Disease relevance of Pyrazoline

• Triaryl pyrazoline compound inhibits flavivirus RNA replication [1].
• Cerebroprotective effects of a novel pyrazoline derivative, MS-153, on focal ischemia in rats [2].
• MS-153 ((R)-(-)-5-methyl-1-nicotinoyl-2-pyrazoline) is a novel pyrazoline compound that has potent cerebroprotective effects in the rat focal cerebral ischemia model [2].
• The most active of these new oxazolidinones were the dihydro-1,2-oxazine 6 and the 2-pyrazoline 20 both of which had potency similar to linezolid against a panel of Gram-positive bacteria [3].
• Studies on the effects of pyrazoline insecticides on mammalian sodium channels have been limited to experimentation on the tetrodotoxin-sensitive (TTX-S) and tetrodotoxin-resistant (TTX-R) sodium channel populations of rat dorsal root ganglion (DRG) neurons [4].

High impact information on Pyrazoline

• The molecular modeling work was carried out combining the Glide docking approach with CoMFA with the aim to rationalize the structure-activity relationships of each pyrazoline inhibitor toward MAO-A and MAO-B isoforms and to derive a suitable selectivity model [5].
• 4,5-dihydro-1H-pyrazole derivatives with inhibitory nNOS activity in rat brain: synthesis and structure-activity relationships [6].
• BW755C, a phenyl pyrazoline derivative, which is an inhibitor of both the cyclooxygenase and lipoxygenase pathways of arachidonic acid metabolism was the most active nonsteroidal compound and had an anti-inflammatory profile similar to dexamethasone [7].
• A regioselective synthesis has been developed for the preparation of unsymmetrical 1,3,5-triaryl-4-alkylpyrazolines and -pyrazoles by treatment of alpha-benzotriazolyl-alpha,beta-unsaturated ketones with monosubstituted hydrazines followed by alkylation at the 4-position of the pyrazoline ring [8].
• This study employed the Xenopus oocyte expression system to examine the relative sensitivity of rat Na(v)1.2a, Na(v)1.4, Na(v)1.5, and Na(v)1.8 sodium channel alpha subunit isoforms to the pyrazoline-type insecticides indoxacarb, DCJW, and RH 3421 [9].

Biological context of Pyrazoline

• Also, apoptotic cell death, calculated as a percent of DNA fragmentation, occurred to a greater extent in cells exposed to pyrazoline derivatives [10].
• These data imply that the binding site for pyrazoline insecticides overlaps with that for therapeutic sodium channel blockers [4].
• The relatively rapid formation of pyrazoline adducts is a serious side reaction in the esterification of 15-oxo-PGF2alpha with ethereal diazomethane under conditions used routinely in the chemical derivatization of prostaglandins [11].
• The best pyrazoline 5e of this series displayed an IC50 of 20 and 25 nmol/L for the CCK-A, and CCK-B receptor, respectively [12].

Anatomical context of Pyrazoline

• Pyrazoline reception: a possible role of opioid receptors of sensory neurons [13].

Associations of Pyrazoline with other chemical compounds

• Two new germacranolides, carpelipine A and carpelipine B in the form of its pyrazoline derivative were isolated from the whole plants of CARPESIUM LIPSKYI, and their structures were elucidated by spectroscopic methods including 2D NMR techniques ( (1)H- (1)H COSY, (1)H- (1)H NOESY, HMQC, HMBC) and chemical transformations [14].
• Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists [15].
• In contrast, we have not found any positive results from 10 normal donors without sensitivity to pyrazoline drugs after ingestion of metamizol 500 mg/day for 14 days [16].
• The X-ray structure analysis of the unexpected product of the reaction between 4-(4-methylphenyl)but-3-en-2-one and aminoguanidine revealed the title compound, C(12)H(17)N(4)(+) x -C(2)H(3)O(2)(-) x 0.5C(3)H(6)O, consisting of a protonated amidine moiety joined to a substituted pyrazoline ring at the N1 atom [17].

Gene context of Pyrazoline

• In an attempt to find new compounds with neuroprotective activity, we have designed, synthesized and characterized 19 new nNOS inhibitors with a 4,5-dihydro-1H-pyrazole structure [6].
• These data suggested that newly synthesized N-substituted pyrazoline derivatives can be evaluated as both MAO-B and cholinesterase inhibitors which may have promising features in the treatment of Alzheimer's and Parkinson's diseases [18].
• Antibacterials and antimycotics: Part 1: Synthesis and activity of 2-pyrazoline derivatives [19].
• State-dependent block of rat Nav1.4 sodium channels expressed in xenopus oocytes by pyrazoline-type insecticides [4].

Analytical, diagnostic and therapeutic context of Pyrazoline

• Triaryl pyrazoline {[5-(4-chloro-phenyl)-3-thiophen-2-yl-4,5-dihydro-pyrazol-1-yl]-phenyl-methanone} inhibits flavivirus infection in cell culture [1].

References