Category: 197958-29-5

Yang, Christine published the artcileDiscovery of Benzimidazole Oxazolidinediones as Novel and Selective Nonsteroidal Mineralocorticoid Receptor Antagonists, Safety of 2-Pyridinylboronic acid, the publication is ACS Medicinal Chemistry Letters (2015), 6(4), 461-465, database is CAplus and MEDLINE.

Elaboration of the oxazolidinedione series led to replacement of the exocyclic amides with substituted benzimidazoles. The structure-activity relationship exploration resulted in the discovery of potent and selective nonsteroidal mineralocorticoid receptor antagonists with significantly improved microsomal stability and pharmacokinetic profile relative to the HTS hit. One compound I possessed comparable efficacy as spironolactone at 100 mg/kg (p.o.) in the rat natriuresis model. As such, this series was validated as a lead series for further optimization.

ACS Medicinal Chemistry Letters published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C19H14Cl2, Safety of 2-Pyridinylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Romagnoli, Romeo published the artcileSynthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A₁ adenosine receptor, Application In Synthesis of 197958-29-5, the publication is Bioorganic & Medicinal Chemistry (2014), 22(1), 148-166, database is CAplus and MEDLINE.

2-Amino-3-benzoyl thiophenes have been widely reported to act as allosteric enhancers at the A₁ adenosine receptor. Their activity can be increased considerably by appropriate substitutions at the 4- and 5-positions of the thiophene ring. Substituent size at the thiophene C-4 position seemed to be a factor closely related to activity, with the 4-neopentyl (2,2-dimethylpropyl) substitution showing the greatest enhanced activity. A wide series of 2-amino-3-aroyl-4-neopentylthiophene derivatives with general structure I, characterized by the presence of different substituents (bromine, aryl and heteroaryl) at the 5-position of the thiophene ring, have been identified as potent AEs at the A₁AR. With only one exception, all of the synthesized compounds proved to be superior to the reference compound PD 81,723 in a functional assay. Derivatives I (R = Ph, R¹ = 4-Me; R = 4-OMePh, R¹ = 4-Me; R = 3-OMePh, R¹ = 4-Cl; R = 3,4-(O-CH₂-O)Ph, R¹ = 4-Cl; and R = 4-MePh, R¹ = 4-Cl) were the most active compounds in binding (saturation and competition) and functional cAMP studies, being able to potentiate agonist [³H]CCPA binding to the A₁ receptor.

Bioorganic & Medicinal Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Application In Synthesis of 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Zipp, G. Greg published the artcileNovel inhibitors of the high-affinity L-proline transporter as potential therapeutic agents for the treatment of cognitive disorders, Computed Properties of 197958-29-5, the publication is Bioorganic & Medicinal Chemistry Letters (2014), 24(16), 3886-3890, database is CAplus and MEDLINE.

The incidence of cognitive disorders such as Alzheimer’s disease continues to increase unabated. While cures for such diseases have eluded investigators, progress is being made on alleviating certain symptoms of these diseases. Mouse knockouts of the proline transporter (PROT), a high affinity Na⁺/Cl^–-dependent transporter, indicated its potential as a novel therapeutic target for cognition improvement. Herein we report our investigation into a novel class of PROT inhibitors.

Bioorganic & Medicinal Chemistry Letters published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C11H10O, Computed Properties of 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Guay, Daniel published the artcileSynthesis and SAR of pyrimidine-based, non-nucleotide P2Y₁₄ receptor antagonists, SDS of cas: 197958-29-5, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(10), 2832-2835, database is CAplus and MEDLINE.

A weak antagonist of the pyrimidinergic receptor P2Y₁₄ containing a dihydropyridopyrimidine core was identified through high-throughput screening. Subsequent optimization led to potent, non-UTP competitive antagonists and represent the first reported non-nucleotide antagonists of this receptor. Dihydropyridopyrimidine I was identified as a 10 nM P2Y₁₄ antagonist with good oral bioavailability and provided sufficient exposure in mice to be used as a tool for future in vivo studies.

Bioorganic & Medicinal Chemistry Letters published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, SDS of cas: 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Shao, Ning published the artcileSynthesis and structure-activity relationship (SAR) study of 4-azabenzoxazole analogues as H₃ antagonists, Related Products of pyridine-derivatives, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(5), 2075-2078, database is CAplus and MEDLINE.

The synthesis and SAR of a novel series of 4-azabenzoxazole histamine H₃ antagonists is described. Introduction of substituted Ph, pyridyl, and fused heterocyclic groups to the 6-position of the 4-azabenzoxazole core gave a series of compounds with good H₃ antagonist activity in both ex vivo and in vivo assays.

Bioorganic & Medicinal Chemistry Letters published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C13H19Br2ClN2O, Related Products of pyridine-derivatives.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Konda, Yesuraju published the artcileSynthesis, Alpha-Glucosidase Inhibition and Antibacterial Activities of the New Chiral (R)-3,3′-Disubstituted BINOL-Phosphates, Formula: C5H6BNO2, the publication is Russian Journal of General Chemistry (2022), 92(5), 898-907, database is CAplus.

A new class of 3,3′-disubstituted chiral (R)-BINOL-derived phosphoric acid derivatives has been prepared The synthetic method has been optimized by involving Pd/C as a catalyst in the Suzuki-Miyaura cross coupling using a non-protected BINOL derivative The target compounds have been characterized and tested for their α-glucosidase inhibitory and antibacterial activities.

Russian Journal of General Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Formula: C5H6BNO2.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Chatterjee, Nachiketa published the artcileA Metal and Base-Free Chemoselective Primary Amination of Boronic Acids Using Cyanamidyl/Arylcyanamidyl Radical as Aminating Species: Synthesis and Mechanistic Studies by Density Functional Theory, Recommanded Product: 2-Pyridinylboronic acid, the publication is Journal of Organic Chemistry (2016), 81(12), 5120-5127, database is CAplus and MEDLINE.

An efficient, metal and base-free, chemoselective synthesis of aryl-, heteroaryl-, and alkyl primary amines from the corresponding boronic acids has been achieved at ambient temperature mediated by [bis(trifluoroacetoxy)iodo]benzene (PIFA) and N-bromosuccinimide (NBS) using cyanamidyl/arylcyanamidyl radicals as the aminating species. The primary amine compounds were initially obtained as their corresponding ammonium trifluoroacetate salts which, on treatment with aq NaOH, provide the free amines. Finally, the primary amines were isolated through column chromatog. over silica-gel using hexane-EtOAc solvent system as the eluent. The reactions are sufficiently fast, completing within 1 h. Quantum chem. calculations in combination with exptl. observations validate that the ipso amination of substituted boronic acids involves the formation of cyanamidyl/arylcyanamidyl radical, followed by regiospecific interaction of its nitrile-N center with boron atom of the boronic acids, leading to chemoselective primary amination.

Journal of Organic Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Recommanded Product: 2-Pyridinylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Ontoria, Jesus M. published the artcileIdentification of Novel, Selective, and Stable Inhibitors of Class II Histone Deacetylases: Validation Studies of the Inhibition of the Enzymatic Activity of HDAC4 by Small Molecules as a Novel Approach for Cancer Therapy, Synthetic Route of 197958-29-5, the publication is Journal of Medicinal Chemistry (2009), 52(21), 6782-6789, database is CAplus and MEDLINE.

5-Aryl-2-(trifluoroacetyl)thiophenes were identified as a new series of class II HDAC inhibitors (HDACi). Further development of this new series led to compounds such as 6h(I), a potent inhibitor of HDAC4 and HDAC6 (HDAC4 WT IC₅₀ = 310 nM, HDAC6 IC₅₀ = 70 nM) that displays 40-fold selectivity over HDAC1 and improved stability in HCT116 cancer cells (t₁/₂ = 11 h). Compounds 6h and 2(II) show inhibition of α-tubulin deacetylation in HCT116 cells at 1 μM concentration and antiproliferation effects only at concentrations where inhibition of histone H3 deacetylation is observed

Journal of Medicinal Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Synthetic Route of 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Sayed, Ahmed M. published the artcileArylpyrazole as selective anti-enterococci; synthesis and biological evaluation of novel derivatives for their antimicrobial efficacy, HPLC of Formula: 197958-29-5, the publication is Journal of Heterocyclic Chemistry, database is CAplus.

Condensation of the 1-(1-[4-substituted aryl]phenyl-5-methyl-1H-pyrazol-4-yl)ethan-1-ones with the aminoguanidinehydrochloride gave target compounds 2-(1-(1-(4-[aryl or alkyl] phenyl)-5-methyl-1Hpyrazol-4-yl)ethylidene)hydrazine-1-carboximidamides I [R = Ph, Bn, 4-MeC₆H₄, etc.]. Exploring the structure-activity relationships (SAR) of a new set of phenylpyrazoles I [R = Ph, Bn, 4-MeC₆H₄, etc.] unveiled a potential anti-enterococcus lead compound I [R = benzofuran-2-yl]. The benzofuran moiety linked to the phenylpyrazole I [R = benzofuran-2-yl] was 32 times better than vancomycin against Enterococcus fecalis ATCC 51299. Besides, compound I [R = benzofuran-2-yl] is expected to have an excellent oral bioavailability according to the in silico studies. In SAR anal., it was found that the benzofuran side chain was essential for the activity. Changing the benzofuran with either benzothiophene, Ph, pyridinyl, tolyl, or naphthyl reduces/nullifies the pharmacol. action. Besides the anti-enterococcal activity, derivatives I [R = furan-2-yl, Ph] could be used to develop new broad-spectrum antibiotics as they exhibited activity against the wild-type highly virulent Escherichia coli isolate. Moreover, compound I [R = benzothiophen-2-yl] was proved to show antifungal activity (MIC = 4 μg/mL) against the Candida albicans SS5314 (wild type).

Journal of Heterocyclic Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, HPLC of Formula: 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem

Duroux, Romain published the artcileAntagonists of the adenosine A_2A receptor based on a 2-arylbenzoxazole scaffold: Investigation of the C5- and C7-positions to enhance affinity, Application In Synthesis of 197958-29-5, the publication is European Journal of Medicinal Chemistry (2018), 151-163, database is CAplus and MEDLINE.

The authors have recently reported a series of 2-furoyl-benzoxazoles as potential A_2A adenosine receptor (A_2AR) antagonists. Two hits were identified with interesting pharmacokinetic properties but were find to bind the hA_2AR receptor in the micromolar-range. Herein, to enhance affinity toward the hA_2AR, the authors explored the C5- and C7-position of the hits based on docking studies. These modifications led to compounds with nanomolar-range affinity (e.g., 6a (2,7-di(furan-2-yl)benzoxazol-5-amine), Ki = 40 nM) and high antagonist activity (e.g., 6a, IC₅₀ = 70.6 nM). Selected compounds also exhibited interesting in vitro DMPK (Drug Metabolism and Pharmacokinetics) properties including high solubility and low cytotoxicity. Therefore, the benzoxazole ring appears as a highly effective scaffold for the design of new A_2A antagonists.

European Journal of Medicinal Chemistry published new progress about 197958-29-5. 197958-29-5 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester, name is 2-Pyridinylboronic acid, and the molecular formula is C5H6BNO2, Application In Synthesis of 197958-29-5.

Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem