709649-72-9

Upstream product

• 1379401-47-4 C₁₀H₁₀N₂ 
• 1154383-44-4 (N-methyl)indole-4-carboxamide 
• 1196-69-6 1H-indole-5-carboxaldehyde 
• 74-89-5 methylamine 

Relevant academic research and scientific papers

Structure-Guided Identification of DNMT3B Inhibitors

Methyltransferase 3 beta (DNMT3B) inhibitors that interfere with cancer growth are emerging possibilities for treatment of melanoma. Herein we identify small molecule inhibitors of DNMT3B starting from a homology model based on a DNMT3A crystal structure.

Novel Terminal Bipheny-Based Diapophytoene Desaturases (CrtN) Inhibitors as Anti-MRSA/VISR/LRSA Agents with Reduced hERG Activity

CrtN has been identified as an attractive and druggable target for treating pigmented Staphylococcus aureus infections. More than 100 new compounds were synthesized, which target the overwhelming the defects of the CrtN inhibitor 1. Analogues 23a and 23b demonstrated a significant activity against pigmented S. aureus Newman and 13 MRSA strains (IC50 = 0.02-10.5 nM), along with lower hERG inhibition (IC50 > 30 μM, ～10-fold decrease in comparison with 1). Furthermore, 23a and 23b were confirmed to reduce the staphylococcal load in the kidney and heart in a mouse model with normal treatment deeper than pretreatment ones, comparable even with vancomycin and linezolid. Remarkably, 23a could strongly block the pigment biosynthesis of these nine multidrug-resistant MRSA strains, including excellent activity against LRSA strains and VISA strains in vivo, and all of which demonstrated that 23a has a huge potential against intractable MRSA, VISA, and LRSA issues as a therapeutic drug.

HETEROCYCLIC COMPOUNDS, METHODS OF MAKING THEM AND THEIR USE IN THERAPY

In part, the present invention is directed to antibacterial compounds of formula (I) wherein A is a bicyclic heteroaryl ring or a tricyclic ring and R2 is an heterocyclic residue; L is a bond, or L is alkyl, alkenyl or cycloalkyl.

Indole and indazole derivatives, for the treatment and prophylaxis of cerebral disorders, their preparation and their use

Compounds of formula (I) : [in which R1 and R2 are each hydrogen or various organic groups, pis 0, 1, 2 or 3, U is -CO- or -CH(OR3)- where R3 is hydrogen or a hydroxy-protecting group, V is an optionally unsaturated aliphatic hydrocarbon group and W is a nitrogen-containing group] are useful in the treatment and prophylaxis of dementia especially of the Alzheimer's type.