52240-00-3

Upstream product

• 87702-21-4 4-(thien-2-yl)-4-oxobutyric acid methyl ester 
• 4653-08-1 4-oxo-4-thiophen-2-yl-butyric acid 

Downstream Products

• 54558-07-5 6-(thien-2-yl)-2,3-dihydropyridazin-3-one 
• 75792-87-9 3-hydrazino-6-thien-2-ylpyridazine 
• 28657-41-2 3-chloro-6-(2'-thienyl)pyridazine 
• 78490-15-0 (bromo-5 thienyl-2)-6 tetrazolo<1,5-b>pyridazine 
• 1444311-31-2 ethyl 2-[5-(4-methoxybenzyl)-6-oxo-3-(thiophen-2-yl)pyridazin-1(6H)-yl]acetate 
• 1444311-32-3 ethyl 2-[5-(3-methoxybenzyl)-6-oxo-3-(thiophen-2-yl)pyridazin-1(6H)-yl]acetate 
• 1444311-47-0 2-[5-(4-methoxybenzyl)-6-oxo-3-(thiophen-2-yl)pyridazin-1(6H)-yl]acetic acid 
• 1444311-48-1 2-[5-(3-methoxybenzyl)-6-oxo-3-(thiophen-2-yl)pyridazin-1(6H)-yl]acetic acid 
• 1444311-20-9 4-(3-methoxybenzyl)-6-(thiophen-2-yl)pyridazin-3(2H)-one 
• 123716-48-3 4-(4-methoxybenzyl)-6-(thiophen-2-yl)pyridazin-3(2H)-one 

Relevant academic research and scientific papers

Synthesis, anti-convulsant activity and molecular docking study of novel thiazole pyridazinone hybrid analogues

Pyridazinone analogues have been known to be potential candidates for anticonvulsant agents. We have identified several pyridazinone-based anticonvulsant agents. As a continuation to our previous research, a series of hybrid pyridazinone-thiazole connected through amide linkage were designed and synthesized. Among these, compound SP-5F demonstrated significant anticonvulsant activity with median effective dose of 24.38 mg/kg (MES) and 88.23 mg/kg (scPTz). Results of GABA estimation showed a marked increase in the GABA level when compared with control. Molecular docking studies at the active site of GABA receptor, further confirmed the GABA modulatory effects of SP-5F.

Design, Synthesis, and Pharmacological Screening of Pyridazinone Hybrids as Anticonvulsant Agents

A series of new hybrid benzimidazole containing pyridazinones derivatives were designed and synthesized in accordance with the pharmacophoric requirements essential for the anticonvulsant activity. The synthesized compounds were evaluated for anticonvulsant activity on mice by the gold standard maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ)-induced seizure models. Among the compounds tested, SS-4F showed significant anticonvulsant activity in both the screens with ED50 values of 25.10 and 85.33 mg/kg in the MES and scPTZ screens, respectively. Compound SS-4F emerged as safer and effective anticonvulsant due to its several-fold higher protective indices. Further, the gamma-aminobutyric acid (GABA) estimation result showed a marked increase in the GABA level (1.7-fold) as compared to the control, which was further confirmed by good binding properties with the GABAA receptor.

Further studies on 2-arylacetamide pyridazin-3(2H)-ones: Design, synthesis and evaluation of 4,6-disubstituted analogs as formyl peptide receptors (FPRs) agonists

Formyl peptide receptors (FPRs) play an essential role in the regulation of endogenous inflammation and immunity. In the present studies, a large series of pyridazin-3(2H)-one derivatives bearing an arylacetamide chain at position 2 was synthesized and te

Syntheses and antiinflammatory activity of some 6-aryl-2,3,4,5-tetrahydro-3-pyridazinones

6-Aryl-2, 3, 4, 5-tetrahydro-3-pyridazinones (2c-22c) are obtained by dehydrocyclisation of various hydrazides formed by the reaction of appropriate methyl β-aroylpropionate and hydrazine hydrate in the presence of anhydrous sodium acetate. They show promising antiinflammatory activity during their evaluation by carrageenin induced paw edema test in rats.

Endothelin receptor antagonists

This invention relates to pyridizinone derivatives of formula I STR1 wherein the various substituents are defined in the specification, and salts thereof, which have useful pharmacological properties, in particular endothelin receptor-antagonistic properties. The compounds are thus useful for the treatment of illnesses associated with endothelin activities, such as hypertension, cardiac insufficiency, coronary heart disease, renal, cerebral and myocardial ischaemia, renal insufficiency, cerebral infarct, subarachnoid haemorrhage, arteriosclerosis pulmonary high blood pressure, inflammations, asthma, prostate hyperplasia, endotoxic shock and in complications after the administration of immunosuppressants which produce renal vasoconstriction.

COUPLING OF ORGANOTIN REAGENTS WITH ARYL, ACYL AND HETEROARYL HALIDES: SYNTHESIS OF PYRIDAZINE AND QUINOXALONE DERIVATIVES

Couplin of organotin reagents Bu3SnAr (Ar = 2- or 3-thienyl, 2- or 3-pyridyl) with ClCOCH2CH2CO2Et in the presence of PdCl(CH2Ph)(PPh3)2 yields β-ketoesters ArCOCH2CH2CO2Et which were converted with hydrazine hydrate into 6-substituted 4,5-dihydropyridazin-3(2H)-ones, and thence to 3-halogeno-6-substituted pyridazines.The latter also couple under similar conditions with Bu3SnAr to yield 3-heteroarylpyridazines.With catalysts, coupling of ClCOCO2Et and Bu3SnAr proceeds with loss of carbon monoxide giving ArCO2Et, but without catalyst ArCOCO2Et is formed from which the3-heteroarylquinoxalin-3-one is prepared.The reactions of Bu3SnAr with 4-XC6H4Br (X = H,-OMe, -CN, -NO2) are also described.

Synthesis and antihypertensive activity of new 6-heteroaryl-3-hydrazinopyridazine derivatives

The synthesis and pharmacological activity of new 6-heteroaryl-3-hydrazinopyridazines with antihypertensive action are described. The introduction of pyrrole, pyrazole, imidazole, triazole, tetrazole, thiophene, indole, and carbazole heterocyclic rings into the 6 position of the pyridazine nucleus has been carried out by three different methods of synthesis. The hypotensive action has been examined on normotensive and spontaneously hypertensive rats by comparison with dihydralazine (I). 6-Imidazol-1-yl derivatives have proved particularly active. Of these derivatives 3-hydrazino-6-(2-methylimidazol-1-yl)pyridazine (7c) achieves 4.9 times the activity of dihydralazine when administered orally to spontaneously hypertensive rats. The LD50 values of 7c and dihydralazine are very similar.