77206-97-4

Upstream product

• 394-02-5 5-fluoro-2-nitrobenzoyl chloride 
• 455-38-9 3-fluorobenzoic acid 
• 320-98-9 5-fluoro-2-nitrobenzoic acid 

Downstream Products

• 421558-77-2 2-nitro-5-(piperidin-1-yl)benzamide 
• 371945-79-8 6-fluoro-2-phenyl-3H,4H-quinazolin-4-one 
• 1241234-79-6 6-fluoro-2-(3-fluorophenyl)-4-quinazolinone 
• 885277-09-8 C₁₄H₈ClFN₂ 
• 1272776-34-7 C₁₄H₇ClF₂N₂ 
• 1304764-83-7 4-anilino-6-fluoro-2-phenylquinazoline 
• 1304764-85-9 4-anilino-6-fluoro-2-(3-fluorophenyl)quinazoline 
• 1304764-87-1 6-fluoro-2-(3-fluorophenyl)-4-(4-methoxyanilino)quinazoline 
• 1304764-89-3 6-fluoro-2-(3-fluorophenyl)-4-(3-methoxyanilino)quinazoline 
• 1304764-91-7 6-fluoro-2-(3-fluorophenyl)-4-(2-methoxyanilino)quinazoline 
• 1304764-93-9 6-fluoro-2-(3-fluorophenyl)-4-(4-fluoroanilino)quinazoline 
• 1304764-95-1 6-fluoro-2-(3-fluorophenyl)-4-(3-fluoroanilino)quinazoline 
• 1304764-97-3 6-fluoro-2-(3-fluorophenyl)-4-(2-fluoroanilino)quinazoline 
• 1304764-99-5 6-fluoro-2-(3-fluorophenyl)-4-(4-chloroanilino)quinazoline 

Relevant academic research and scientific papers

2-((3,5-Dinitrobenzyl)thio)quinazolinones: Potent Antimycobacterial Agents Activated by Deazaflavin (F420)-Dependent Nitroreductase (Ddn)

Swapping the substituents in positions 2 and 4 of the previously synthesized but yet undisclosed 5-cyano-4-(methylthio)-2-arylpyrimidin-6-ones 4, ring closure, and further optimization led to the identification of the potent antitubercular 2-thio-substituted quinazolinone 26. Structure-activity relationship (SAR) studies indicated a crucial role for both meta-nitro substituents for antitubercular activity, while the introduction of polar substituents on the quinazolinone core allowed reduction of bovine serum albumin (BSA) binding (63c, 63d). While most of the tested quinazolinones exhibited no cytotoxicity against MRC-5, the most potent compound 26 was found to be mutagenic via the Ames test. This analogue exhibited moderate inhibitory potency against Mycobacterium tuberculosis thymidylate kinase, the target of the 3-cyanopyridones that lies at the basis of the current analogues, indicating that the whole-cell antimycobacterial activity of the present S-substituted thioquinazolinones is likely due to modulation of alternative or additional targets. Diminished antimycobacterial activity was observed against mutants affected in cofactor F420 biosynthesis (fbiC), cofactor reduction (fgd), or deazaflavin-dependent nitroreductase activity (rv3547), indicating that reductive activation of the 3,5-dinitrobenzyl analogues is key to antimycobacterial activity.

SUBSTITUTED QUINAZOLINONE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR4

The present invention relates to novel quinazolinone derivatives of formula (I) as well as pharmaceutical compositions containing these compounds. The compounds of formula (I) as provided herein can act as positive allosteric modulators of metabotropic glutamate receptor subtype 4 (mGluR4), and can thus be used as therapeutic agents, particularly in the treatment or prevention of conditions associated with altered glutamatergic signalling and/or functions or conditions which can be affected by alteration of glutamate level or signalling.

TETRAHYDROISOQUINOLIN-2-YL-(QUINAZOLIN-4-YL) METHANONE COMPOUNDS AS CANCER CELL GROWTH INHIBITORS

Tetrahydroisoquinolin-2-yl-(quinazolin-4-yl)methanone derivatives represented by formula (I), pharmacologically acceptable salts thereof, and compositions containing such compounds are described. Methods for treating hyperproliferative disorders by administering the compounds are also described. 1,2,3,4-tetrahydroisoquinoline derivatives for making tetrahydroisoquinolin-2-yl-(quinazolin-4-yl)methanone compounds are also described.

The synthesized novel fluorinated compound (LJJ-10) induces death receptor- and mitochondria-dependent apoptotic cell death in the human osteogenic sarcoma U-2 OS cells

We designed the 6-fluoro-2-(3-fluorophenyl)-4-substituted anilinoquinazoline derivatives as less toxic anti-cancer candidates. Our result demonstrated that LJJ-10 has greater cytotoxicity than that of the other compounds in human osteogenic sarcoma U-2 OS cells. LJJ-10-induced apoptosis was associated with enhancing ROS generation, DNA damage, and an increase of the protein levels of Fas, FasL, FADD, caspase-8, cytochrome c, Apaf-1, AIF, Endo G, caspase-9 and caspase-3 in U-2 OS cells. LJJ-10-triggered growth inhibition was significantly attenuated by N-acetylcysteine, cyclosporine A, anti-FasL monoclonal antibody, and caspase-8, -9 and -3 specific inhibitors in U-2 OS cells. We suggest that LJJ-10-induced apoptotic cell death in U-2 OS cells through death receptor- and mitochondria-dependent apoptotic signaling pathways.

HOMOGENEOUS TIME RESOLVED FLUORESCENCE BASED TEST SYSTEM

The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the HIV gp41 six-helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN36 (SEQ ID NO:1); a second helical polypeptide consisting essentially of the sequence of C34 (SEQ ID NO: 2) wherein said IQN36 is labeled with a light emitting fluorophore and said C34 is labeled with an ultra-violet excitable fluorophore.

Small Molecule Inhibitors of Toll-Like Receptor 9

Small molecule compounds and compositions containing said compounds useful for inhibiting signaling by certain Toll-like receptors (TLRs), particularly TLR9, are provided. The compounds and compositions can be used to inhibit immune responses, including unwanted immune responses in particular. Compounds, compositions, and methods are provided to treat a variety of conditions involving unwanted immune responses, including for example autoimmune disease, inflammation, transplant rejection, and sepsis.

PHENYL-SUBSTITUTED QUINOLINE AND QUINAZOLINE COMPOUNDS FOR THE TREATMENT OF DIABETES

The invention relates to 2-phenyl-substituted quinoline and quinazoline compounds, pharmaceutical compositions, and methods for treating diabetes and related disorders.

BENZOTRIAZEPINONE DERIVATIVES

The present invention is concerned with benzotriazepinone derivatives, their intermediates, uses thereof and processes for their production. In particular, the present invention relates to parathyroid hormone (PTH) and parathyroid hormone related protein (PTHrp) receptor ligands, (PTH-l or PTH/PTHrp receptor ligands). The invention also relates to methods of preparing such ligands and to compounds which are useful as intermediates in such methods.

AMINOALCOHOL DERIVATIVES

The present invention relates to a compound formula[I]: wherein X is bond or -O-, R1 is formula[A] or formula [B] in which R5, R6 and R7 are each as defined in the description, R2 is hydrogen or lower alkyl, R3 is hydrogen or an amino protective group , R4 is formula[C], [D] or [E] in which R8, R9, R10, R11, R12, R13 and R16are each as defined in the description, and R14 and R15 are each independently hydrogen or lower alkyl, or a prodrug thereof or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of overactive bladder, micturiation disorder and the like.