Category: 1877-71-0

Bollenbach, Maud published the artcileDesign and synthesis of 3-aminophthalazine derivatives and structural analogues as PDE5 inhibitors: anti-allodynic effect against neuropathic pain in a mouse model, Product Details of C9H8O4, the publication is European Journal of Medicinal Chemistry (2019), 269-290, database is CAplus and MEDLINE.

Herein, a series of aminophthalazine I [R = H, Ph, 1-piperidyl, etc.; R¹ = H, CF₃; R² = 3-ClC₆H₄NH, 4-MeOC₆H₄CH₂NH, Ph(CH₂)₂NH, etc.] and aminoindazole derivatives II [R³ = H, Cl, CF₃; R⁴ = H, Me, Ph, etc.; R⁵ = 3-ClC₆H₄, 4-MeOC₆H₄CH₂, 3-F-4-MeOC₆H₃CH₂, etc.] were synthesized and evaluated for their inhibitory activity toward PDE5. Selectivity profiles towards other PDE1-4 isoenzymes, water solubility and stability in acidic medium of the most potent PDE5 inhibitors were determined and the aminophthalazine I [R = Ph, R¹ = CF₃, R² = 4-OMeC₆H₄CH₂NH] and its mimetic compound II [R³ = CF₃, R⁴ = 3-pyridyl, R⁵ = 4-OMeC₆H₄CH₂NH] were evaluated in comparison to MY 5445 in vivo in a model of neuropathic pain induced by sciatic nerve cuffing in mice (3 and 0.5 mg/kg, i.p. twice a day). Both compounds showed the same efficacy on neuropathic allodynia as MY 5445 and thus produced a significant relief of mech. hypersensitivity after 12 days of treatment.

European Journal of Medicinal Chemistry published new progress about 1877-71-0. 1877-71-0 belongs to esters-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Ester, name is 3-(Methoxycarbonyl)benzoic acid, and the molecular formula is C9H8O4, Product Details of C9H8O4.

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

Zhou, Yi published the artcileDiscovery of Peptide Boronate Derivatives as Histone Deacetylase and Proteasome Dual Inhibitors for Overcoming Bortezomib Resistance of Multiple Myeloma, SDS of cas: 1877-71-0, the publication is Journal of Medicinal Chemistry (2020), 63(9), 4701-4715, database is CAplus and MEDLINE.

While proteasome inhibitors such as bortezomib showed satisfactory clin. benefits in the initial treatment of multiple myeloma (MM), drug resistance and relapse are unavoidable. Recent studies suggested inhibition of histone deacetylases (HDACs) restored sensitivity of bortezomib-resistant MM. Hence, we designed dual inhibitors targeting both HDACs and proteasomes to address the resistance of bortezomib. The most potent inhibitors, ZY-2 and ZY-13 showed excellent inhibition against proteasome and good selectivity against HDACs. In particular, ZY-2 not only exhibited good antiproliferative activities on the MM cell lines RPMI-8226, U266, and KM3 (IC₅₀ values of 6.66, 4.31, and 10.1 nM, resp.) but also showed more potent antiproliferative activities against the bortezomib-resistant MM cell line KM3/BTZ compared with bortezomib (IC₅₀ values of 8.98 vs. 226 nM, P < 0.01) and even better than the combination of the HDAC inhibitor MS-275 and bortezomib (1:1) (IC₅₀ values of 8.98 vs. 98.0 nM, P < 0.01).

Journal of Medicinal Chemistry published new progress about 1877-71-0. 1877-71-0 belongs to esters-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Ester, name is 3-(Methoxycarbonyl)benzoic acid, and the molecular formula is C3H10ClNS, SDS of cas: 1877-71-0.

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

Zeng, Zhongyi published the artcile2,2′-Biaryldicarboxylate Synthesis via Electrocatalytic Dehydrogenative C-H/C-H Coupling of Benzoic Acids, Synthetic Route of 1877-71-0, the publication is ACS Catalysis (2021), 11(11), 6626-6632, database is CAplus.

2,2′-Biaryldicarboxylates are important functionalities in bioactive compounds, functional materials, and chiral catalysts. These compounds have been found to be conveniently accessible from benzoic acids via Rh-catalyzed electrooxidative C-H/C-H couplings, giving valuable dihydrogen as the byproduct. In an undivided cell with Pt electrodes, RhCl₃·3H₂O catalyzes the oxidative carboxylate-directed ortho-homocoupling of various aromatic acids with a current efficiency of 67%. The protocol is operationally simple, tolerates a wide variety of functional groups, and does not require the exclusion of air and moisture. Heterodimerizations via cross-dehydrogenative couplings of naphthyl-1-carboxylic acids with acrylic or benzoic acids were also shown to work.

ACS Catalysis published new progress about 1877-71-0. 1877-71-0 belongs to esters-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Ester, name is 3-(Methoxycarbonyl)benzoic acid, and the molecular formula is C6H9N3, Synthetic Route of 1877-71-0.

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

Joshi, Sumedh published the artcileMenaquinone Biosynthesis: New Strategies to Trap Radical Intermediates in the MqnE-Catalyzed Reaction, HPLC of Formula: 1877-71-0, the publication is Biochemistry (2021), 60(21), 1642-1646, database is CAplus and MEDLINE.

Aminofutalosine synthase (MqnE) is a radical SAM enzyme that catalyzes the conversion of 3-((1-carboxyvinyl)oxy)benzoic acid to aminofutalosine during the futalosine-dependent menaquinone biosynthesis. In this Communication, the authors report the trapping of a radical intermediate in the MqnE-catalyzed reaction using sodium dithionite, mol. oxygen, or 5,5-dimethyl-1-pyrroline-N-oxide. These radical trapping strategies are potentially of general utility in the study of other radical SAM enzymes.

Biochemistry published new progress about 1877-71-0. 1877-71-0 belongs to esters-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Ester, name is 3-(Methoxycarbonyl)benzoic acid, and the molecular formula is C9H8O4, HPLC of Formula: 1877-71-0.

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

Joshi, Sumedh published the artcileAntibacterial Strategy against H. pylori: Inhibition of the Radical SAM Enzyme MqnE in Menaquinone Biosynthesis, Category: esters-buliding-blocks, the publication is ACS Medicinal Chemistry Letters (2019), 10(3), 363-366, database is CAplus and MEDLINE.

Aminofutalosine synthase (MqnE) catalyzes an important rearrangement reaction in menaquinone biosynthesis by the futalosine pathway. We report the identification of previously unreported inhibitors of MqnE using a mechanism-guided approach. The best inhibitor shows efficient inhibitory activity against Helicobacter pylori (IC₅₀ = 1.8 ± 0.4 μM) and identifies MqnE as a promising target for antibiotic development.

ACS Medicinal Chemistry Letters published new progress about 1877-71-0. 1877-71-0 belongs to esters-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Ester, name is 3-(Methoxycarbonyl)benzoic acid, and the molecular formula is C9H8O4, Category: esters-buliding-blocks.

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

Fang, Kun published the artcileDiscovery of Novel Indoleamine 2,3-Dioxygenase 1 (IDO1) and Histone Deacetylase (HDAC) Dual Inhibitors, Application In Synthesis of 1877-71-0, the publication is ACS Medicinal Chemistry Letters (2018), 9(4), 312-317, database is CAplus and MEDLINE.

In order to take advantage of both immunotherapeutic and epigenetic antitumor agents, the first generation of dual indoleamine 2,3-dioxygenase 1 (IDO1) and histone deacetylase (HDAC) inhibitors were designed. The highly active dual inhibitor 10 showed excellent and balanced activity against both IDO1 (IC₅₀ = 69.0 nM) and HDAC1 (IC₅₀ = 66.5 nM), whose dual targeting mechanisms were validated in cancer cells. Compound 10 had good pharmacokinetic profiles as an orally active antitumor agent and significantly reduced the L-kynurenine level in plasma. In particular, it showed excellent in vivo antitumor efficacy in the murine LLC tumor model with low toxicity. This proof-of-concept study provided a novel strategy for cancer treatment. Compound 10 represents a promising lead compound for the development of novel antitumor agents and can also be used as a valuable probe to clarify the relationships and mechanisms between cancer immunotherapy and epigenetics.

ACS Medicinal Chemistry Letters published new progress about 1877-71-0. 1877-71-0 belongs to esters-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Ester, name is 3-(Methoxycarbonyl)benzoic acid, and the molecular formula is C9H8O4, Application In Synthesis of 1877-71-0.

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

Bera, Sourav Sekhar published the artcileCp*Co^III-Catalyzed syn-Selective C-H Hydroarylation of Alkynes Using Benzamides: An Approach Toward Highly Conjugated Organic Frameworks, Application of 3-(Methoxycarbonyl)benzoic acid, the publication is Journal of Organic Chemistry (2017), 82(1), 420-430, database is CAplus and MEDLINE.

Hydroarylation of internal alkynes by cost effective CoIII-catalysis, directed by N-tert-Bu amides, is achieved to avail mono- or di-hydroarylated amide products selectively in an atom and step economic way. Several important functional groups were tolerated the reaction conditions, and syn-hydroarylation products were exclusively isolated. Notably, a fourfold C-H hydroarylation provided a highly conjugated organic framework (I) in one step. Kinetic study with extensive deuterium labeling experiments were performed to support the proposed mechanism.

Journal of Organic Chemistry published new progress about 1877-71-0. 1877-71-0 belongs to esters-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Ester, name is 3-(Methoxycarbonyl)benzoic acid, and the molecular formula is C9H8O4, Application of 3-(Methoxycarbonyl)benzoic acid.

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

Diego, Rosa published the artcileDesigned asymmetric coordination helicates with bis-β-diketonate ligands, Recommanded Product: 3-(Methoxycarbonyl)benzoic acid, the publication is Dalton Transactions (2019), 48(45), 16844-16847, database is CAplus and MEDLINE.

A new bis-(β-diketone) ligand featuring built-up structural asymmetry yields non-sym. Fe(III) and Ga(III) dinuclear, triple-stranded helicates by design. Their structural properties have been studied, both in solid state and in solution, and compared with their corresponding sym. analogs. The robustness observed shows the potential of this synthetic strategy to develop non-sym. helicoidal motifs with specific functional groups.

Dalton Transactions published new progress about 1877-71-0. 1877-71-0 belongs to esters-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Ester, name is 3-(Methoxycarbonyl)benzoic acid, and the molecular formula is C9H8O4, Recommanded Product: 3-(Methoxycarbonyl)benzoic acid.

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

Kwak, Se Hun published the artcileN-Aminopyridinium Ylide-Directed, Copper-Promoted Amination of sp² C-H Bonds, Quality Control of 1877-71-0, the publication is Journal of Organic Chemistry (2019), 84(20), 13022-13032, database is CAplus and MEDLINE.

N-Aminopyridinium ylides were used as monodentate directing groups for copper-promoted C-H/N-H coupling of sp² C-H bonds with pyrazoles, imidazoles, and sulfonamides. Reactions proceed in fluorinated alc. solvents at elevated temperatures and require use of 1.3-3 equiv of copper(II) acetate. This appears to be the first method for copper-promoted C-H/N-H coupling directed by a removable monodentate auxiliary in absence of added ligands.

Journal of Organic Chemistry published new progress about 1877-71-0. 1877-71-0 belongs to esters-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Ester, name is 3-(Methoxycarbonyl)benzoic acid, and the molecular formula is C9H8O4, Quality Control of 1877-71-0.

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

Kwak, Se Hun published the artcileN-Iminopyridinium ylide-directed, cobalt-catalysed coupling of sp² C-H bonds with alkynes, HPLC of Formula: 1877-71-0, the publication is Chemical Communications (Cambridge, United Kingdom) (2020), 56(75), 11070-11073, database is CAplus and MEDLINE.

N-Iminopyridinium ylides were competent monodentate directing groups for cobalt-catalyzed annulation of sp² C-H bonds with internal alkynes. The pyridine moiety in the ylide serves as an internal oxidant and was cleaved during the reaction. The annulation reactions possess excellent compatibility with heterocyclic substrates, tolerating furan, thiophene, pyridine, pyrrole, pyrazole, and indole functionalities.

Chemical Communications (Cambridge, United Kingdom) published new progress about 1877-71-0. 1877-71-0 belongs to esters-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Ester, name is 3-(Methoxycarbonyl)benzoic acid, and the molecular formula is C9H8O4, HPLC of Formula: 1877-71-0.

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