882854-64-0

Upstream product

• 5960-69-0 2-acetylphenanthrene 
• 100-16-3 4-nitrophenylhydrazone 
• 1100051-52-2 C₂₄H₁₄F₃N₃O₂ 

Downstream Products

• 1092540-88-9 C₃₁H₂₇F₃N₄O₃ 
• 742112-33-0 2-amino-N-{4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}acetamide 
• 1148047-04-4 (N-{4-[5-(phenanthren-2-yl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl}sulfuric diamide) 
• 1148046-99-4 C₂₇H₂₁F₃N₄O 
• 1148046-97-2 C₃₀H₂₈F₃N₅O 
• 1148046-98-3 C₃₀H₂₈F₃N₅O 

Relevant academic research and scientific papers

Development of novel antibacterial agents against methicillin-resistant Staphylococcus aureus

Methicillin-resistant Staphylococcus aureus (MRSA) poses a serious threat to public health because of its resistance to multiple antibiotics most commonly used to treat infection. In this study, we report the unique ability of the cyclooxygenase-2 (COX-2) inhibitor celecoxib to kill Staphylococcus aureus and MRSA with modest potency. We hypothesize that the anti-Staphylococcus activity of celecoxib could be pharmacologically exploited to develop novel anti-MRSA agents with a distinct mechanism. Examination of an in-house, celecoxib-based focused compound library in conjunction with structural modifications led to the identification of compound 46 as the lead agent with high antibacterial potency against a panel of Staphylococcus pathogens and different strains of MRSA. Moreover, this killing effect is bacteria-specific, as human cancer cells are resistant to 46. In addition, a single intraperitoneal administration of compound 46 at 30 mg/kg improved the survival of MRSA-infected C57BL/6 mice. In light of its high potency in eradicating MRSA in vitro and its in vivo activity, compound 46 and its analogues warrant continued preclinical development as a potential therapeutic intervention against MRSA.

ANTI-INFECTIVE AGENTS AGAINST INTRACELLULAR PATHOGENS

A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R′ is L-Lys, D-Lys, β-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2

PDK-1/AKT SIGNALING INHIBITORS

A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula (I): wherein X is selected from the group consisting of alkyl and haloalkyl; Ar is an aryl radical selected from the group consisting of phenyl, biphenyl, naphthyl, anthryl,