49839-35-2

Upstream product

• 100-02-7 4-nitro-phenol 
• 7693-46-1 4-Nitrophenyl chloroformate 
• 100-61-8 N-methylaniline 
• 92289-43-5 imidazole-1-carboxylic acid methylphenylamide 
• 4285-42-1 N-phenyl-N-methylcarbamoyl chloride 

Downstream Products

• 548763-89-9 methyl-phenyl-carbamic acid-(4-amino-phenyl ester) 

Relevant academic research and scientific papers

Synthesis, biological activities and docking studies of pleuromutilin derivatives with piperazinyl urea linkage

Antibiotics resistance is becoming increasingly common, involving almost all antibiotics on the market. Diseases caused by drug resistant bacteria, such as MRSA, have high mortality and negatively affect public health. The development of new drugs would be an effective means of solving this problem. Modifications based on bioactive natural products could greatly shorten drug development time and improve success rate. Pleuromutilin, a natural product from the basidiomycete bacterial species, is a promising antibiotic candidate. In this study, a series of novel pleuromutilin derivatives possessing piperazinyl urea linkage were efficiently synthesised, and their antibacterial activities and bactericidal properties were evaluated via MIC, MBC and Time-kill kinetics assays. The results showed that all compounds exhibited potent activities against tested strains, especially MRSA strains with MIC values as low as 0.125 μg/mL; 8 times lower than that of marketed antibiotic Tiamulin. Docking studies indicate substituted piperazinyl urea derivatives could provide hydrogen bonds and initiate π-π stacking between molecules and surrounding residues.

NOVEL COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME

The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) inhibitory activity, isomers thereof, or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions comprising the same, a method of treating disease using the composition, and methods for preparing the novel compounds. The novel compounds according to the present invention have histone deacetylase 6 (HDAC6) inhibitory activity, and are effective for the prevention or treatment of HDAC6-associated diseases, including cancer, inflammatory diseases, autoimmune diseases, neurological diseases and neurodegenerative disorders.

A new protocol for the formation of carbamates and thiocarbamates using carbamoyl imidazolium salts

Carbamoyl imidazolium salts are demonstrated to act as useful carbamoylation reagents, in reactions with alcohols, phenols, thiols and thiophenols to form carbamates and thiocarbamates under relatively mild conditions. The salts are stable and easily prepared from the corresponding amines using CDI.