Tag: M.W=100-150

Manley, Peter J. published the artcile2,4-Disubstituted pyrimidines: A novel class of KDR kinase inhibitors, Safety of 4-Amino-2-picoline, the publication is Bioorganic & Medicinal Chemistry Letters (2003), 13(10), 1673-1677, database is CAplus and MEDLINE.

2,4-Disubstituted pyrimidines were synthesized as a novel class of KDR kinase inhibitors. Evaluation of the SAR of the screening lead compound I (R = H) (KDR IC₅₀=105 nM, Cell IC₅₀=8% inhibition at 500 nM) led to the potent 3,5-dimethylaniline derivative I (R = Me) (KDR IC₅₀=6 nM, cell IC₅₀=19 nM).

Bioorganic & Medicinal Chemistry Letters published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, Safety of 4-Amino-2-picoline.

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

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

Bandarage, Upul K. published the artcileDiscovery of a Novel Series of Potent and Selective Alkynylthiazole-Derived PI3Kγ Inhibitors, Product Details of C8H7NO, the publication is ACS Medicinal Chemistry Letters (2021), 12(1), 129-135, database is CAplus and MEDLINE.

Phosphoinositide 3-kinases (PI3Ks) are a family of enzymes that control a wide variety of cellular functions such as cell growth, proliferation, differentiation, motility, survival, and intracellular trafficking. PI3Kγ plays a critical role in mediating leukocyte chemotaxis as well as mast cell degranulation, making it a potentially interesting target for autoimmune and inflammatory diseases. We previously disclosed a novel series of PI3Kγ inhibitors derived from a benzothiazole core. The truncation of the benzothiazole core led to the discovery of a structurally diverse alkynyl thiazole series which displayed high PI3Kγ potency and subtype selectivity. Further medicinal chem. optimization of the alkynyl thiazole series led to identification of compounds such as 14 and 32, highly potent, subtype selective, and CNS penetrant PI3Kγ inhibitors. Compound 14 showed robust inhibition of PI3Kγ mediated neutrophil migration in vivo.

ACS Medicinal Chemistry Letters published new progress about 1060816-39-8. 1060816-39-8 belongs to pyridine-derivatives, auxiliary class Pyridines, name is 4-Ethynyl-2-methoxypyridine, and the molecular formula is C8H7NO, Product Details of C8H7NO.

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

Rombouts, Frederik J. R. published the artcileDiscovery of N-(Pyridin-4-yl)-1,5-naphthyridin-2-amines as Potential Tau Pathology PET Tracers for Alzheimer’s Disease, Recommanded Product: 4-Amino-2-picoline, the publication is Journal of Medicinal Chemistry (2017), 60(4), 1272-1291, database is CAplus and MEDLINE.

A mini-HTS on 4000 compounds selected using 2D fragment-based similarity and 3D pharmacophoric and shape similarity to known selective tau aggregate binders identified N-(6-methylpyridin-2-yl)quinolin-2-amine 10 as a novel potent binder to human AD aggregated tau with modest selectivity vs. aggregated β-amyloid (Aβ). Initial medicinal chem. efforts identified key elements for potency and selectivity, as well as suitable positions for radiofluorination, leading to a first generation of fluoroalkyl-substituted quinoline tau binding ligands with suboptimal physicochem. properties. Further optimization toward a more optimal pharmacokinetic profile led to the discovery of 1,5-naphthyridine 75, a potent and selective tau aggregate binder with potential as a tau PET tracer.

Journal of Medicinal Chemistry published new progress about 18437-58-6. 18437-58-6 belongs to pyridine-derivatives, auxiliary class Pyridine,Amine, name is 4-Amino-2-picoline, and the molecular formula is C6H8N2, Recommanded Product: 4-Amino-2-picoline.

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