67579-92-4

Upstream product

• 5081-36-7 3-methoxy-4-nitrobenzoic acid 
• 79-37-8 oxalyl dichloride 
• 185629-31-6 methyl 3-fluoro-4-nitrobenzoate 
• 403-21-4 3-fluoro-4-nitrobenzoic acid 
• 38512-82-2 3-methoxy-4-nitrotoluene 
• 5081-37-8 methyl 3-methoxy-4-nitrobenzoate 

Downstream Products

• 92241-87-7 3-methoxy-4-nitrobenzamide 
• 123330-91-6 tert-Butyl 3-methoxy-4-nitrobenzoate 
• 90323-26-5 2-diazo-1-(3-methoxy-4-nitro-phenyl)-ethanone 
• 607713-39-3 2-[1-(3-methoxy-4-nitrophenyl)ethylidene]malononitrile 
• 607713-40-6 2-amino-4-(3-methoxy-4-nitrophenyl)-3-thiophenecarbonitrile 
• 607713-42-8 5-(4-amino-3-methoxyphenyl)thieno[2,3-d]pyrimidin-4-amine 
• 16292-88-9 3-methoxy-4-nitroanilin 
• 5081-36-7 3-methoxy-4-nitrobenzoic acid 
• 92241-91-3 2-methoxy-4-deuterioaniline 
• 92241-90-2 C₇H₆⁽²⁾HNO₃ 
• 870090-66-7 3-methoxy-4-nitro-N-(3-methanesulfonylamino-4-methoxyphenyl)benzamide 
• 457098-02-1 3-methoxy-4-nitro-benzoic acid (3S)-1-benzyl-pyrrolidin-3-yl ester 
• 851202-59-0 4-amino-3-methoxy-N-thiazol-2-ylbenzamide 
• 1233094-58-0 (3-methoxy-4-nitrophenyl)(4-methylpiperazin-1-yl)methanone 

Relevant academic research and scientific papers

Augmenting the Activity of Macrolide Adjuvants against Acinetobacter baumannii

Approximately 1.7 million Americans develop hospital associated infections each year, resulting in more than 98,000 deaths. One of the main contributors to such infections is the Gram-negative pathogen Acinetobacter baumannii. Recently, it was reported that aryl 2-aminoimidazole (2-AI) compounds potentiate macrolide antibiotics against a highly virulent strain of A. baumannii, AB5075. The two lead compounds in that report increased clarithromycin (CLR) potency against AB5075 by 16-fold, lowering the minimum inhibitory concentration (MIC) from 32 to 2 μg/mL at a concentration of 10 μM. Herein, we report a structure-activity relationship study of a panel of derivatives structurally inspired by the previously reported aryl 2-AI leads. Substitutions around the core phenyl ring yielded a lead that potentiates clarithromycin by 64- and 32-fold against AB5075 at 10 and 7.5 μM, exceeding the dose response of the original lead. Additional probing of the amide linker led to the discovery of two urea containing adjuvants that suppressed clarithromycin resistance in AB5075 by 64- and 128-fold at 7.5 μM. Finally, the originally reported adjuvant was tested for its ability to suppress the evolution of resistance to clarithromycin over the course of nine consecutive days. At 30 μM, the parent compound reduced the CLR MIC from 512 to 2 μg/mL, demonstrating that the original lead remained active against a more CLR resistant strain of AB5075.

Diphenyl-aminopyrimidine compound for inhibiting kinase activity

The invention relates to a diphenyl-aminopyrimidine compound with an inhibiting function on protein tyrosine kinase, a pharmaceutical composition containing the diphenyl-aminopyrimidine compound, andpreparation and application of the diphenyl-aminopyrimidine compound, in particular to a compound shown as the formula (I) and pharmaceutically acceptable salt or crystal forms or prodrugs or metabolin or aquo-complex or solvate or isotope derivatives thereof, wherein R1, R2, R5, R6, R7, R8 and W are defined as the description. The compound can be used for treating ALK-mediated cancer related symptoms, such as non-small cell lung cancer or breast cancer or neural tumors or esophagus cancer or soft tissue cancer or lymphoma or leukemia. The formula is shown in the specification.

Synthesis and Preliminary Evaluation of [11C]GNE-1023 as a Potent PET Probe for Imaging Leucine-Rich Repeat Kinase 2 (LRRK2) in Parkinson's Disease

Leucine-rich repeat kinase 2 (LRRK2) is a large protein involved in the pathogenesis of Parkinson's disease (PD). It has been demonstrated that PD is mainly conferred by LRRK2 mutations that bring about increased kinase activity. As a consequence, selecti

TYK2 INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

Heterocyclic Compounds and Methods of Use

This disclosure provides compounds and methods of using those compounds to treat liver fibrosis, including liver fibrosis which is a precursor to, is concurrent with, is associated with, or is secondary to nonalcoholic steatohepatitis (NASH); elevated cholesterol levels, and insulin resistance.

PYRIMIDOINDOLIZINE DERIVATIVES AS LEUCINE RICH REPEAT KINASE 2 INHIBITORS

The present invention relates to a pyrimidoindolizine derivative having leucine rich repeat kinase 2 (LRRK2) kinase inhibition activation, a manufacturing method thereof, and a composition for preventing or treating degenerative brain diseases including t

Total Synthesis and Biological Assessment of Novel Albicidins Discovered by Mass Spectrometric Networking

Natural products represent an important source of potential novel antimicrobial drug leads. Low production by microorganisms in cell culture often delays the structural elucidation or even prevents a timely discovery. Starting from the anti-Gram-negative antibacterial compound albicidin produced by Xanthomonas albilineans, we describe a bioactivity-guided approach combined with non-targeted tandem mass spectrometry and spectral (molecular) networking for the discovery of novel antimicrobial compounds. We report eight new natural albicidin derivatives, four of which bear a β-methoxy cyanoalanine or β-methoxy asparagine as the central α-amino acid. We present the total synthesis of these albicidins, which facilitated the unambiguous determination of the (2 S,3 R)-stereoconfiguration which is complemented by the assessment of the stereochemistry on antibacterial activity.

HETEROCYCLIC COMPOUNDS AND METHODS OF USE

This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists. Compounds of the invention may also find use in treating cancer. Presented herein are novel compounds bearing a perhaloalkylsulfonamide moiety. Such compounds, in addition to being highly effective SREBP inhibitors, are also unexpectedly highly bioavailable in vivo. Heteroaromatic compounds bearing sulfonamide groups are prone to several ionic states, based on the inherent pKa values.

HETEROCYCLIC COMPOUNDS AND METHODS OF USE

This disclosure provides compounds and methods of using those compounds to treat metabolic disorders and hyperproliferative disorders, including administration of the compounds in conjunction with hormone receptor antagonists.

Perturbation of the c-Myc-Max Protein-Protein Interaction via Synthetic α-Helix Mimetics

The rational design of inhibitors of the bHLH-ZIP oncoprotein c-Myc is hampered by a lack of structure in its monomeric state. We describe herein the design of novel, low-molecular-weight, synthetic α-helix mimetics that recognize helical c-Myc in its transcriptionally active coiled-coil structure in association with its obligate bHLH-ZIP partner Max. These compounds perturb the heterodimer's binding to its canonical E-box DNA sequence without causing protein-protein dissociation, heralding a new mechanistic class of "direct" c-Myc inhibitors. In addition to electrophoretic mobility shift assays, this model was corroborated by further biophysical methods, including NMR spectroscopy and surface plasmon resonance. Several compounds demonstrated a 2-fold or greater selectivity for c-Myc-Max heterodimers over Max-Max homodimers with IC50 values as low as 5.6 μM. Finally, these compounds inhibited the proliferation of c-Myc-expressing cell lines in a concentration-dependent manner that correlated with the loss of expression of a c-Myc-dependent reporter plasmid despite the fact that c-Myc-Max heterodimers remained intact. (Chemical Equation Presented).