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Upstream product

• 766-40-5 Mucochloric acid 
• 71-43-2 benzene 
• 87-56-9 mucochloric acid 
• 57697-64-0 mucochloric acid 

Downstream Products

• 67052-07-7 (Z)-2,3-Dichloro-4-phenyl-4-p-tolyl-but-2-enoic acid 
• 33389-38-7 5-chloro-2-methyl-6-phenylpyridazin-3(2H)-one 
• 132814-16-5 6-phenyl-5-(N¹-piperazinyl)-2H-pyridazin-3-one 
• 132814-12-1 6-phenyl-5-(N⁴-benzoyl-N¹-piperazinyl)-2H-pyridazin-3-one 
• 132814-13-2 6-phenyl-5-(N⁴-(2-furoyl)-N¹-piperazinyl)-2H-pyridazin-3-one 
• 87769-63-9 5-amino-6-phenyl-1,6-dihydropyridazin-3(2H)-one 
• 23066-93-5 3,4-dichloro-5-methoxy-2-(5H)furanone 
• 1610354-27-2 1-((3S,4R)-4-(3,4-difluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(6-oxo-3-phenyl-1-(2,2,2-trifluoroethyl)-1,6-dihydropyridazin-4-yl)urea 
• 1610354-26-1 1-((3S,4R)-4-(3,4-difluorophenyl)-1-(2-methoxyethyl)pyrrolidin-3-yl)-3-(1-methyl-6-oxo-3-phenyl-1,6-dihydropyridazin-4-yl)urea 
• 1610354-61-4 5-amino-6-phenyl-2-(2,2,2-trifluoroethyl)pyridazin-3(2H)-one 
• 1610354-60-3 5-azido-6-phenyl-2-(2,2,2-trifluoroethyl)pyridazin-3(2H)-one 
• 1610354-59-0 phenyl 1-methyl-6-oxo-3-phenyl-1,6-dihydropyridazin-4-ylcarbamate 
• 126336-94-5 5-amino-2-methyl-6-phenylpyridazin-3(2H)-one 
• 126337-06-2 5-azido-2-methyl-6-phenylpyridazin-3(2H)-one 

Relevant academic research and scientific papers

N-substituted 5-chloro-6-phenylpyridazin-3(2H)-ones: Synthesis, insecticidal activity against Plutella xylostella (L.) and SAR study

A series of N-substituted 5-chloro-6-phenylpyridazin-3(2H)-one derivatives were synthesized based on our previous work; all compounds were characterized by spectral data and tested for in vitro insecticidal activity against Plutella xylostella. The result

Cholecystokinin-1 receptor antagonists: 5-hydroxy-5-aryl-pyrrol-2-ones as anticancer agents

A new class of 5-arylated 5-hydroxypyrrolones was derived from mucochloric acid in 2 synthetic steps and the chemical structure was confirmed additionally by X-ray analysis. Using a radiolabelled binding assay, potent CCK1 selective ligands were identified (CCK1: 12 nM) and the antagonism was confirmed by using isolated tissue preparations. A series of isobutyl derivatives displayed unsurmountable CCK antagonistic properties and in vitro excellent inhibition of proliferation was obtained in cholecystokinin related cancer cell lines in the nanomolar range. Finally, using xenograft studies in nude mice, two selected pyrrolone derivatives, X = H and X = F a fluorinated analogue (PNB-028), showed a strong inhibition of tumour growth in a chemo-resistant colon cancer-(MAC 16) and a human pancreatic cell line (MIAPACA) at 50 mg kg-1 by oral administration.

Design, synthesis, and In vitro antituberculosis activity of 2(5H)-Furanone derivatives

A series of 2(5H)-furanone-based compounds were synthesized from commercially available mucohalic acids. From the first-generation compounds, three showed inhibitory activity (10 μg/mL) of at least 35% against Mycobacterium smegmatis mc2 155 growth (Bioscreen C system). In screening the active first-generation compounds for growth inhibition against Mycobacterium tuberculosis H37Rv, the most active compound was identified with a minimum inhibitory concentration (MIC99) of 8.07 μg/mL (15.8 μM) using BACTEC 460 system. No cross-resistance was observed with some current first-line anti-TB drugs, since it similarly inhibited the growth of multidrug resistant (MDR) clinical isolates. The compound showed a good selectivity for mycobacteria since it did not inhibit the growth of selected Gram-positive and Gram-negative bacteria. It also showed synergistic activity with rifampicin (RIF) and additive activity with isoniazid (INH) and ethambutol (EMB). Additional time-kill studies showed that the compound is bacteriostatic to mycobacteria, but cytotoxic to the Chinese Hamster Ovarian (CHO) cell line. From a second generation library, two compounds showed improved anti-TB activity against M. tuberculosis H37Rv and decreased CHO cell cytotoxicity. The compounds exhibited MIC values of 2.62 μg/mL (5.6 μM) and 3.07 μg/mL (5.6 μM) respectively. The improved cytotoxicity against CHO cell line of the two compounds ranged from IC50 = 38.24 μg/mL to IC50 = 45.58 μg/mL when compared to the most active first-generation compound (IC50 = 1.82 μg/mL). The two second generation leads with selectivity indices (SI) of 14.64 and 14.85 respectively, warrant further development as anti-TB drug candidates.

Cholecystokinin-2/gastrin antagonists: 5-hydroxy-5-aryl-pyrrol-2-ones as anti-inflammatory analgesics for the treatment of inflammatory bowel disease

Arylated 5-hydroxy-pyrrol-2-ones were prepared in 2 synthetic steps from mucochloric acid and optimised as CCK2-selective ligands using radiolabelled binding assays. CCK antagonism was confirmed for the ligands in isolated tissue preparations.

COMPOSITIONS AND METHODS FOR VIRAL SENSITIZATION

Provided are compounds that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the antigen expression from a virus, gene or trans-gene expression from a virus, or virus protein expression in cells. Other uses, compositions and methods of using same are also provided.

Ureido-Pyridazinone Derivatives: Insights into the Structural and Conformational Properties for STAT3 Inhibition

Three new ureido-pyridazinone derivatives, which are structurally related to the known STAT3 inhibitor AVS-0288, were designed by taking into account the structure-activity relationships determined for several ureido-oxadiazole derivatives previously studied by our group. Their synthesis was first attempted through suitable 5-aminopyridazinone intermediates (6a and 6b), which molecular structures were confirmed by means of X-ray diffraction data on 6a. Amine functionalization was unsuccessful, therefore, an alternative method was devised. Dual-luciferase and AlphaScreen-based assays were used to test their activity. The obtained data were rationalized on the basis of a modeling study, which focused our attention on the geometrical preferences of the ureido moiety. Computational results seem to indicate that both the 1,2,5-oxadiazole ring and the extended ZZ arrangement are essential and probably act in a synergistic way to confer significant activity against STAT3.

PYRROLIDINYL UREA, THIOUREA, GUANIDINE AND CYANOGUANIDINE COMPOUNDS AS TRKA KINASE INHIBITORS

Compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Ring B, and Ring C are as defined herein, and wherein Ring B moiety and the NH-C(=X)-NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.

NOVEL CHOLECYSTOKININ RECEPTOR LIGANDS

The present invention relates to novel compounds of formula (I): wherein X is selected from hydrogen, a halogen, or a substituent and R is selected from hydrogen, a halogen, phenyl, aryl as specified and Y is selected from H, hydroxy, as specified and Rs

Synthesis and antifungal activity of 5-chloro-6-phenyl- pyridazin-3(2H)-one derivatives

An effective method has been developed for the preparation under mild conditions of novel pyridazine derivatives from the easily accessible starting materials mucochloric acid and benzene. All the synthesized compounds were fully characterized and some of

NOVEL 4-AMINO-2(5H)-FURANONES

The present invention relates to compounds of formula (I): wherein X is selected from hydrogen, a halogen, a substituted or unsubstituted cyclic and heterocyclic moiety, substituted or unsubstituted, linear or branched alkyl, alkyloxy, alkylcarbonyl, alky