132815-69-1

Upstream product

• 18804-77-8 ethyl 3-oxo-2-(p-tolylhydrazono)butanoate 
• 106-49-0 p-toluidine 
• 105-39-5 chloroacetic acid ethyl ester 
• 609-15-4 ethyl 2-chloro-3-oxo-butyrate 
• 2028-84-4 p-methylbenzenediazonium chloride 
• 56-23-5 tetrachloromethane 
• 7782-50-5 chlorine 

Downstream Products

• 144309-63-7 (4S,5R)-4-Benzo[1,3]dioxol-5-yl-5-(4-methoxy-benzoyl)-1-p-tolyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid ethyl ester 
• 121580-44-7 5-Oxo-4-p-tolyl-4,5-dihydro-benzo[f][1,3,4]thiadiazepine-2-carboxylic acid ethyl ester 
• 117620-62-9 5-Carbamoyl-1-p-tolyl-4,5-dihydro-1H-pyrazole-3-carboxylic acid ethyl ester 
• 63514-80-7 ethyl 4-acetyl-5-methyl-1-(p-tolyl)-1H-pyrazole-3-carboxylate 
• 204512-10-7 3-(p-Tolyl-hydrazono)-3,4-dihydro-1H-quinoxalin-2-one 
• 444902-79-8 ethyl 1-(4-methylphenyl)-7-phenyl-1,2,4-triazolo[4,3-a]-5(1H)-pyrimidinone-3-carboxylate 

Relevant academic research and scientific papers

Stereoselective synthesis of spiro and condensed pyrazolines of steroidal α,β-unsaturated ketones and nitrilimines by 1,3-dipolar cycloaddition

Effective syntheses of endo- and exocyclic α,β-unsaturated ketones as C{double bond, long}C dipolarophiles were carried out in the 13α-estrone series. The 1,3-dipolar cycloadditions of 15,16α,β-unsaturated ketones of 13α-estrone 3-methyl and 3-benzyl ethe

Design, synthesis and anti-tumor evaluation of 1,2,4-triazol-3-one derivatives and pyridazinone derivatives as novel CXCR2 antagonists

Chemokine receptor 2 (CXCR2) is the receptor of glutamic acid–leucine–arginine sequence-contained chemokines CXCs (ELR+ CXCs). In recent years, CXCR2-target treatment strategy has come a long way in cancer therapy. CXCR2 antagonists could block

Azologization of serotonin 5-HT3 receptor antagonists

The serotonin 5-hydroxytryptamine 3 receptor (5-HT3R) plays a unique role within the seven classes of the serotonin receptor family, as it represents the only ionotropic receptor, while the other six members are G protein-coupled receptors (GPCRs). The 5-HT3 receptor is related to chemo-/radiotherapy provoked emesis and dysfunction leads to neurodevelopmental disorders and psychopathologies. Since the development of the first serotonin receptor antagonist in the early 1990s, the range of highly selective and potent drugs expanded based on various chemical structures. Nevertheless, on-off-targeting of a pharmacophore’s activity with high spatiotemporal resolution as provided by photopharmacology remains an unsolved challenge bearing additionally the opportunity for detailed receptor examination. In the presented work, we summarize the synthesis, photochromic properties and in vitro characterization of azobenzene-based photochromic derivatives of published 5-HT3R antagonists. Despite reported proof of principle of direct azologization, only one of the investigated derivatives showed antagonistic activity lacking isomer specificity.

Bis-heterocycles. Part I: Tetrahydro-5,5′- bi(1,2,4-triazin-6-ones)

Selected sets of tetrahydro-5,5′-bi(1,2,4-triazines) (1-3) appended with acetyl, benzoyl, and ester moieties at C-3 position and N-1 (p-substituted)phenyl ring have been prepared and characterized by spectral (IR, NMR, MS) data and X-ray diffraction for c

TOLL-LIKE RECEPTOR ANTAGONIST COMPOUNDS AND METHODS OF USE

The invention relates to compounds of formula (I): or a salt or solvate thereof, wherein the variables are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are antagonists of toll-like receptors such as TLR7, TLR8 and/or TLR9 that are useful for inhibiting immune response and treating diseases associated with undesirable immune response.

Development of Pyridazinone Chemotypes Targeting the PDEδ Prenyl Binding Site

The K-Ras GTPase is a major target in anticancer drug discovery. However, direct interference with signaling by K-Ras has not led to clinically useful drugs yet. Correct localization and signaling by farnesylated K-Ras is regulated by the prenyl binding protein PDEδ. Interfering with binding of PDEδ to K-Ras by means of small molecules provides a novel opportunity to suppress oncogenic signaling. Here we describe the identification and structure-guided development of novel K-Ras–PDEδ inhibitor chemotypes based on pyrrolopyridazinones and pyrazolopyridazinones that bind to the farnesyl binding pocket of PDEδ with low nanomolar affinity. We delineate the structure–property relationship and in vivo pharmacokinetic (PK) and toxicokinetic (Tox) studies for pyrazolopyridazinone-based K-Ras–PDEδ inhibitors. These findings may inspire novel drug discovery efforts aimed at the development of drugs targeting oncogenic Ras.

Separation of PALMITIC acid from over used oil for production of heterogeneous organic derivatives of potential biological activities

PALMITIC acid was extracted from Over-used cooking oil where oil was filtered off, then it was hydrolyzed with distilled water in high pressure reactor at 250°C and 2 MPa to produce glycerol and mixture of fatty acids. Fatty acids mixture was cooled at 7°C in order to precipitate all saturated fatty acids, which were then filtered off, Palmitic acid was extracted from this mixture by means of supercritical CO2 extractor at 35.0 MPa and 55°C, followed by its methylation and confirmation by GC mass. Then it was used as precursor for production of a different heterocyclic compounds which were then tested for their antimicrobial activities. Thus the long-chain methyl palmitate was interacted with hydrazine hydrate to produce the corresponding acid hydrazide (2), and then it was treated with phenyl isothiocyanate, furnished the corresponding thiosemicarbazide 4. The later was reacted with ethyl chloro(arylhydrazono) acetate 5a-b in dimethylformamide, in the presence of triethylamine, afforded thiadiazole derivatives 7a-b. A solution of thiosemicarbazide 4 in ethanol was interacted with the a-haloketones 9 in the presence of triethylamine, produced the parallel thiadiazine 12. The structure elucidation of all synthesized compounds is based on the elemental analysis and spectral data (IR, 1H NMR, 13C NMR and MS).

Pyridazinones for the treatment of cancer

The present invention relates to novel substituted pyrrolo- and pyrazolopyridazinones, as well as pharmaceutical compositions containing at least one of these substituted pyrrolo- and pyrazolo- pyridazinones together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said novel substituted pyrrolo- and pyrazolo- pyridazinones are binding to the prenyl binding pocket of PDEδ and therefore, are useful for the prophylaxis and treatment of cancer by inhibition of the binding of PDEδ to K-Ras and of Ras signaling in cells.

Methyl 3-cyclopropyl-3-oxopropanoate in the synthesis of heterocycles having a cyclopropyl substituent

Reactions of methyl 3-cyclopropyl-3-oxopropanoate with chloroacetone and ammonia, benzaldehyde and ammonia, and benzoquinone gave, respectively, methyl 2-cyclopropyl-5-methyl-1H-pyrrole-3-carboxylate, dimethyl 2,6-dicyclopropyl-4- phenyl-1,4-dihydropyridi

PHENYLTHIOACETIC ACID DERIVATIVES AND USE THEREOF

The invention relates to novel phenylthioacetic acid derivatives of formula (I), to a method for the production thereof, to the use thereof for the treatment and/or prophylaxis of diseases, in addition to the use thereof in the production of medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prevention of cardiovascular diseases, in particular dyslipidaemia and arteriosclerosis. The compounds act as modulators for the PRAR-alpha receptor.