pyrazoles-derivatives

Lizarzaburu, Mike published the artcileDiscovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus, SDS of cas: 724710-02-5, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(18), 5942-5947, database is CAplus and MEDLINE.

N-alkylphenylalaninamides of pyridinylphenyl- and oxobipyridinylamines such as I were prepared as GPR142 agonists for potential use as antidiabetic agents for type 2 diabetes and tested for their agonism of GPR142 in vitro and in human plasma and their inhibition of cytochrome P 450 enzymes such as isoforms 3A4 and 2D6. Optimization of the original lead compound gave agonists 90 times more potent against human GPR142. Inhibition of cytochrome P 450 isoforms 3A4 and 2D6 was reduced by increasing the polarity of the biarylamine moiety. The pharmacokinetics of I and a thiazolylmethyl phenylalaninamide of an aminopyridinylbenzoate were determined in rats.

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, SDS of cas: 724710-02-5.

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

Faust, Thomas B. published the artcileControlling magnetic communication through aromatic bridges by variation in torsion angle, Formula: C8H7N3, the publication is Dalton Transactions (2012), 41(44), 13626-13631, database is CAplus and MEDLINE.

Heteroaromatic bridging ligands (L, e.g., 4,4′-bipyridine) are employed in the synthesis of a family of paramagnetic, heterometallic ring dimers derived from {Cr₇Ni(N-Et-D-glucamine)F₃(O₂CCMe₃)₁₅(H₂O)}, to give [{Cr₇Ni(N-Et-D-glucamine)F₃(O₂CCMe₃)₁₅}₂L]. The extent of spin propagation between the rings via the organic conduit was studied through micro-SQUID magnetometry and EPR spectroscopy from which conclusions over the mechanism of spin-communication are drawn.

Dalton Transactions 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 C8H7N3, Formula: C8H7N3.

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

Lu, Rong-Jian published the artcileDesign and Synthesis of Human Immunodeficiency Virus Entry Inhibitors: Sulfonamide as an Isostere for the α-Ketoamide Group, Safety of (1H-Pyrazol-5-yl)boronic acid, the publication is Journal of Medicinal Chemistry (2007), 50(26), 6535-6544, database is CAplus and MEDLINE.

The crystal structures of many tertiary α-ketoamides reveal an orthogonal arrangement of the two carbonyl groups. Based on the hypothesis that the α-ketoamide HIV attachment inhibitor BMS 806 (formally BMS378806, 26) might bind to its gp120 target via a similar conformation, we designed and synthesized a series of analogs in which the ketoamide group is replaced by an isosteric sulfonamide group. The most potent of these analogs, 14i (I), demonstrated antiviral potency comparable to 26 in the M33 pseudotyped antiviral assay. Flexible overlay calculations of a ketoamide inhibitor with a sulfonamide inhibitor revealed a single conformation of each that gave significantly better overlap of key pharmacophore features than other conformations and thus suggest a possible binding conformation for each class.

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, Safety of (1H-Pyrazol-5-yl)boronic acid.

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

Lu, Rong-Jian published the artcileHeterobiaryl Human Immunodeficiency Virus Entry Inhibitors, Formula: C3H5BN2O2, the publication is Journal of Medicinal Chemistry (2009), 52(14), 4481-4487, database is CAplus and MEDLINE.

Previously disclosed HIV (human immunodeficiency virus) attachment inhibitors, exemplified by BMS 806 (formally BMS 378806), are characterized by a substituted indole or azaindole ring linked to a benzoylpiperazine via a ketoamide or sulfonamide group. In the present report, we describe the discovery of a novel series of potent HIV entry inhibitors in which the indole or azaindole ring of previous inhibitors is replaced by a heterobiaryl group. Several of these analogs exhibited IC₅₀ values of less than 5 nM in a pseudotyped antiviral assay, and a methylisoxazolylphenyloxoacetyl piperazine was demonstrated to exhibit potency and selectivity similar to those of BMS 378806 against a panel of clin. viral isolates. Moreover, current structure-activity relation studies of these novel biaryl gp120 inhibitors revealed that around the biaryl, a fine crevice might exist in the gp120 binding site. Taken in sum, these data reveal a hitherto unsuspected flexibility in the structure-activity relationships for these inhibitors and suggest new avenues for exploration and gp120 inhibitor design.

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, Formula: C3H5BN2O2.

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

Arkhipova, Anna Alexandrovna published the artcileSorbents with non-covalently immobilized β-diketones for preconcentration of rare earth elements, HPLC of Formula: 4551-69-3, the publication is Talanta (2016), 497-502, database is CAplus and MEDLINE.

A comparison of the efficiency of sorbents obtained by different methods of non-covalent immobilization of β-diketones on some low-polar matrixes with respect to extraction of rare earth elements (REEs) was carried out. Sorbents containing reagent amounts of 1-8 mmol/g can be obtained by sorption of reagents on low-polar matrixes from aqueous and aqueous-organic solutions, and the value for the maximum capacity of the sorbent correlates with the sp. surface of the matrix. Similar sorbents were also prepared by impregnating the matrix with reagent. It was found out that, under the chosen conditions, sorbents modified by extracting reagent from the aqueous solutions are more stable and extract lanthanum with higher distribution coefficients than those obtained by impregnation. We have found conditions for quant. extraction of REEs from seawater in the proposed preconcentration systems (pH 4.0, minicolumn dimensions 2×10 mm, v=4 mL/min). All REE may be quant. recovered in both ways: on modified sorbents and as complexes with reagents on unmodified matrixes. We have proposed a sorbent for lanthanum preconcentration from large volumes of water samples (500 mL). The sorbent is stable in dynamic conditions and is based on hyper cross-linked polystyrene modified with 1-phenyl-3-methyl-4-benzoylpyrazol-5-one (PMBP). Desorption could be carried out with 1-2 M HNO₃. REEs were determined by ICP-MS, LODs achieved were in ng/l range.

Talanta 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, HPLC of Formula: 4551-69-3.

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

Kharbanda, Anupreet published the artcileDiscovery of 4-aminoquinolines as highly selective TGFβR1 inhibitors with an attenuated MAP4K4 profile for potential applications in immuno-oncology, Formula: C3H5BN2O2, the publication is European Journal of Medicinal Chemistry (2021), 113763, database is CAplus and MEDLINE.

The tumor microenvironment contains high concentrations of TGFβ, a crucial immunosuppressive cytokine. TGFβ stimulates immune escape by promoting peripheral immune tolerance to avoid tumoricidal attack. Small-mol. inhibitors of TGFβR1 are a prospective method for next-generation immunotherapies. In the present study, we identified selective 4-aminoquinoline-based inhibitors of TGFβR1 through structural and rational-based design strategies. This led to the identification of [N-(2-(2,5-difluorophenyl)pyridin-4-yl)-7-(4-(methylsulfonyl)phenyl)quinolin-4-amine], which was found to be selective for TGFβR1 with the exception of MAP4K4 in the kinase profiling assay. The compound was then further optimized to remove MAP4K4 activity, since MAP4K4 is vital for proper T-cell function and its inhibition could exacerbate tumor immunosuppression. Optimization efforts led to [7-(4-(methylsulfonyl)phenyl)-N-(2-(m-tolyl)pyridin-4-yl)quinolin-4-amine] that inhibited TGFβR1 at an IC₅₀ of 0.79 ± 0.19 nM with 2000-fold selectivity against MAP4K4. 7-(4-(Methylsulfonyl)phenyl)-N-(2-(m-tolyl)pyridin-4-yl)quinolin-4-amine, represents a highly selective TGFβR1 inhibitor that has potential applications in immuno-oncol.

European 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, Formula: C3H5BN2O2.

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

Berger, Dan M. published the artcileNon-hinge-binding pyrazolo[1,5-a]pyrimidines as potent B-Raf kinase inhibitors, Safety of 1H-Pyrazole-4-boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2009), 19(23), 6519-6523, database is CAplus and MEDLINE.

As part of our research effort to discover B-Raf kinase inhibitors, we prepared a series of C-3 substituted N-(3-(pyrazolo[1,5-a]pyrimidin-7-yl)phenyl)-3-(trifluoromethyl)benzamides. X-ray crystallog. studies revealed that one of the more potent inhibitors bound to B-Raf kinase without forming a hinge-binding hydrogen bond. With basic amine residues appended to C-3 aryl residues, cellular activity and solubility were enhanced over previously described compounds of this class.

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, Safety of 1H-Pyrazole-4-boronic acid.

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

Sun, Wen-Qing published the artcileProgrammable Self-Assembly of Heterometallic Palladium(II)-Copper(II) 1D Grid-Chain using Dinuclear Palladium(II) Corners with Pyrazole-Carboxylic Acid Ligands, Product Details of C8H7N3, the publication is Chemistry – An Asian Journal (2018), 13(9), 1108-1113, database is CAplus and MEDLINE.

A novel heterometallic diPd^II-diCu^II grid-chain, {[(bpy)₄Pd₄Cu₂L₄](NO₃)₄}_n (2; bpy = 2,2′-bipyridine), was synthesized through a programmable self-assembly approach from the mol. corners [(bpy)₂Pd₂(HL)(L)](NO₃) (1) as linkers with Cu^II nitrate by using the bifunctional H₂L ligand 4-(3,5-dimethyl-1H-pyrazol-4-yl)benzoic acid featuring primary (pyrazole) and secondary (HOBz) groups. Structural anal. revealed that 1-dimensional structure 2 consists of one [Cu₂(O₂CPh)₄]_n unit as a bridge and two [(bpy)₂Pd₂L₂]_n corners. Addnl., the catalytic effect of the heterometallic synergy on the Suzuki coupling reaction by using 2 was further explored.

Chemistry – An Asian Journal 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 C8H13NO3, Product Details of C8H7N3.

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

Simov, D. published the artcileAzo dye from 10-methyl-2-aminophenothiazine, Safety of 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone, the publication is Godishnik na Sofiiskiya Universitet Sv. Kliment Okhridski, Khimicheski Fakultet (1975), 543-54, database is CAplus.

Azo dyes (I, R = pyrazolone, hydroxynaphthalene, aniline, aminonaphthalene residues) were prepared by coupling diazotized 2-amino-10-methylphenothiazine [2031-24-5] with RH and dyed protein and synthetic fibers wetfast and, in some cases, lightfast shades. All dyes were characterized by elementary anal., m.p., visible, uv, and ir spectra, and Rf. In I where R is not a pyrazolone residue the equilibrium between the azo enol form and the quinone hydrazone form is fully shifted to the azo enol form.

Godishnik na Sofiiskiya Universitet Sv. Kliment Okhridski, Khimicheski Fakultet 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 C8H17Br, Safety of 1-(2-Chlorophenyl)-3-methyl-5-pyrazolone.

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

Kajita, Harutake published the artcileA Oxidative Bromination of (Hetero)Arenes in the TMSBr/DMSO System: A Non-Aqueous Procedure Facilitates Synthetic Strategies, Formula: C4H6N2, the publication is ChemistrySelect (2017), 2(3), 1117-1121, database is CAplus.

An oxidative bromination protocol for aromatic compounds using trimethylsilyl bromide (TMSBr) and DMSO has been developed. This mild bromination system tolerates a wide variety of functionalities including amide, aldehyde, ester and acetal groups. Arylbromides and heteroarylbromides are produced in up to 95 % yield at 25°. Arenes bearing electron-donating groups are selectively brominated at the para position unless it is blocked. The highlight of this protocol consists in its non-aqueous conditions, which are fruitful particularly in the context of integrated synthetic systems. The utility of this method was demonstrated with three examples, in either of which the bromination was followed by another reaction: a “click” triazole formation, a Suzuki-Miyaura cross-coupling, or an aldehyde formation via lithium-bromine exchange, without the isolation of the bromide intermediate in any case. It is particularly remarkable for this non-aqueous protocol to allow lithiation reactions to sequentially follow the bromination.

ChemistrySelect 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, Formula: C4H6N2.

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