Tag: 200-300

On September 8, 2005, Arora, Nidhi; Billedeau, Roland Joseph; Dewdney, Nolan James; Gabriel, Tobias; Goldstein, David Michael; O’Yang, Counde; Soth, Michael published a patent.Electric Literature of 85426-79-5 The title of the patent was Preparation of fused pyrazolo pyrimidine and pyrazolo pyrimidinone derivatives as p38 kinase inhibitors. And the patent contained the following:

The title compounds I-III [R1 = (hetero)aryl, aralkyl, cycloalkyl; R2 = (hetero)aryl, cycloalkyl, alkyl, heterocyclyl; R3 = H, alkyl; R4 = H, alkyl, OH, etc.; R5 = H, alkyl, heteroalkyl, etc.; X, Y = N, or one of X and Y = N and the other = CR6 (R6 = H, alkyl, OH, etc.); Z = N, CR6; W = O, SOm, CH2, (un)substituted NH; m = 0-2; A = O, CH2, SOm, C(O), etc.; B = O, SOm, C(O), etc.; k = 0-1], useful in treating p38 mediated disorders, were prepared and formulated. E.g., a multi-step synthesis of (S)-IV, starting from 4,6-dichloro-2-(methylthio)pyrimidine and 2-chlorobenzaldehyde, was given. The compounds I were found to be inhibitors of p38 MAP kinase. IV showed a p38 IC50 of 0.004 μM. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Electric Literature of 85426-79-5

The Article related to fused pyrazolo pyrimidine pyrimidinone preparation p38 kinase inhibitor, pyrazolopyrimidine preparation p38 kinase inhibitor, pyrazolopyrimidinone preparation p38 kinase inhibitor and other aspects.Electric Literature of 85426-79-5

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Ali, Sahar A.; Awad, Samir Mohamed; Said, Ahmed Mohammed; Mahgoub, Shahenda; Taha, Heba; Ahmed, Naglaa Mohamed published an article in 2020, the title of the article was Design, synthesis, molecular modelling and biological evaluation of novel 3-(2-naphthyl)-1-phenyl-1H-pyrazole derivatives as potent antioxidants and 15-Lipoxygenase inhibitors.Safety of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde And the article contains the following content:

Oxidative stress is one of the main causes of significant severe diseases. The discovery of new potent antioxidants with high efficiency and low toxicity is a great demand in the field of medicinal chem. Herein, we report the design, synthesis mol. modeling and biol. evaluation of novel hybrids containing pyrazole, naphthalene and pyrazoline/isoxazoline moiety. Chalcones were synthesized efficiently and were used as starting materials for synthesis of a variety of heterocycles. A novel series of pyrazoline , phenylpyrazoline , isoxazoline and pyrazoline carbothioamide derivatives were synthesized and screened for in vitro antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO) and superoxide radical scavenging assay as well as 15-lipoxygenase (15-LOX) inhibition activity. Compounds and showed excellent radical scavenging activity in all three methods in comparison with ascorbic acid and 15-LOX inhibition potency using quercetin as standard then were subjected to in vivo study. Catalase (CAT) activity, glutathione (GSH) and malondialdehyde (MDA) levels were assayed in liver of treated rats. Compounds and showed significant in vivo antioxidant potentials compared to control group at dose of 100 mg/kg B. W. Mol. docking of compound endorsed its proper binding at the active site pocket of the human 15-LOX which explains its potent antioxidant activity in comparison with standard ascorbic acid. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Safety of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to naphthyl phenyl pyrazole derivative preparation antioxidants lipoxygenase inhibitor, 15-lipoxygenase inhibitors, pyrazole, antioxidant activity, hybrids, scavenging activity and other aspects.Safety of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On November 30, 2016, Ashok, Dongamanti; Rangu, Kavitha; Gundu, Srinivas; Rao, Velagapuri Hanumantha published an article.Application In Synthesis of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde The title of the article was Synthesis of pyrazolylfuro[2,3-f]chromenes and evaluation of their antimicrobial activity. And the article contained the following:

A new series of furochromene-based pyrazole derivatives were synthesized from their chalcone precursors upon reaction with 2-bromo-1-(4-bromophenyl)ethanone in the presence of anhydrous K2CO3 under conventional, ultrasound and microwave irradiation The shorter reaction times and high yields render the microwave irradiation approach as an advanced method to synthesize the title compounds All obtained compounds were evaluated for their antimicrobial activity against various bacterial and fungal strains. Most of the compounds exhibited variable range of antimicrobial activity and few compounds emerged as prospective antimicrobial agents by displaying promising microbial inhibitory potency. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).Application In Synthesis of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

The Article related to bromobenzoyl aryl phenylpyrazolylvinyl furochromene diastereoselective preparation antibacterial antifungal sar, Heterocyclic Compounds (One Hetero Atom): Benzopyrans (Including Coumarins, Isocoumarins, Chromones, Benzopyrones, Dibenzopyrans, and Other Arenopyrans) and other aspects.Application In Synthesis of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On January 6, 2022, Reynolds, Dominic; Seiler, Michael W.; Agrawal, Anant A.; Vaillancourt, Frederic; Smith, Peter; Hopper, Allen T.; Prajapati, Sudeep; Vyskocil, Stepan published a patent.HPLC of Formula: 2089292-88-4 The title of the patent was Preparation of 2-(indazol-5-yl)-6-(piperidin-4-yl)-1,7-naphthyridine derivatives and related compounds as modulators for splicing nucleic acids for the treatment of proliferative diseases. And the patent contained the following:

The disclosure relates to the title compounds I, wherein A and B are independently (un)substituted heterocyclyl and heteroaryl; L1 and L2 are independently absent, O, CO, etc.; X and Y are independently N and CR6; R2 and R3 are independently C1-6 alkyl, halo, CN, etc.; R6 is H, halo, CN, etc.; m = 0-1; N = 0-2; and pharmaceutically acceptable salts thereof, solvates, hydrates, tautomers, and stereoisomers thereof, that modulate nucleic acid splicing, e.g., splicing of a pre-mRNA, as well as methods of use thereof. Example compound II was prepared by a multistep procedure (procedure given). Compounds described herein were used to modulate RNA transcript abundance in cells (data given for representative compounds I). The experimental process involved the reaction of 5-Bromo-2-methyl-2H-pyrazolo[3,4-c]pyridine(cas: 2089292-88-4).HPLC of Formula: 2089292-88-4

The Article related to indazolyl piperidinylnaphthyridine preparation nucleic acid mrna splicing modulator antiproliferative, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.HPLC of Formula: 2089292-88-4

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On March 17, 2022, Yang, Shengyong; Li, Linli published a patent.Electric Literature of 1187582-58-6 The title of the patent was Preparation of 5-substituted indole-3-amide derivatives for disease treatments targeting RIPK1. And the patent contained the following:

Provided are a 5-substituted indole 3-amide derivative, a preparation method and a use thereof, belonging to the field of medicine. A compound represented by formula I [wherein X1 and X3 = independently N or (un)substituted CH; X2 = (un)substituted NH or CH=CH; R2B = -R2-B; R2 = (un)substituted alkylene,; B = (un)substituted aryl, cycloalkyl, heteroaryl, etc.; R3 = H or (un)substituted alkyl; R4 and R5 = independently H, alkyl, CN, OH, CO2H, etc.; A = (un)substituted aryl or heteroaryl] or a pharmaceutically acceptable salt thereof is provided. For example, II was prepared in a multi-step synthesis. This type of compound can significantly inhibit the activity of RIPK1 kinase, has high selectivity and excellent safety, serves as a RIPK1 kinase inhibitor, and can be used as a potential therapeutic drug for inflammation, immune diseases, tumors and neurodegenerative diseases. TNFα-induced SIRS model experiments proved that the compound can inhibit a RIPK1 kinase in vivo. Pharmacokinetic results showed that this series of compounds has excellent pharmacokinetic properties, thus providing a novel strategy and means for disease treatments targeting RIPK1. The experimental process involved the reaction of 5-Bromo-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazole(cas: 1187582-58-6).Electric Literature of 1187582-58-6

The Article related to preparation indole amide disease treatment ripk1 human, inflammation immune tumor neurodegenerative disease, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Electric Literature of 1187582-58-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Vlasenko, Yulia A.; Kuczmera, Thomas J.; Antonkin, Nikita S.; Postnikov, Pavel S.; Nachtsheim, Boris J. published an article in 2022, the title of the article was Site selective nucleophilic aromatic substitutions of azole-ligated diaryliodonium salts.SDS of cas: 57446-04-5 And the article contains the following content:

Herein the application of azole-stabilized diaryliodonium salts with addnl. thiophen-2-yl-ligands as substrates for metal-free nucleophilic arylations was presented. Besides their synthesis, their application in chemoselective nitrations, oxygenations, aminations as well as thiolations under umpolung conditions was demonstrated. Convenient one-pot procedures that are based on their in situ formation are also discussed. The experimental process involved the reaction of Methyl 3-(2-nitrophenyl)-1H-pyrazole-5-carboxylate(cas: 57446-04-5).SDS of cas: 57446-04-5

The Article related to diaryliodonium triflate regioselective nucleophilic aromatic nitration reaction, nitro biaryle preparation, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.SDS of cas: 57446-04-5

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On March 31, 2016, Ashok, Dongamanti; Rangu, Kavitha; Hanumantha Rao, Velagapuri; Gundu, Srinivas; Srilata, Ballu; Vijjulatha, Manga published an article.COA of Formula: C20H14N2O The title of the article was Microwave-assisted synthesis, molecular docking and antimicrobial activity of novel 2-(3-aryl-1-phenyl-1H-pyrazol-4-yl)-8H-pyrano[2,3-f]chromen-4-ones. And the article contained the following:

A series of pyrano[2,3-f]chromenones I [Ar = C6H5, 4-BrC6H4, 3,4-(MeO)2C6H3, 2-naphthyl, etc.] was synthesized via microwave-assisted cyclization of chalcones II in the presence of iodine in DMSO. Precursor chalcones II were prepared by Claisen-Schmidt condensation of 1-(5-hydroxy-2H-chromen-6-yl)ethanone and substituted pyrazole aldehydes using KOH under microwave irradiation This approach for the preparation of pyrano[2,3-f]chromenones I offers the advantages of short reaction time (3-5 min), mild reaction conditions and high yields of products. The newly synthesized compounds I and II were tested in vitro for their antibacterial and antifungal activities. Among the tested compounds, compounds I [Ar = 4-ClC6H4, 4-HOC6H4, 3,4-(MeO)2C6H3] and II [Ar = 3-EtOC6H4] were found to be potent against tested bacterial strains whereas compounds I [Ar = 4-ClC6H4, 3,4-(MeO)2C6H3] and II [Ar = 4-EtOC6H4] were found to be potent against tested fungal strains. Furthermore, the synthesized compounds were subjected to mol. docking studies for the inhibition of enzyme DNA gyrase and compounds I [Ar = 4-HOC6H4, 4-EtOC6H4] showed promising dock score values. The in silico mol. docking results of compounds I and II were in accordance with the in vitro antimicrobial studies and they may be considered as good inhibitor of DNA gyrase. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).COA of Formula: C20H14N2O

The Article related to pyranochromenone pyrazolyl preparation antibacterial antifungal mol docking, hydroxychromenyl pyrazolyl propenone preparation oxidative cyclization microwave irradiation, pyrazole aldehyde hydroxychromenyl ethanone claisen schmidt condensation microwave irradiation, pyrazolyl hydroxychromenyl propenone antibacterial antifungal mol docking and other aspects.COA of Formula: C20H14N2O

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

On March 31, 2007, Jagadhani, S. G.; Kale, S. B.; Chaudhari, C. S.; Sangle, M. D.; Randhavane, P. V.; Karale, B. K. published an article.SDS of cas: 36640-53-6 The title of the article was Knoevenagel reactions of 3-formyl chromones and 4-formyl pyrazoles with pyrazolone by conventional and non-conventional methods. And the article contained the following:

3-Formyl chromones when heated with 1,2-dihydro-1-phenyl-3-propylpyrazol-5-one (I) in presence of acetic acid afforded the compounds 4-(4-oxo-4H-chromon-3-yl)methylene-1-phenyl-3-propyl-1H-pyrazol-5-(4H)-ones. 4-Formyl pyrazoles on treatment with compound I in presence of acetic acid gave compounds (4)-1-phenyl-4-((1-phenyl-1H-pyrazol-4-yl)methylene)-3-propyl-1H-pyrazol-5-(4H)-ones. These compounds are synthesized by traditional, microwave, and ultrasonic irradiations. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).SDS of cas: 36640-53-6

The Article related to formyl chromone condensation pyrazolone microwave ultrasonic irradiation, pyrazole formyl condensation pyrazolone microwave ultrasonic irradiation, chromonyl methylene pyrazolone preparation microwave ultrasonic irradiation, pyrazolyl methylene pyrazolone preparation and other aspects.SDS of cas: 36640-53-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Rajashakar, V.; Saisree, K.; Sikender, M.; Naveen, S.; Madhava Reddy, B.; Harinadha Babu, V. published an article in 2016, the title of the article was Synthesis of pyrazolyl thiobarbituric acids and their cytotoxic and antimicrobial evaluation.HPLC of Formula: 36640-53-6 And the article contains the following content:

Synthesis, cytotoxic and anti-microbial screening of novel thiobarbituric acid incorporated pyrazole derivatives I [Ar = Ph, 4-H3CC6H4, 4-HOC6H4, 4-ClC6H4 and 2-naphthyl] were performed. Vilsmeier-Haack reaction of different Ph hydrazones afforded pyrazole-4-carbaldehydes in good yields. Knoevenagel condensation of compounds with thiobarbituric acid gave a series of 5-ylidene derivatives I in reasonable yields. The synthesized compounds were characterized with the help of IR, 1H-NMR and mass spectral data. The compounds were tested for cytotoxic activity against Vero, MCF-7 and HCT-116 cell lines. Among the tested compounds, compound I [Ar = 4-HOC6H4] was found to be most active mol. with the activity against both MCF-7 and HCT-116 cell lines with IC50 values of 14.0 μM and 18.12 μM. In anti-microbial screening, none of the compounds exhibited anti-bacterial activity. The experimental process involved the reaction of 3-(Naphthalen-2-yl)-1-phenyl-1H-pyrazole-4-carbaldehyde(cas: 36640-53-6).HPLC of Formula: 36640-53-6

The Article related to arylethylideneamino aniline preparation vilsmeir haack reaction, aryl phenylpyrazolyl carboxaldehyde preparation thiobarbituric acid knoevenagel condensation, phenyl arylpyrazolylmethylene thioxopyrimidine dione preparation antibacterial antitumor activity sar and other aspects.HPLC of Formula: 36640-53-6

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Seela, Frank; Jawalekar, Anup M.; Sun, Lijuan; Leonard, Peter published an article in 2005, the title of the article was Oligonucleotides Containing Pyrazolo[3,4-d]Pyrimidines: 8-Aza-7-deazaadenines With Bulky Substituents in the 2- or 7-Position.Product Details of 85426-79-5 And the article contains the following content:

The synthesis of the 2′-deoxyadenosine analogs, e.g. I, modified at the 7- and/or 2-position is described. The effect of 7-chloro and 2-methylthio groups on the duplex stability is evaluated. For that, the nucleosides, e.g. I, were converted to the corresponding phosphoramidites, which were employed in the solid-phase oligonucleotide synthesis. In oligonucleotide duplexes, compound I forms stable base pairs with dT, of which the separated I-dT base pairs contribute stronger than that of the consecutive base pairs. Nucleoside II shows universal base pairing properties while its N8 isomer forms duplexes with lower stability. The experimental process involved the reaction of 4-Chloro-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidine(cas: 85426-79-5).Product Details of 85426-79-5

The Article related to structure property thermodn thermal stability dna duplex synthesis, dna duplex synthesis thermal stability thermodn, oligonucleotide pyrazolopyrimidine azadeazaadenine synthesis dna duplex stability nucleoside phosphoramidite and other aspects.Product Details of 85426-79-5

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics