Category: pyrazoles-derivatives

Guccione, Salvatore published the artcileSynthesis of 3-methyl-substituted pyrazolotriazolopyrimidin-4-one and pyrazolothiazolopyrimidin-4-one derivatives, SDS of cas: 23286-70-6, the publication is Journal of Heterocyclic Chemistry (1996), 33(2), 459-463, database is CAplus.

As a part of a research on anti-inflammatory analgesic compounds 3-Me substituted pyrazolotriazolopyrimidin-4-one derivatives (R = Ph, 4-chlorophenyl) and pyrazolothiazolopyrimidin-4-one derivatives II (R¹ = H, Br) were prepared by previously reported procedures. None of the compounds showed improved activity when compared with the previously reported unsubstituted analogs.

Journal of Heterocyclic Chemistry published new progress about 23286-70-6. 23286-70-6 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Amine,Ester, name is Ethyl 5-amino-3-methyl-1H-pyrazole-4-carboxylate, and the molecular formula is C7H11N3O2, SDS of cas: 23286-70-6.

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

Lee, Angeline C.-H. published the artcileThieno[3,2-d]pyrimidin-4(3H)-one derivatives as PDK1 inhibitors discovered by fragment-based screening, Computed Properties of 763120-58-7, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(12), 4023-4027, database is CAplus and MEDLINE.

Ligand efficient fragments binding to PDK1 were identified by an NMR fragment-based screening approach. Computational modeling of the fragments bound to the active site led to the design and synthesis of a series of novel 6,7-disubstituted thienopyrimidin-4-one compounds e. g., I, with low micromolar inhibitory activity against PDK1 in a biochem. enzyme assay.

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 C3H5BN2O2, Computed Properties of 763120-58-7.

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

Yang, Guang published the artcileCadmium(II) Complexes of 4-(4-Pyridyl)Pyrazole: A Case of Two Conformational Supramolecular Isomers Polythreaded in the Same Crystal and a Rare Example of 5-Connected nov Net, Related Products of pyrazoles-derivatives, the publication is Crystal Growth & Design (2008), 8(3), 981-985, database is CAplus.

Stoichiometric control of the reactions of Cd(BF₄)₂ with 4-(4-pyridyl)pyrazole (4-py-pzH) gave four different crystalline products: mononuclear [Cd(4-py-pzH)₄(H₂O)₂](BF₄)₂ (1), a polythreaded two-dimensional (2D) + 1-dimensional (1D) complex [Cd(NCS)₂(μ-4-py-pzH)₂]_n (2), a 1-dimensional chain {[Cd(NCS)₂(4-Hpy-pzH)₂][Cd(NCS)₄]}_n (3), and a 3-dimensional [Cd(NCS)₂(μ-4-py-pzH)]_n (4). Complex 2 consists of stacked 2-dimensional square layers penetrated by columns of 1-dimensional ribbons. The 2-dimensional and 1-dimensional components of 2 are conformational supramol. isomers [Cd(NCS)₂(μ-4-py-pzH)₂]_n. The topol. underlying 4 represents a rare example of a 5-connected nov net observed in metal-organic frameworks.

Crystal Growth & Design published new progress about 19959-71-8. 19959-71-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Pyridine, name is 4-(1H-Pyrazol-4-yl)pyridine, and the molecular formula is C42H63O3P, Related Products of pyrazoles-derivatives.

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

Megahed, Sarah H. published the artcileNovel 2,4-disubstituted quinazoline analogs as antibacterial agents with improved cytotoxicity profile: Modification of the benzenoid part, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2022), 128531, database is CAplus and MEDLINE.

Bacterial resistance to currently used antibiotics demands the development of novel antibacterial agents with good safety margins and sufficient efficacy against multi-drug resistant isolates. We have previously described the synthesis of N-butyl-2-(butylthio)quinazolin-4-amine (I) as an optimized hit with broad-spectrum antibacterial activity and low cytotoxicity. In addition, we have identified a potential growing vector for this series of compounds Herein, we describe further hit optimization which includes systematic diversifications of both the benzenoid part and the substituents at position 6 and 7 of compound I. Growing of the mol. beside the core modifications yielded several compounds with remarkable anti(myco)bacterial activity against a panel of pathogenic bacteria, including drug-resistant strains. 3-(4-(Butylamino)-2-(butylthio)quinazolin-6-yl)phenol showed a 2-4 fold improvement in activity than I against S. aureus Newman, S. pneumoniae DSM-20566 and E. faecalis DSM-20478. The compounds also showed a good safety profile towards human HepG2 cells.

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 C3H5BN2O2, Recommanded Product: 1H-Pyrazole-4-boronic acid.

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

Trivedi, A. R. published the artcileSynthesis and biological evaluation of 1-aryl-3-methyl-4-(5′-chloro-3′-methyl-1′-phenylpyrazol-4′-yl)-4,4a-dihydro-6H-pyrazolo[3,4-d]-1,3-thiazolidino[3,2-a]pyrimidine-5-ones, COA of Formula: C10H9ClN2O, the publication is Journal of the Institution of Chemists (India) (2009), 81(1), 26-32, database is CAplus.

Pyrazolo[3,4-d]pyrimidines I (R = 2-ClC₆H₄, 3-ClC₆H₄, 4-MeC₆H₄, etc.) were obtained via 3-component coupling of 5-chloro-4-formyl-3-methyl-1-phenylpyrazol, thiourea, and 3-methyl-1-R-5-pyrazolone followed by cyclocondensation of the intermediates II with chloroacetic acid. Compounds I were tested for antimycobacterial, antibacterial and antifungal activities.

Journal of the Institution of Chemists (India) 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 C7H5Cl2NO2, COA of Formula: C10H9ClN2O.

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

Parmar, Deepa R. published the artcileDesign, Synthesis, In Silico Studies and In Vitro Anticancer Activity of 3-(4-Methoxyphenyl)azetidine Derivatives, Recommanded Product: 1H-Pyrazole-4-boronic acid, the publication is ChemistrySelect (2020), 5(45), 14296-14302, database is CAplus.

A series of 3-(4-methoxyphenyl)azetidine analogs I [Ar = Ph, 4-MeC₆H₄, 4-FC₆H₄, etc.] were synthesized and screened for their in vitro anticancer activity against nine different human cancer cell lines using the cell counting kit-8 (CCK-8) assay. The toxicity, bioavailability and lipophilicity of all the synthesized compounds I were predicted by using osiris and molinspiration model. Mol. docking study revealed that, compound I [Ar = 2-aminopyridin-4-yl, 2-methoxypyridin-4-yl] were found to be potential inhibitor of human topoisomerase IIα. The cell viability studies exhibited promising antiproliferative activities of the compound I [Ar = 2-aminopyridin-4-yl] (EC₅₀ 0.03μM) was found to be more potent than standard Doxorubicin (EC₅₀ 0.07μM) in U251 cancer cell lines. Similarly, compound I [Ar = 2-methoxypyridin-4-yl] showed considerable potency against four different cancer cell lines (HepG2, U251, A431, 786-O) with EC₅₀ values ranging from 0.46 to 2.13μM.

ChemistrySelect 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

Sudheer Reddy, V. published the artcileSynthesis of Some New N-Substituted Imidazole Derivatives and Their In Vitro Antibacterial Investigation, Product Details of C3H5BN2O2, the publication is Russian Journal of Bioorganic Chemistry (2022), 48(3), 643-650, database is CAplus.

Here the synthesis of N-substituted imidazole derivatives I (X = 3-MeOC₆H₄, 4-O₂NC₆H₄, 3,5-F₂C₆H₃, etc.) based on Suzuki coupling reaction of I (X = Br) with various arylboronic acids using Pd(dppf)Cl₂·CH₂Cl₂ as the catalyst and K₂CO₃ as a base in 1,4-dioxane/H₂O (2 : 1) is described. The products were screened for their antibacterial activity against gram-pos. bacterial strains, Bacillus subtilis and Staphylococcus aureus, where the compounds I (X = 4-pyridinyl, 3-F-4-MeOC₆H₃, 3-NCC₆H₄, 3-FC₆H₄, 4-F-3-MeC₆H₃, 4-pyrazolyl) exhibited remarkable activity compared to the reference streptomycin.

Russian Journal of Bioorganic Chemistry published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C14H20BClO2, Product Details of C3H5BN2O2.

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

Sudheer Reddy, V. published the artcileSynthesis of Some New N-Substituted Imidazole Derivatives and Their In Vitro Antibacterial Investigation, Application In Synthesis of 763120-58-7, the publication is Russian Journal of Bioorganic Chemistry (2022), 48(3), 643-650, database is CAplus.

Here the synthesis of N-substituted imidazole derivatives I (X = 3-MeOC₆H₄, 4-O₂NC₆H₄, 3,5-F₂C₆H₃, etc.) based on Suzuki coupling reaction of I (X = Br) with various arylboronic acids using Pd(dppf)Cl₂·CH₂Cl₂ as the catalyst and K₂CO₃ as a base in 1,4-dioxane/H₂O (2 : 1) is described. The products were screened for their antibacterial activity against gram-pos. bacterial strains, Bacillus subtilis and Staphylococcus aureus, where the compounds I (X = 4-pyridinyl, 3-F-4-MeOC₆H₃, 3-NCC₆H₄, 3-FC₆H₄, 4-F-3-MeC₆H₃, 4-pyrazolyl) exhibited remarkable activity compared to the reference streptomycin.

Russian Journal of Bioorganic 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 C8H5F3O3, Application In Synthesis of 763120-58-7.

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

Mueller, Rudolf published the artcileLerisetron Analogues with Antimalarial Properties: Synthesis, Structure-Activity Relationship Studies, and Biological Assessment, SDS of cas: 724710-02-5, the publication is ACS Omega (2020), 5(12), 6967-6982, database is CAplus and MEDLINE.

A phenotypic whole cell high-throughput screen against the asexual blood and liver stages of the malaria parasite identified a benzimidazole chem. series. Among the hits were the antiemetic benzimidazole drug Lerisetron 1 (IC₅₀ NF54 = 0.81μM) and its methyl-substituted analog 2 (IC₅₀ NF54 = 0.098μM). A medicinal chem. hit to lead effort led to the identification of chloro-substituted analog 3 with high potency against the drug-sensitive NF54 (IC₅₀ NF54 = 0.062μM) and multidrug-resistant K1 (IC₅₀ K1 = 0.054μM) strains of the human malaria parasite Plasmodium falciparum. Compounds 2 and 3 gratifyingly showed in vivo efficacy in both Plasmodium berghei and P. falciparum mouse models of malaria. Cardiotoxicity risk as expressed in strong inhibition of the human ether-a-go-go-related gene (hERG) potassium channel was identified as a major liability to address. This led to the synthesis and biol. assessment of around 60 analogs from which several compounds with improved antiplasmodial potency, relative to the lead compound 3, were identified.

ACS Omega published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C3H5BN2O2, SDS of cas: 724710-02-5.

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