-erythromycin derivatives): a novel class of macrolide antibiotics.
The 3-O-nitrophenylacetyl derivative TEA0777 showed significantly potent activity against not only erythromycin-susceptible Gram-positive pathogens but also inducibly macrolides-lincosamides-streptogramin B (MLS(B))-resistant Staphylococcus aureus and efflux-resistant Streptococcus pneumoniae.
Synthesis and antibacterial activity of a novel series of acylides: 3-O-(3-pyridyl)acetylerythromycin A derivatives.
A novel series of acylides, 3-O-(aryl)acetylerythromycin A derivatives, showed potent antibacterial activity against not only Gram-positive pathogens, including inducibly macrolide-lincosamide-streptogramin B (MLS(B))-resistant and efflux-resistant strains, but also Gram-negative pathogens, such as H. influenzae.
Photostability of Lycopene Dispersed in an Aqueous Solution
Results indicate that dissolved oxygen would also be involved in the photolysis of lycopene, and there was a proportional relationship between the degradation content of Lycopene and the consumption of dissolved oxygen.
Total synthesis of schizocommunin and revision of its structure.
After reinvestigating the spectral data for natural schizocommunin, the quinazolinone derivative (Z)-2 was synthesized as a revised structure for schizOCommunin and showed moderate antiproliferative activity.
Development of isomerization and cycloisomerization with use of a ruthenium hydride with N-heterocyclic carbene and its application to the synthesis of heterocycles.
A pure ruthenium hydride complex with N-heterocyclic carbene (NHC) ligand was efficiently generated from the reaction of a second-generation Grubbs ruthenium catalyst with vinyloxytrimethylsilane and