pyrazoles-derivatives

Li, Hao published the artcileEfficient Synthesis of 1,9-Substituted Benzo[h][1,6]naphthyridin-2(1H)-ones and Evaluation of their Plasmodium falciparum Gametocytocidal Activities, COA of Formula: C3H5BN2O2, the publication is ACS Combinatorial Science (2017), 19(12), 748-754, database is CAplus and MEDLINE.

A novel three-component, two-step, 1-pot nucleophilic aromatic substitution (S_NAr)-intramol. cyclization-Suzuki coupling reaction was developed for the synthesis of benzo[h][1,6]naphthyridin-2(1H)-ones (Torins). On the basis of the new efficiently convergent synthetic route, a library of Torin 2 analogs was synthesized. The antimalarial activities of these compounds were evaluated against asexual parasites using a growth inhibition assay and gametocytes using a viability assay.

ACS Combinatorial Science published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, COA of Formula: C3H5BN2O2.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Yang, Xiaoqun published the artcileAsymmetric Synthesis of Structurally Sophisticated Spirocyclic Pyrano[2,3-c]pyrazole Derivatives Bearing a Chiral Quaternary Carbon Center, Name: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is Organic Letters (2022), 24(29), 5474-5479, database is CAplus and MEDLINE.

A carbene-catalyzed enantio- and diastereoselective [2 + 4] cycloaddition reaction is developed for quick and efficient access to structurally complex multicyclic pyrano[2,3-c]pyrazole mols. I (R = Me, Ph, 1-naphthyl, etc.; R¹ = H, Me, F; R² = H, Br, F; R³ = H, Me; R⁴ = Me, Bn, Ac, H; R⁵ = Me, Ph, 2-chlorophenyl). The reaction tolerates a broad scope of substrates bearing various substitution patterns, with the multicyclic pyrano[2,3-c]pyrazole products I afforded in generally good to excellent yields and optical purities. The chiral mols. obtained from this approach have found promising applications in the development of novel bactericides for plant protection.

Organic Letters published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C5H8N2O, Name: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Teng, Qing-Hu published the artcileDesign, syntheses and antitumor activities evaluation of 1,5-diaryl substituted pyrazole secnidazole ester derivatives, Computed Properties of 13599-22-9, the publication is Journal of Heterocyclic Chemistry (2021), 58(8), 1656-1664, database is CAplus.

According to the drug hybridization principle, a series of novel 1,5-diaryl substituted pyrazole secnidazole ester derivatives I (R¹ = 4-I, 3-Me, 4-Cl, etc.; R² = H, Me, Cl) have been synthesized by the combinations of various 1,5-diarylpyrazole-3-carboxylic acids II with secnidazole. The in vitro antitumor/cytotoxicities activities against tumor and normal cell lines, including NCI-H460 (lung tumor cell), MCG-803 (gastric tumor cell), Skov-3 (ovarian tumor cell), BEL-7404 (liver tumor cell) and HL-7702 (normal liver cell), have been evaluated using MTT assay. All compounds I showed promising inhibitory activities against four tumor cell lines. The IC₅₀ of I (R¹ = 4-I; R² = H) against the BEL-7404 cell was 2.03μM, and those of I (R¹ = 3-Me; R² = H) against the NCI-H460, MCG-803 and Skov-3 were 1.34, 0.14, and 0.87μM, resp. All these values were much lower than those of the cisplatin. Furthermore, I (R¹ = 3-Me, R² = H; R¹ = 4-I, R² = H) were also verified to be considerably safe for normal human liver cell, since the lower IC₅₀ values than cisplatin. Based on these results, the cell cycle anal., apoptosis ratio detection and mitochondrial membrane potential assay of I (R¹ = 3-Me, R² = H; R¹ = 4-I, R² = H) were further performed aiming to investigate their inhibition mechanism of BEL-7404 cells. It is revealed that they have effectively inhibited the cell growth by arresting the BEL-7404 cells at S phase and induced apoptosis through the mitochondria-mediated pathway.

Journal of Heterocyclic Chemistry published new progress about 13599-22-9. 13599-22-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Carboxylic acid,Benzene, name is 1,5-Diphenyl-1H-pyrazole-3-carboxylic acid, and the molecular formula is C8H15ClN2, Computed Properties of 13599-22-9.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Toonchue, Saowanee published the artcileMetal-free direct oxidative C-C bond coupling of pyrazolones and quinoxalinones, Product Details of C10H9ClN2O, the publication is Organic Chemistry Frontiers (2018), 5(12), 1928-1932, database is CAplus.

A highly efficient transition metal-free oxidative chemo- and regioselective C-C bond coupling of pyrazolones and quinoxalinones mediated by K₂S₂O₈ was described. This reaction was conveniently carried out under mild conditions which gave various hydroxy-pyrazolyl quinoxalinone products in moderate to excellent yields in a short reaction time.

Organic Chemistry Frontiers published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C5H5NO3S, Product Details of C10H9ClN2O.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Gouda, Ayman A. published the artcileDevelopment of cloud-point extraction method for preconcentration of trace quantities of cobalt and nickel in water and food samples, Related Products of pyrazoles-derivatives, the publication is RSC Advances (2016), 6(96), 94048-94057, database is CAplus.

A new, efficient, and sensitive cloud point methodol. was developed for preconcentration of trace quantities of cobalt and nickel in water and food samples prior to their determination by flame at. absorption spectrometry (FAAS). The metals react with 2-(benzothiazolylazo)-4-nitrophenol (BTANP) at pH 7.0 and micelle-mediated extraction using the nonionic surfactant Triton X-114 medium. The surfactant-rich phase was diluted with acidified methanol and the cobalt and nickel content was determined by FAAS. The optimum conditions (e.g. pH, reagent and surfactant concentrations, temperature and centrifugation times) were evaluated and optimized. The proposed CPE method showed linear calibration within the ranges 5.0-100 and 5.0-150 ng mL^-1 of cobalt and nickel, resp., and the limits of detection of the method was 1.4 and 1.0 ng mL^-1 of cobalt and nickel, resp. The interference effect of some cations and anions was also studied. The method was applied to the determination of both metals in water and food samples with a recovery from the spiked water samples in the range of 95-102%. The validation of the procedure was carried out by anal. of a certified reference material.

RSC Advances published new progress about 4551-69-3. 4551-69-3 belongs to pyrazoles-derivatives, auxiliary class Benzenes, name is 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, and the molecular formula is C17H14N2O2, Related Products of pyrazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Padmaja, Pannala published the artcileSynthesis, molecular docking and in vitro antiproliferative activity of novel pyrano[3,2-c]carbazole derivatives, Recommanded Product: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is New Journal of Chemistry (2016), 40(10), 8305-8315, database is CAplus.

A new series of polycyclic pyrano[3,2-c]carbazole derivatives have been synthesized by domino Knoevenagel-hetero-Diels-Alder reactions. The key strategy involves ethylenediamine diacetate (EDDA) catalyzed cyclization of the O-prenyl derivative of N-Boc-carbazole-3-carboxaldehyde with cyclic 1,3-diketones or pyrazol-5-ones to afford cis-fused N-Boc-pyrano[3,2-c]carbazole derivatives The reactions were clean and highly diastereoselective, affording the desired products in good yields. The deprotection of the Boc group under acidic conditions led to pyrano[3,2-c]carbazole derivatives The antiproliferative activity of all the synthesized compounds on three cancer cell lines such as PANC 1 (pancreatic), HeLa (cervical) and MDA-MB-231 (breast cancer) was investigated. Three compounds including I displayed pronounced antiproliferative activity. The antimicrobial activity of these compounds was assayed against three representative Gram-pos. organisms and Gram-neg. organisms. Compound I exhibited significant antimicrobial activity. Mol. docking studies revealed that the lead compounds selectively occupy the colchicine binding site of tubulin.

New Journal of Chemistry published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C10H9ClN2O, Recommanded Product: 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Zhang, Xingmei published the artcileCoupling of propylene sulfide (PS) and carbon disulfide (CS₂) catalyzed by the asymmetrical Cr(III)-bis-Schiff-base complex, Safety of 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, the publication is Inorganic Chemistry Communications (2017), 59-61, database is CAplus.

With an asym. Cr(III)-bis-Schiff-base complex [Cr(L)Cl] (1; H₂L obtained from reaction of HL⁰ ((Z)-4-((2-aminophenylimino)(phenyl)methyl)-3-methyl-1H-pyrazol-5(4H)-one) and 3,5-dibromo-2-hydroxybenzaldehyde) as the catalyst, the [PPN]Cl-assisted ([PPN]⁺ = [Ph₃P = N = PPh₃]⁺) coupling of PS (propylene sulfide) and CS₂ for the formation of poly[trithio]carbonate and [trithio]carbonate was efficiently realized, in which, the pre-activation of catalytic system and the coupling procedure have much influential to poly[trithio]carbonate selectivity.

Inorganic Chemistry Communications published new progress about 4551-69-3. 4551-69-3 belongs to pyrazoles-derivatives, auxiliary class Benzenes, name is 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one, and the molecular formula is C21H37BO, Safety of 4-Benzoyl-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Chattaway, F. D. published the artcileHalogen-substituted 1-arylpyrazolones, Related Products of pyrazoles-derivatives, the publication is Journal of the Chemical Society, Transactions (1924), 2423-7, database is CAplus.

The 1-chlorophenyl-3-methyl-5-pyrazolones are very similar in properties to the unsubstituted base, neither the position of the substituted halogen nor its accumulation in the Ph residue appearing greatly to affect the reactivity of the CH₂ group. 1-o-Chlorophenyl-3-methyl-5-pyrazoline (I), m. 199°, results by heating MeC(:NNHC₆H₄Cl)CH₂CO₂Et at 150-70° for about 90 mins.; HCl salt, m. 154°, decomposes 172°; 4-oximino derivative, golden brown, m. 174°; 4-benzylidene derivative, orange, m. 159°; 4-azo-o-chlorobenzene derivative, golden yellow, m. 212°. I, heated with MeI in MeOH in a sealed tube at 100-20° for 10 hrs., gives the 2,3-di-Me derivative (o-chloroantipyrine), m. 113°, whose aqueous solution has a strong bitter taste. 1-m-Chloro derivative (II), m. 131°; HCl salt, m. 184° (decomposition); 4-oximino derivative, orange, m. 173° (decomposition); 4-benzylidene derivative, red, m. 128°; 4-azo-2′,4′-dichlorobenzene, golden brown, m. 190°; II, heated with Me₂CO 4 hrs., gives the 4-isopropylidene derivative, S-yellow, m. 110°; 2,3-di-Me derivative (m-chloroantipyrine), m. 89-90°; its aqueous solution has an extremely bitter taste. II, heated with PhNHNH₂ until NH₃ is no longer liberated, and NaNO₂ in NaOH, added to an excess of dilute H₂SO₄, give m-chloropyrazole-blue, C₂₀H₁₄O₂N₄Cl₂, dark blue, m. 209° (decomposition); this also results by boiling II with FeCl₃; the other Cl derivatives do not show this reaction. It is easily reduced to the bispyrazolone. 1-p-Chloro HCl salt, m. 194-5° (decomposition); 4-oximino derivative, orange needles, m. 180° (decomposition); it also exists as the unstable form, brick-red, compact triclinic prisms; 4-benzylidene derivative, scarlet, m. 156°; 4-azo-p-chlorobenzene, orange-red, m. 232°; 2, 3-di-Me derivative (p-chloroantipyrine), m. 126°; this also has a very bitter taste. Bis-1-chlorophenyl-3-methyl-5-pyrazolone, decomposes without melting; p-chloropyrazole-blue, blue, decomposed at about 300°. 1,2,4-Dichlorophenyl-3-methyl-5-pyrazolone, m. 178°; HCl salt, m. 153°, decomposes 170°; 4-oximino derivative, canary-yellow, m. 166-8° (decomposition); 4-benzylidene derivative, orange, m. 131°; 4-azobenzene derivative, orange, m. 137-8°; 2, 3-di-Me derivative, m. 143°; the aqueous solution has a bitter taste.

Journal of the Chemical Society, Transactions published new progress about 14580-22-4. 14580-22-4 belongs to pyrazoles-derivatives, auxiliary class Organic Pigment, name is 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, and the molecular formula is C10H9ClN2O, Related Products of pyrazoles-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Popkova, Anna published the artcileA Cdc42-mediated supracellular network drives polarized forces and Drosophila egg chamber extension, Application of 4-(5-(4-Methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Nature Communications (2020), 11(1), 1921, database is CAplus and MEDLINE.

Abstract: Actomyosin supracellular networks emerge during development and tissue repair. These cytoskeletal structures are able to generate large scale forces that can extensively remodel epithelia driving tissue buckling, closure and extension. How supracellular networks emerge, are controlled and mech. work still remain elusive. During Drosophila oogenesis, the egg chamber elongates along the anterior-posterior axis. Here we show that a dorsal-ventral polarized supracellular F-actin network, running around the egg chamber on the basal side of follicle cells, emerges from polarized intercellular filopodia that radiate from basal stress fibers and extend penetrating neighboring cell cortexes. Filopodia can be mechanosensitive and function as cell-cell anchoring sites. The small GTPase Cdc42 governs the formation and distribution of intercellular filopodia and stress fibers in follicle cells. Finally, our study shows that a Cdc42-dependent supracellular cytoskeletal network provides a scaffold integrating local oscillatory actomyosin contractions at the tissue scale to drive global polarized forces and tissue elongation.

Nature Communications published new progress about 71203-35-5. 71203-35-5 belongs to pyrazoles-derivatives, auxiliary class GPCR/G Protein,Ras, name is 4-(5-(4-Methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide, and the molecular formula is C22H21N3O3S, Application of 4-(5-(4-Methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics

Glatthar, Ralf published the artcileDiscovery of Imidazoquinolines as a Novel Class of Potent, Selective, and in Vivo Efficacious Cancer Osaka Thyroid (COT) Kinase Inhibitors, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is Journal of Medicinal Chemistry (2016), 59(16), 7544-7560, database is CAplus and MEDLINE.

Cancer Osaka thyroid (COT) kinase is an important regulator of pro-inflammatory cytokines in macrophages. Thus, pharmacol. inhibition of COT should be a valid approach to therapeutically intervene in the pathogenesis of macrophage-driven inflammatory diseases such as rheumatoid arthritis. We report the discovery and chem. optimization of a novel series of COT kinase inhibitors, with unprecedented nanomolar potency for the inhibition of TNFα. Pharmacol. profiling in vivo revealed a high metabolism of these compounds in rats which was demonstrated to be predominantly attributed to aldehyde oxidase. Due to the very low activity of hepatic AO in the dog, the selected candidate 32 displayed significant blood exposure in dogs which resulted in a clear prevention of inflammation-driven lameness. Taken together, the described compounds both potently and selectively inhibit COT kinase in primary human cells and ameliorate inflammatory pathologies in vivo, supporting the notion that COT is an appropriate therapeutic target for inflammatory diseases.

Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, Recommanded Product: 1H-Pyrazole-4-boronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyrazole,
Pyrazoles – an overview | ScienceDirect Topics