Chang Yong Hong

5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents

5-Arylamino-2-methyl-4,7-dioxobenzothiazoles were synthesized as inhibitors of cyclin-dependent kinase 4 (CDK4) and cytotoxic agents. Most of the 4,7-dioxobenzothiazoles exhibited selective inhibitory activities for the CDK4 and cytotoxic potential against human cancer cell lines.

Methyloxime-substituted aminopyrrolidine: A new surrogate for 7-basic group of quinolone

Novel fluoroquinolones containing oxime functionalized aminopyrrolidines have been synthesized. They were found to possess potent antibacterial activities against both Gram-negative and Gram-positive organisms, including methicillin resistant Staphylococcus aureus (MRSA). Among these compounds, LB20277 (compound 12) showed the most favorable in vivo efficacy and pharmacokinetic profile in animals. Based on these promising results, LB20277 was selected as a candidate for further evaluation.

Novel 5-amino-6-methylquinolone antibacterials: A new class of non-6-fluoroquinolones☆

Abstract A novel 5-amino-6-methylquinoline carboxylic acid was synthesized from 2,3,4-trifluoro aniline in 12 steps and coupled with various types of amines to furnish new quinolone antibacterial agents. Depending on the structure of amine, some of quinolones showed comparable activity to ciprofloxacin or better Gram positive activity than ciprofloxacin, demonstrating that the C6 fluorine atom is not a necessary requirement for good antibacterial potency.