Tag: M.W=100-150

Desroy, Nicolas published the artcileNovel HldE-K Inhibitors Leading to Attenuated Gram Negative Bacterial Virulence, Recommanded Product: (1H-Pyrazol-5-yl)boronic acid, the publication is Journal of Medicinal Chemistry (2013), 56(4), 1418-1430, database is CAplus and MEDLINE.

The optimization of an HldE kinase inhibitor to low nanomolar potency is reported here, which resulted in the identification of the first reported compounds active on selected Escherichia coli strains. One of the most interesting candidates, compound 86, was shown to inhibit specifically bacterial LPS heptosylation on efflux pump deleted E. coli strains. This compound did not interfere with E. coli bacterial growth (MIC > 32 μg/mL) but sensitized this pathogen to hydrophobic antibiotics like macrolides normally inactive on Gram-neg. bacteria. In addition, 86 could sensitize E. coli to serum complement killing. These results demonstrate that HldE kinase is a suitable target for drug discovery. They also pave the way toward novel possibilities of treating or preventing bloodstream infections caused by pathogenic Gram-neg. bacteria by inhibiting specific virulence factors.

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, Recommanded Product: (1H-Pyrazol-5-yl)boronic acid.

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

Latha, Ganesapandian published the artcileNickel-catalyzed oxidative hydroxylation of arylboronic acid: Ni(HBTC)BPY MOF as an efficient and ligand-free catalyst to access phenolic motifs, SDS of cas: 763120-58-7, the publication is Catalysis Communications, database is CAplus.

A straightforward and mild oxidative ipso-hydroxylation of arylboronic acids was achieved using a simple and non-noble metal, nickel-based reusable heterogeneous catalyst Ni(HBTC)BPY MOF (HBTC = benzene-1,3,5-tricarboxylate, BPY = 4,4′-bipyridine) in the presence of benign hydrogen peroxide as an oxidant under ambient reaction condition. The Ni(HBTC)BPY MOF exhibited excellent catalytic activity towards the formation of phenols from diverse arylboronic acids within short time and was reused up to five times without any notable loss in its activity as well as shown high functional group tolerance even in the presence of sensitive functionalities and useful to achieve hydroxyl group in heterocycles.

Catalysis Communications 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, SDS of cas: 763120-58-7.

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

Dorn, Helmut published the artcileElectrophilic substitution of 3(5)-aminopyrazole, HPLC of Formula: 3553-12-6, the publication is Justus Liebigs Annalen der Chemie (1967), 141-6, database is CAplus.

3(5)-Aminopyrazole (I) was halogenated to give 3(5)-amino-4-halopryazole. Acetylation of I yielded 3(5)-acetamidopyrazole (II), as shown by ir spectroscopy. II was nitrated to give 3(5)-acetamido-4-nitropyrazole, resp. The tautomerism of I and the site of the preferred electrophilic substitution are discussed based on the N.M.R. spectra.

Justus Liebigs Annalen der Chemie published new progress about 3553-12-6. 3553-12-6 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Amine,Amide, name is 3-Acetamidopyrazole, and the molecular formula is C5H7N3O, HPLC of Formula: 3553-12-6.

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

Remya, Chandran published the artcileNeuroprotective derivatives of tacrine that target NMDA receptor and acetyl cholinesterase – Design, synthesis and biological evaluation, Recommanded Product: (1H-Pyrazol-5-yl)boronic acid, the publication is Computational and Structural Biotechnology Journal (2021), 4517-4537, database is CAplus and MEDLINE.

An novel high affinity multi-target directed ligands (MTDLs) against AChE and NMDAR, with reduced hepatotoxicity, performed in-silico structure-based modifications on tacrine, chem. synthesis of the derivatives and in-vitro validation of their activities. Nineteen such derivatives I [R = H, methylcarbamoyl, hydrazinecarbonyl, ethoxycarbonyl; R¹ = 2-furanyl, 1-methylpyrazol-4-yl, 2-FC₆H₄, etc.] showed inhibition with IC₅₀ values in the range of 18.53 ± 2.09 – 184.09 ± 19.23 nM against AChE and 0.27 ± 0.05 – 38.84 ± 9.64μM against NMDAR. Some of the selected compounds protected rat primary cortical neurons from glutamate induced excitotoxicity. Two of the tacrine derived MTDLs, I [R = H, R¹ = 1-methylpyrazol-4-yl; R = H, R¹ = 2-FC₆H₄] exhibited in-vivo efficacy in rats by protecting against behavioral impairment induced by administration of the excitotoxic agent, monosodium glutamate. Addnl., several of these synthesized compounds also exhibited promising inhibitory activitiy against butyrylcholinesterase. MTDL-201 I [R = H, R¹ = 1-methylpyrazol-4-yl] was also devoid of hepatotoxicity in-vivo. Given the therapeutic potential of MTDLs in disease-modifying therapy, studies revealed several promising MTDLs among which I [R = H, R¹ = 1-methylpyrazol-4-yl] appeared to be a potential candidate for immediate preclin. evaluations.

Computational and Structural Biotechnology Journal 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, Recommanded Product: (1H-Pyrazol-5-yl)boronic acid.

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

Rheault, Tara R. published the artcileHeteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: Potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties, Product Details of C3H5BN2O2, the publication is Bioorganic & Medicinal Chemistry Letters (2010), 20(15), 4587-4592, database is CAplus and MEDLINE.

Potent inhibitors of PLK1 with acceptable solubility, mouse iv clearance, and reduced CYP450 inhibition were identified. Drug-like properties were improved using a heteroaryl ring as a functional handle for manipulation of inhibitors’ physiochem. and DMPK properties.

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, Product Details of C3H5BN2O2.

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

Lu, Chunliang published the artcileRegioselective Bromination of Thieno[2′,3′:4,5]pyrrolo[1,2-d][1,2,4]triazin-8(7H)-one and Sequential Suzuki Couplings, Quality Control of 763120-58-7, the publication is Journal of Organic Chemistry (2017), 82(17), 9229-9234, database is CAplus and MEDLINE.

Regioselective bromination of 5-methylthieno[2′,3′:4,5]pyrrolo[1,2-d][1,2,4]triazin-8(7H)-one (I) at 2 or 9-position was achieved by modulating the basicity of the reaction conditions. An anion directed site-specific bromination mechanism was proposed. In addition, a one-pot bromination-Suzuki coupling protocol was developed for quick access of analogs at 9-position, II [Ar = Ph, C₆H₄F-4, C₆H₄Cl-4, C₆H₄(CF₃)-4, C₆H₄OMe-4, C₆H₄Me-3, C₆H₄Me-2, 1-methylpyrazin-4-yl, thien-2-yl, pyridin-3-yl].

Journal of Organic 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, Quality Control 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

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

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

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