Day: December 1, 2022

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

Di Fabio, Romano published the artcileSynthesis and Pharmacological Characterization of Novel Druglike Corticotropin-Releasing Factor 1 Antagonists, Quality Control of 3553-12-6, the publication is Journal of Medicinal Chemistry (2008), 51(23), 7370-7379, database is CAplus and MEDLINE.

To identify new CRF₁ receptor antagonists, an attempt to modify the bis-heterocycle moiety present in the top region of the dihydropyrrole[2,3]pyridine template was made following new pharmacophoric hypothesis on the CRF₁ receptor antagonists binding pocket. In particular, the 2-thiazole ring, present in the previous series of compounds, was replaced by more hydrophilic non aromatic heterocycles able to make appropriate H-bond interactions with amino acid residues Thr192 and Tyr195. This exploration, followed by an accurate anal. of the substitution of the pendant aryl ring, enabled identification of in vitro potent compounds, e.g., I, showing excellent pharmacokinetics and outstanding in vivo activity in animal models of anxiety, both in rodents and primates.

Journal of Medicinal Chemistry published new progress about 3553-12-6. 3553-12-6 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Amine,Amide, name is 3-Acetamidopyrazole, and the molecular formula is C5H7N3O, Quality Control of 3553-12-6.

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

Tereshchenkova, Anna A. published the artcileSolid-phase extraction of lanthanum on modified low-polarity sorbents, Product Details of C17H14N2O2, the publication is Vestnik Moskovskogo Universiteta, Seriya 2: Khimiya (2013), 54(4), 203-209, database is CAplus.

Preconcentration of lanthanum on various low-polarity sorbents (hexadecyl-silica, hyper cross-linked polystyrene, polyvinylidene difluoride, activated carbon) dynamically coated with 1-phenyl-3-methyl-4-benzoylpyrazol-5-one (PMBP) was studied. Reagent and lanthanum distribution coefficients were evaluated under dynamic conditions. Reagent elution was studied. Recovery of lanthanum with coated and uncoated sorbents was studied. Efficiency of desorption with nitric acid solutions or ethanol was studied.

Vestnik Moskovskogo Universiteta, Seriya 2: Khimiya 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 C10H10N2, Product Details of C17H14N2O2.

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

Arkhipova, A. A. published the artcileDifferent Approaches to Solid-Phase Extraction of Lanthanum with Low-Polar Sorbents: Comparison of Dynamic Coating, Impregnation and On-Line Mixing, SDS of cas: 4551-69-3, the publication is Separation Science and Technology (Philadelphia, PA, United States) (2015), 50(5), 729-734, database is CAplus.

Three different approaches to preconcentration of metal ions using low-polar sorbents were compared: dynamic coating of the sorbent surface with hydrophobic chelating reagent; impregnation of the sorbent with a solution of the reagent in a suitable volatile organic solvent; and online merging of sample and reagent streams prior to solid-phase extraction of metal-reagent complexes. Lanthanum was used as a model analyte; 1-phenyl-3-methyl-4-benzoylpyrazol-5-one (PMBP) as a reagent for preconcentration It was found out that the most effective approach for the analyte recovery from a large sample volume is the use of a dynamically coated sorbent with high sp. surface.

Separation Science and Technology (Philadelphia, PA, United States) 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, SDS of cas: 4551-69-3.

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

Guise, G. B. published the artcileNew approaches to washfast dyes for wool. II. Synthesis and dyeing properties of model isothiouronium dyes, Product Details of C10H9ClN2O, the publication is Journal of the Society of Dyers and Colourists (1975), 91(8), 259-64, database is CAplus.

Nine dyes with the CH2CH2SC(NH2):NH2+X- group (X = Br, iodine) were prepared and gave fast dyeings on wool in cationic form and on polyesters in disperse form (by decomposition to the thiol immediately before application). P-C6H4(NH2)2 [106-50-3] was acylated with BrCH2CH2COCl [15486-96-1], and the resulting 4-BrCH2CH2CONHC6H4NH2.HCl [57058-91-0] was diazotized and coupled with 1-(2-chlorophenyl)-3-methyl-5-pyrazolone [14580-22-4] to give an azopyrazolone, which was treated with (H2N)2CS to give I [57058-92-1]. The 8 other azo and anthraquinone dyes were prepared as described in Ger. Offen. 1,962,859 (1970). Level dyeings on wool-polyester blends could be obtained by decomposing the dye to the disperse form in an alk. bath, neutralizing, and adding more dye to give a mixture of the cationic and disperse forms. The cationic dyes also readily dyed silk, hair, and acrylic fibers, but their fastness on cellulosics was inadequate. It seems unlikely that the fastness on wool is due to formation of mixed disulfides with cystine units.

Journal of the Society of Dyers and Colourists 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, Product Details of C10H9ClN2O.

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

Wang, Lan published the artcileFragment-based identification and optimization of a class of potent pyrrolo[2,1-f][1,2,4]triazine MAP4K4 inhibitors, Application In Synthesis of 763120-58-7, the publication is Bioorganic & Medicinal Chemistry Letters (2014), 24(18), 4546-4552, database is CAplus and MEDLINE.

MAP4K4 has been shown to regulate key cellular processes that are tied to disease pathogenesis. In an effort to generate small mol. MAP4K4 inhibitors, a fragment-based screen was carried out and a pyrrolotriazine fragment with excellent ligand efficiency was identified. Further modification of this fragment guided by X-ray crystal structures and mol. modeling led to the discovery of a series of promising compounds with good structural diversity and physicochem. properties. These compounds exhibited single digit nanomolar potency and compounds 35 and 44 achieved good in vivo exposure.

Bioorganic & Medicinal Chemistry Letters 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 C12H21NO7, Application In Synthesis of 763120-58-7.

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