[On the reaction products of bromometric titrations of various sulfonamides of the pyridazine, pyrazine and pyrazole series].
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Chemistry, Pharmaceutical↗
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Results for “Pyridazines”
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[On heterocycles, XLVI: syntheses of thiazolo(4,5-d)pyridazines].
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Methods↗
[Pyridazine analogues of biologically active compounds, I: trans-4-Styrylpyridazines (author's transl)].
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Choline O-Acetyltransferase↗
[Thiophene as a structural element in physiologically active substances. 15. Thiophene analogs of an anxiolytic acting 1,2,4-triazolo[4,3-b]pyridazine].
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Animals↗
4,5-disubstituted pyridazin-3(2H)-ones as hypotensive drugs: incorporation of a beta-blocking moiety.
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Adrenergic beta-Antagonists↗
Pyridazines. XXXVIII. Pyridazino[4,5-e]-1,4-diazepine--a novel ring system of potential pharmaceutical interest.
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Azepines↗
Pyridazine derivatives, VI. Synthesis and hypotensive activity of 3-hydrazinethieno(2,3-h)cinnoline and its derivatives.
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Animals↗
Synthesis and antihypertensive properties of some dopamino-pyridazin-3(2H)-one derivatives.
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Animals↗
Selected pharmacological studies of a series of substituted imidazo(4,5-d)pyridazines.
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Animals↗
Characterization of polymorphs and solvates of 3-amino-1-(m-trifluoromethylphenyl)-6-methyl-1H-pyridazin-4-one.
The characterization of two polymorphs of the title compound (F2692; 1) by differential scanning calorimetry (DSC), microanalysis, proton nuclear magnetic resonance spectroscopy, thermogravimetry, thermomicroscopy, infrared spectroscopy, and X-ray diffractometry is described. Both polymorphs are crystalline, with form II being more stable at temperatures less than 160 degrees C. The thermal behavior was studied at different rates of heating, and the enthalpies of transition were calculated from DSC data. The transformation of aqueous suspensions of form I to the water-stable form II is described, and the heats of solution and intrinsic aqueous dissolution rates of both polymorphs were determined. 1 also formed solvates with dimethyl sulfoxide and 1-methyl-2-pyrrolidinone. The solvates were studied by thermogravimetry, DSC, and infrared spectroscopy.
Anti-Anxiety Agents↗
Disposition and metabolism of 3-hydrazino-6-[N,N-bis(2-hydroxyethyl)amino] pyridazine dihydrochloride in man.
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Adult↗
A new antihypertensive compound: 3 hydrazino-6- [(2-hydroxypropyl)methylamino] pyridazine dihydrochloride (ISF 2123).
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Administration, Oral↗
A selective inhibitor of thromboxane synthetase activity of rabbit heart tissue: a pyridazinic derivative.
The effects of 2-(2 dimethylaminoethyl) 5-benzylidene 6-methyl (2H,4H)-3-pyridazinone (III) were studied on the biosynthesis of TXA2 and PGI2 in vitro the TXA2 and PGI2 synthetase activity of heart tissue. Biosyntheses of TXA2 and PGI2 were carried out using arachidonic acid as a substrate and horse platelet and aorta microsomes as sources of TXA2 and PGI2 synthetases respectively. TXB2 and 6-keto PGF1 alpha were determined by RIA. III--did not significantly modify either the biosynthesis of PGI2 in vitro or the PGI2 synthetase activity of heart tissue. did not significantly inhibit TXA2 biosynthesis in vitro but markedly reduced the TXA2 synthetase activity of heart tissue: for a microsomal fraction concentration of 100 micrograms protein, the ID50 was 6.37 X 10(-5) M +/- 1.29 X 10(-8) M. Thus III behaves as a specific inhibitor of the TXA2 synthetase activity of heart tissue and could have a beneficial use in therapeutics.
Animals↗
Pyridazines. Part 36: Synthesis and antiplatelet activity of 5-substituted-6-phenyl-3(2H)-pyridazinones.
A convenient and efficient palladium-catalysed retro-ene-assisted method has been developed to prepare a series of 5-substituted-6-phenyl-3(2H)-pyridazinones as potential antiplatelet drugs. The most active compounds were those that contain a 3-phenyl-3-oxo-propenyl fragment or a phenylthio group at position 5 of the heterocyclic ring.
Humans↗
New pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective PDE5 inhibitors.
A series of potent PDE5 inhibitors with high selectivity versus PDE6 isoenzymes was identified.
3',5'-Cyclic-GMP Phosphodiesterases↗
Synthesis and anti-microbial activity of some imidazo[1',2':5,6]pyrimido[4,5-c]pyridazines and related heterocycles.
The synthesis of the title heterocycles was achieved using 3-amino-5,6-diphenylpyridazine-4-carbonitrile (4) as a starting material. This compound was converted into the corresponding 4-imidazolinyl derivative 5 which was then subjected to cyclization reactions to afford the title compounds.
Anti-Bacterial Agents↗
Photo-induced oxygenation by pyridazine N-oxides. II.
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Cyclic N-Oxides↗
Pharmacologically active pyridazine derivatives. Part 2.
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Bronchodilator Agents↗