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Isolation and X-ray characterization of {[phthalazinium](CuCl 2)}?: A new example of a dichlorocuprate(I) presenting a rare staircase Chain structure

Air-sensitive complexes [Cu2(mu-phtz)3(PR 3)2][CF3SO3]2 (phtz = C8H6N2), 3 (R = phenyl) and 4 (R = benzyl) have been synthesized from {[Cu(CF3SO3)]2 C 6H5Me} (1) at room temperature, in acetonitrile solution, after successive additions of stoichiometric amounts of phthalazine (phtz) and triphenylphosphine and tribenzylphosphine, respectively. The dissolution of 4 in an excess of benzyl chloride gave rise to the slow formation of orange needles, characterized by an X-ray crystallographic analysis as the title compound, {[phthalazinium](CuCl2)}? (5). The solid-state structure of 5 can be described as a one-dimensional anionic chain, [(CuCl2) -]?, presenting a rare staircase shape with terminal chloride ligands. The negative charges are compensated by monoprotonated phthalazinium cations [phtzH]+ which are stacked through pi-pi interactions between N-heterocyclic rings, and are also in N-H hydrogen bonding interaction with the terminal chloride ligands of the anionic chain. The formation of 5 was unexpected and can be explained by the dechlorination of benzyl chloride molecules.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N341 – PubChem

Extended knowledge of 6-(tert-Butyl)-8-fluorophthalazin-1(2H)-one

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Finding the perfect spot for fluorine: Improving potency up to 40-fold during a rational fluorine scan of a Bruton’s Tyrosine Kinase (BTK) inhibitor scaffold

A rational fluorine scan based on co-crystal structures was explored to increase the potency of a series of selective BTK inhibitors. While fluorine substitution on a saturated bicyclic ring system yields no apparent benefit, the same operation on an unsaturated bicyclic ring can increase HWB activity by up to 40-fold. Comparison of co-crystal structures of parent molecules and fluorinated counterparts revealed the importance of placing fluorine at the optimal position to achieve favorable interactions with protein side chains.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N690 – PubChem

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Synthesis and cytotoxicity evaluation of some new 6-nitro derivatives of thiazole-containing 4-(3H)-quinazolinone

Quinazolinones are a group of fused heterocyclic compounds which have valuable biological properties including cytotoxic, antibacterial and antifungal activities. Thiazole group-containing compounds have been also reported to have a wide range of biological activities such as antitumor, anti-inflammatory, analgesic and antibacterial effects. Due to valuable cytotoxic effects of both thiazole groups and quinazoline derivatives, in this study a series of quinazolinone-thiazole hybrids were synthesized and evaluated for their cytotoxic effects on three cell lines including MCF-7, HT-29, and PC-3. Among tested compounds (quinazolinones and three intermediates), k5 and k6 showed highest cytotoxic activities against PC3 cell line. K6 and C were most active compounds against MCF7 and K6 showed best cytotoxicity on HT-29 cell line.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N190 – PubChem

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Selective cobalt nanoparticles for catalytic transfer hydrogenation of N-heteroarenes

Nitrogen modified cobalt catalysts supported on carbon were prepared by pyrolysis of the mixture generated from cobalt(ii) acetate in aqueous solution of melamine or waste melamine resins, which are widely used as industrial polymers. The obtained nanostructured materials catalyze the transfer hydrogenation of N-heteroarenes with formic acid in the absence of base. The optimal Co/Melamine-2@C-700 catalyst exhibits high activity and selectivity for the dehydrogenation of formic acid into molecular hydrogen and carbon dioxide and allows for the reduction of diverse N-heteroarenes including substrates featuring sensitive functional groups.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N104 – PubChem

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Recent advances in the chemistry of macroline, sarpagine and ajmaline-related indole alkaloids

The chemistry of indole alkaloids related to macroline, sarpagine, and ajmaline was investigated. The Pictet-Spengler reaction remains a key strategic transformation for the synthesis of molecules of indole alkaloids. The chemistry shows that considerable advances have been made in the field of indole alkaloids. Several macroline-related alkaloids have been isolated and it is believed that macroline,or an equivalent is a likely biosynthetic precursor of various sarpagine alkaloids. Ajmaline-related alkaloids are defined as those having the same skeletal connectivity as ajmaline with an N4-C21 linkage but with the C16-(S) configuration. Sarpagine-related alkaloids are defined as those having the same skeletal connectivity as sarpagine with N4-C21 linkage. It is expected that further advances in the chemistry of macroline/ sarpagine/ ajmaline indole alkaloids will be reported by many laboratories.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N253 – PubChem

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Studies on Quinoline and Isoquinoline Derivatives. VII. Addition Reactions of Acetic Anhydride and Active Methylene Compounds to the Carbon-Nitrogen Double Bond of the Isoquinoline Ring

Acetic anhydride reacted with isoquinoline (IV) itself under reflux to give an addition product, whereas quinoline did not react with acetic anhydride under the same conditions.The structure of the product was determined to be 2-acetyl-1,2-dihydroisoquinoline-1-acetic acid (V) by means of chemical reactions.Active methylene (or methyl) compounds were observed to react with IV competitively to give the corresponding 1,2-dihydroisoquinolines when they were heated with IV in acetic anhydride.Keywords – acetic anhydride; active methylene compound; phthalazine; isoquinoline; C-C bond formation; 1,2-dihydroisoquinoline

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N489 – PubChem

New explortion of 6-Amino-2,3-dihydrophthalazine-1,4-dione

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Oral polymorphonuclear neutrophil characteristics in relation to oral health: A cross-sectional, observational clinical study

Polymorphonuclear neutrophils (PMNs) have a major role in the innate immune system. However, little is known about PMN contribution in relation to oral health. The objective of this study was to investigate the numbers and functional characteristics of oral PMNs (oPMNs) compared with circulatory PMNs (cPMNs). Oral rinse and venous blood samples were obtained from 268 systemically and orally healthy volunteers in a cross-sectional observational study. PMN counts, cell cycle analysis and cellular activation state were investigated. Also, reactive oxygen species (ROS) production was analyzed, with and without bacterial stimulation (Fusobacterium nucleatum). In males, 1.2 ¡Á 10 6 ¡À1.0 ¡Á 10 6 oPMNs were collected, and showed a tendency to correlate with the levels of gingival bleeding (r=0.215, P=0.008). Comparable oPMNs counts were found among females (1.0 ¡Á 10 6 ¡À0.7 ¡Á 10 6). More late-stage apoptotic/necrotic cells were found among the oPMNs (53.1%) compared with the cPMNs (8.5%; P<0.001). Without additional stimulation, oPMNs were more activated than cPMNs, as indicated by higher expression of CD11b, CD63 and CD66b, and higher constitutive ROS levels (P<0.001). Notably, in response to bacterial stimulation, oPMNs released comparable ROS levels as cPMNs (P=0.042). In conclusion, this study provides data on viable oPMNs showing high levels of activation in orally and systemically healthy individuals, free of apparent caries lesions and periodontal disease. These data suggests that although the oPMNs are in a more mature stage of their life cycle compared with the cPMNs, oPMNs are still responsive to stimulation, which indicates their functional potential and possible contribution to a healthy oral ecosystem. Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Synthetic Route of 3682-14-2. In my other articles, you can also check out more blogs about 3682-14-2

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Phthalazine – Wikipedia,
Phthalazine | C8H6N625 – PubChem

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Synthesis and characterization of some CoIII and Cr III complexes containing diazine ligands

Preparation and characterization of a number of CoIII and CrIII complexes containing one heterocyclic ligand was reported. The complexes [(NH3)5ML](ClO4)3 (M=Co, Cr, L=phthalazine, 1-methylphthalazine, pyridazine, 3-methylpyridazine) were prepared by reaction of triflato complex [(NH3)5MOSO2CF3] (CF3SO3)2 with the appropriate ligand in sulfolane. These complexes were recrystallized in warm water by addition of NaClO4 and characterized by 1H and 13C NMR spectroscopy and elemental analysis. NOE and DESERT experiments were carried out in order to characterize the position of coordination.

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Reference£º
Phthalazine – Wikipedia,
Phthalazine | C8H6N291 – PubChem

Properties and Exciting Facts About 2-(3-(4-Bromo-2-fluorobenzyl)-4-oxo-3,4-dihydrophthalazin-1-yl)acetic acid

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Enzymological studies on the mechanisms of pathogenesis of diabetic complications

Aldose reductase (AR) is involved in the pathogenesis of complications in diabetes. In this study, the enzymatic properties of AR isolated from various sources and a recombinant human AR (rh-AR) were analyzed in detail. The sensitivity of different forms of AR to several AR inhibitors (ARIs) was compared. Our findings enabled us to propose that human AR should be used as the target enzyme in the development of ARIs. An enzyme-linked immunosorbent assay (ELISA) for human AR which employed monoclonal antibodies against rh-AR was created, and this method was used to demonstrate the distribution of AR in human tissues. AR was widely distributed in various organs and blood cell components. The levels of erythrocyte AR (e-AR) were 10.1¡À1.9 ng/mg Hb and 10.5¡À3.0 ng/mg Hb in healthy volunteers and diabetic patients, respectively, and thus there was no significant difference between them. The e-AR levels of diabetic patients were assayed using the ELISA developed to investigate the potential correlation between AR levels and the onset of diabetic complications. There were significant correlations between the incidence of diabetic neuropathy and e-AR levels in patients with disease duration of less than 10 years, and between the incidence of diabetic retinopathy and e-AR levels in patients with disease duration of 10-20 years. Our results suggest that measurement of e-AR levels in patients could help optimize drug therapy with ARIs and be a useful method to predict the onset of complications due to the upregulation of the polyol pathway.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N920 – PubChem

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Histidine-Rich Glycoprotein Prevents Septic Lethality through Regulation of Immunothrombosis and Inflammation

Sepsis is a major cause of death worldwide. We show that a plasma protein histidine-rich glycoprotein (HRG) was decreased significantly in septic mice with cecal ligation and puncture (CLP) and supplementary treatment of septic mice with exogenous HRG improved survival, with strong inhibition of tight attachment of neutrophils to pulmonary vasculatures, subsequent immunothrombosis, DIC state, lung inflammation, hypercytokinemia, and activation of vascular endothelial cells (VECs). In contrast, knockdown of HRG by siRNA exacerbated lethality. Purified human HRG reversibly induced morphological changes in human neutrophils in vitro; induction of spherical shape with reduced microvilli and adhesiveness to VECs. HRG maintained the passage of neutrophils through microcapillaries and abolished production of reactive oxygen species. These results suggested that the supplementary therapy with HRG may provide a novel strategy for the treatment of sepsis through suppression of excessive systemic inflammation and immunothrombosis by keeping circulating neutrophils quiescent and preventing uncontrolled activation of VECs.

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Phthalazine – Wikipedia,
Phthalazine | C8H6N650 – PubChem