Day: November 21, 2022

Whitlock, Gavin A. published the artcileNovel 2-imidazoles as potent and selective α_1A adrenoceptor partial agonists, Application of 1H-Pyrazole-4-boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(9), 2930-2934, database is CAplus and MEDLINE.

Novel 2-imidazoles have been identified as potent partial agonists of the α_1A adrenergic receptor, with good selectivity over the α_1B, α_1D and α_2A receptor sub-types. Sulfonamide 23 (I) possessed attractive drug-like properties with respect to physicochem. and ADME properties and wide ligand selectivity.

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 C8H14O2, Application of 1H-Pyrazole-4-boronic acid.

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

Whitlock, Gavin A. published the artcileNovel 2-imidazoles as potent and selective α_1A adrenoceptor partial agonists, Application In Synthesis of 724710-02-5, the publication is Bioorganic & Medicinal Chemistry Letters (2008), 18(9), 2930-2934, database is CAplus and MEDLINE.

Novel 2-imidazoles have been identified as potent partial agonists of the α_1A adrenergic receptor, with good selectivity over the α_1B, α_1D and α_2A receptor sub-types. Sulfonamide 23 (I) possessed attractive drug-like properties with respect to physicochem. and ADME properties and wide ligand selectivity.

Bioorganic & Medicinal Chemistry Letters 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 C14H23N, Application In Synthesis of 724710-02-5.

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

Gomez Guillen, M. published the artcileSynthesis of (pentahydroxypentyl)pyrazoles by reaction of D-galactose arylhydrazones with 2-nitro-1-phenylalkenes, Computed Properties of 13599-22-9, the publication is Anales de Quimica, Serie C: Quimica Organica y Bioquimica (1986), 82(3), 204-10, database is CAplus.

The reactions of aldehydo–D-galactose phenylhydrazones I (R = Ph) with β-nitrostyrene II (R¹ = H, Me) gave diphenylpyrazoles III (R = Ph, R¹ = H, Me); similarly I (R = p-MeC₆H₄) and II (R¹ = Me) gave III (R = p-MeC₆H₄, R¹ = Me). I (R = p-MeC₆H₄) and II (R¹ = H) gave tolylpyrazole IV showing the reverse regiochem. to that previously observed III and IV were converted to pentaacetates or oxidized by IO₄^– to pyrazole-3-carboxaldehydes which were then converted to carboxylic acids by moist Ag₂O.

Anales de Quimica, Serie C: Quimica Organica y Bioquimica 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 C16H12N2O2, Computed Properties of 13599-22-9.

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

Janssen, Joseph W. A. M. published the artcileGeneration and reactivity of N-pyrazolyl radicals in benzene solution, SDS of cas: 53355-55-8, the publication is Journal of Organic Chemistry (1975), 40(7), 915-20, database is CAplus.

The preparations of tert-Bu 1-pyrazolepercarboxylate and its 3-Me derivative are described. Thermolysis of these compounds in benzene at ∼140° proceeds predominantly via homolysis and leads to N-phenylated pyrazoles without formation of isomeric C-Ph derivatives N-pyrazolyl radicals, which are proposed as intermediates, apparently are able to effect homolytic aromatic substitution. Judging from competition with p-dichlorobenzene (partial rate factor ∼0.25), 1-pyrazolyl has a marked electrophilic character. Photolysis of N-nitropyrazoles in benzene, also leading to N-phenylated derivatives, is another way to generate N-pyrazloyl radicals. The unpaired electron is delocalized over (at least) the two N atoms. A σ-type ground state is favored over a π-type electronic structure.

Journal of Organic Chemistry published new progress about 53355-55-8. 53355-55-8 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Chloride,acyl chloride,Amide, name is 1H-Pyrazole-1-carbonyl chloride, and the molecular formula is C4H3ClN2O, SDS of cas: 53355-55-8.

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

Eaton, Amity F. published the artcileExpansion and contraction of the umbrella cell apical junctional ring in response to bladder filling and voiding, Safety of 4-(5-(4-Methoxyphenyl)-3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)benzenesulfonamide, the publication is Molecular Biology of the Cell (2019), 30(16), 2037-2052, database is CAplus and MEDLINE.

The epithelial junctional complex, composed of tight junctions, adherens junctions, desmosomes, and an associated actomyosin cytoskeleton, forms the apical junctional ring (AJR), which must maintain its continuity in the face of external mech. forces that accompany normal physiol. functions. The AJR of umbrella cells, which line the luminal surface of the bladder, expands during bladder filling and contracts upon voiding; however, the mechanisms that drive these events are unknown. Using native umbrella cells as a model, we observed that the umbrella cell’s AJR assumed a nonsarcomeric organization in which filamentous actin and ACTN4 formed unbroken continuous rings, while nonmuscle myosin II (NMMII) formed linear tracts along the actin ring. Expansion of the umbrella cell AJR required formin-dependent actin assembly, but was independent of NMMII ATPase function. AJR expansion also required membrane traffic, RAB13-dependent exocytosis, specifically, but not trafficking events regulated by RAB8A or RAB11A. In contrast, the voiding-induced contraction of the AJR depended on NMMII and actin dynamics, RHOA, and dynamin-dependent endocytosis. Taken together, our studies indicate that a mechanism by which the umbrella cells retain continuity during cyclical changes in volume is the expansion and contraction of their AJR, processes regulated by the actomyosin cytoskeleton and membrane trafficking events.

Molecular Biology of the Cell 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, Safety 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

Leurs, Ulrike published the artcileInhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C), Computed Properties of 724710-02-5, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(18), 5811-5813, database is CAplus and MEDLINE.

The human histone demethylases of the KDM4 (JMJD2) family have been associated to diseases such as prostate and breast cancer, as well as X-linked mental retardation. Therefore, these enzymes are considered oncogenes and their selective inhibition might be a possible therapeutic approach to treat cancer. Here the authors describe a heterocyclic ring system library screened against the histone demethylase KDM4C (JMJD2C) in the search for novel inhibitory scaffolds. A 4-hydroxypyrazole scaffold was identified as an inhibitor of KDM4C; this scaffold could be employed in the further development of novel therapeutics, as well as for the elucidation of the biol. roles of KDM4C on epigenetic regulation.

Bioorganic & Medicinal Chemistry Letters 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, Computed Properties of 724710-02-5.

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

Ding, Yun published the artcileRobust Suzuki-Miyaura Cross-Coupling on DNA-Linked Substrates, Product Details of C3H5BN2O2, the publication is ACS Combinatorial Science (2015), 17(1), 1-4, database is CAplus and MEDLINE.

The Suzuki-Miyaura cross-coupling is one of the most widely employed reactions in medicinal chem. To apply this reaction to DNA-encoded library technol. (ELT), an alternative approach in the discovery of small mol. hits and leads, we explored the Suzuki-Miyaura cross-coupling on DNA-linked aryl halides. Pd(PPh₃)₄ was demonstrated to be an effective catalyst for cross-coupling with on-DNA halide substrates under aqueous conditions. It efficiently catalyzes the coupling of Ph halides (iodide or bromide) and pyridinyl bromides with various boronic acids/esters, including challenging heterocyclic boronic acids/esters.

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, Product Details of C3H5BN2O2.

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

Belen’kii, L. I. published the artcileAlternative mechanisms of electrophilic substitution in azole series, Product Details of C4H6N2, the publication is Russian Chemical Bulletin (2016), 65(6), 1441-1447, database is CAplus.

Data on three mechanisms of aromatic electrophilic substitution in azole series were presented. First of them is similar to an ordinary addition-elimination mechanism including the formation of a cationic σ-complex (Wheland intermediate). The second mechanism is realized according to the elimination-addition scheme and includes a protonation or a formation of a complex on the pyridine N atom, proton abstraction from the C atom adjacent to the above N atom, and addition of a cationoid reagent to the ylide (carbene) formed. The third mechanism proposed by the present authors can be realized for azoles having three and two N atoms of the pyridine type. It does not require the preliminary N-protonation or complex formation and occurs due to a strong electron withdrawing effect of several pyridine atoms, resulting in the CH-deprotonation followed by the interaction of the carbanion formed with a cation under mild conditions.

Russian Chemical Bulletin published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, Product Details of C4H6N2.

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

Demont, Emmanuel H. published the artcileFragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors, Application In Synthesis of 763120-58-7, the publication is Journal of Medicinal Chemistry (2015), 58(14), 5649-5673, database is CAplus and MEDLINE.

Overexpression of ATAD2 (ATPase family, AAA domain containing 2) has been linked to disease severity and progression in a wide range of cancers, and is implicated in the regulation of several drivers of cancer growth. Little is known of the dependence of these effects upon the ATAD2 bromodomain, which has been categorized as among the least tractable of its class. The absence of any potent, selective inhibitors limits clear understanding of the therapeutic potential of the bromodomain. Here, the authors describe the discovery of a hit from a fragment-based targeted array. Optimization of this produced the first known micromolar inhibitors of the ATAD2 bromodomain, e.g. I.

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, Application In Synthesis of 763120-58-7.

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

Demont, Emmanuel H. published the artcileFragment-Based Discovery of Low-Micromolar ATAD2 Bromodomain Inhibitors, HPLC of Formula: 724710-02-5, the publication is Journal of Medicinal Chemistry (2015), 58(14), 5649-5673, database is CAplus and MEDLINE.

Overexpression of ATAD2 (ATPase family, AAA domain containing 2) has been linked to disease severity and progression in a wide range of cancers, and is implicated in the regulation of several drivers of cancer growth. Little is known of the dependence of these effects upon the ATAD2 bromodomain, which has been categorized as among the least tractable of its class. The absence of any potent, selective inhibitors limits clear understanding of the therapeutic potential of the bromodomain. Here, the authors describe the discovery of a hit from a fragment-based targeted array. Optimization of this produced the first known micromolar inhibitors of the ATAD2 bromodomain, e.g. I.

Journal of Medicinal 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 C3H5BN2O2, HPLC of Formula: 724710-02-5.

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