Category: 20029-52-1

Jia, Li published the artcileSynthesis and antibacterial evaluation of novel 11-O-aralkylcarbamoyl-3-O-descladinosylclarithromycin derivatives, Application In Synthesis of 20029-52-1, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(14), 2471-2476, database is CAplus and MEDLINE.

A series of novel 11-O-aralkylcarbamoyl-3-O-descladinosylclarithromycin derivatives were designed, synthesized and evaluated for their in vitro antibacterial activity. The results showed that the majority of the target compounds displayed potent activity against erythromycin-susceptible S. pyogenes, erythromycin-resistant S. pneumoniae A22072 expressing the mef gene and S. pneumoniae AB11 expressing the mef and erm genes. Besides, most of the target compounds exhibited moderate activity against erythromycin-susceptible S. aureus ATCC25923 and B. subtilis ATCC9372. Title compounds exert favorable antibacterial activity against erythromycin-susceptible S. pyogenes with the MIC values of 0.015-0.125 μg/mL. Furthermore, title compounds showed superior activity against erythromycin-resistant S. pneumoniae A22072 with the MIC values of 0.25-0.5 μg/mL. Addnl., compound c was the most effective against all the erythromycin-resistant S. pneumoniae strains (A22072, B1 and AB11), exhibiting 8-, 8- and 32-fold more potent activity than clarithromycin, resp.

Bioorganic & Medicinal Chemistry Letters published new progress about 20029-52-1. 20029-52-1 belongs to quinuclidine, auxiliary class Carboxylic acid,Benzene, name is 4-Cyclohexylbenzoic acid, and the molecular formula is C13H16O2, Application In Synthesis of 20029-52-1.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Gawel, Justyna M. published the artcilePTG-0861: A novel HDAC6-selective inhibitor as a therapeutic strategy in acute myeloid leukaemia, Category: quinuclidine, the publication is European Journal of Medicinal Chemistry (2020), 112411, database is CAplus and MEDLINE.

Dysregulated Histone Deacetylase (HDAC) activity across multiple human pathologies have highlighted this family of epigenetic enzymes as critical druggable targets, amenable to small mol. intervention. While efficacious, current approaches using non-selective HDAC inhibitors (HDACi) have been shown to cause a range of undesirable clin. toxicities. To circumvent this, recent efforts have focused on the design of highly selective HDACi as a novel therapeutic strategy. Beyond roles in regulating transcription, the unique HDAC6 (with two catalytic domains) regulates the deacetylation of α-tubulin; promoting growth factor-controlled cell motility, cell division, and metastatic hallmarks. Recent studies have linked aberrant HDAC6 function in various hematol. cancers including acute myeloid leukemia and multiple myeloma. Herein, we report the discovery, in vitro characterization, and biol. evaluation of PTG-0861 (JG-265), a novel HDAC6-selective inhibitor with strong isoenzyme-selectivity (∼36x ) and low nanomolar potency (IC₅₀ = 5.92 nM) against HDAC6. This selectivity profile was rationalized via in silico docking studies and also observed in cellulo through cellular target engagement. Moreover, PTG-0861 achieved relevant potency against several blood cancer cell lines (e.g. MV4-11, MM1S), while showing limited cytotoxicity against non-malignant cells (e.g. NHF, HUVEC) and CD-1 mice. In examining compound stability and cellular permeability, PTG-0861 revealed a promising in vitro pharmacokinetic (PK) profile. Altogether, in this study we identified a novel and potent HDAC6-selective inhibitor (∼4x more selective than current clin. standards – citarinostat, ricolinostat), which achieves cellular target engagement, efficacy in hematol. cancer cells with a promising safety profile and in vitro PK.

European Journal of Medicinal Chemistry published new progress about 20029-52-1. 20029-52-1 belongs to quinuclidine, auxiliary class Carboxylic acid,Benzene, name is 4-Cyclohexylbenzoic acid, and the molecular formula is C13H16O2, Category: quinuclidine.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Kashida, Hiromu published the artcileInsulator base pairs for lighting-up perylenediimide in a DNA duplex, Related Products of quinuclidine, the publication is Chemistry – A European Journal (2010), 16(38), 11554-11557, S11554/1-S11554/18, database is CAplus and MEDLINE.

Perylenediimide (PDI) is highly quenched by nucleobases, which greatly restricts its application as a fluorescent probe. Here, the authors propose “insulator base pairs” tethering cyclohexane ring through D-threoninol. When “insulator base pairs” were inserted between PDI and nucleobases, the quantum yield of PDI drastically increased several thousand-fold. The “insulator base pairs” reported here also have the potential to increase the quantum yields of other fluorophores.

Chemistry – A European Journal published new progress about 20029-52-1. 20029-52-1 belongs to quinuclidine, auxiliary class Carboxylic acid,Benzene, name is 4-Cyclohexylbenzoic acid, and the molecular formula is C13H16O2, Related Products of quinuclidine.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Quattropani, Anna published the artcilePharmacophore-Based Design of Novel Oxadiazoles as Selective Sphingosine-1-phosphate (S1P) Receptor Agonists with in vivo Efficacy, Recommanded Product: 4-Cyclohexylbenzoic acid, the publication is ChemMedChem (2015), 10(4), 688-714, database is CAplus and MEDLINE.

Sphingosine-1-phosphate (S1P) receptor agonists have shown promise as therapeutic agents for multiple sclerosis (MS) due to their regulatory roles within the immune, central nervous system, and cardiovascular system. Here, the design and optimization of novel [1,2,4]oxadiazole derivatives as selective S1P receptor agonists are described. The structure-activity relation exploration was carried out on the three dominant segments of the series: modification of the polar head group (P), replacement of the oxadiazole linker (L) with different five-membered heterocycles, and the use of diverse 2,2′-disubstituted biphenyl moieties as the hydrophobic tail (H). All three segments have a significant impact on potency, S1P receptor subtype selectivity, physicochem. properties, and in vitro absorption, distribution, metabolism, excretion and toxicity (ADMET) profile of the compounds From these optimization studies, a selective S1P₁ agonist, N-methyl-N-(4-{5-[2-methyl-2′-(trifluoromethyl)biphenyl-4-yl]-1,2,4-oxadiazol-3-yl}benzyl)glycine (45), and a dual S1P_1,5 agonist, N-methyl-N-(3-{5-[2′-methyl-2-(trifluoromethyl)biphenyl-4-yl]-1,2,4-oxadiazol-3-yl}benzyl)glycine (49), emerged as frontrunners. These compounds distribute predominantly in lymph nodes and brain over plasma and induce long lasting decreases in lymphocyte count after oral administration. When evaluated head-to-head in an exptl. autoimmune encephalomyelitis mouse model, together with the marketed drug fingolimod, a pan-S1P receptor agonist, S1P_1,5 agonist 49 demonstrated comparable efficacy while S1P₁-selective agonist 45 was less potent. Compound 49 is not a prodrug, and its improved property profile should translate into a safer treatment of relapsing forms of MS.

ChemMedChem published new progress about 20029-52-1. 20029-52-1 belongs to quinuclidine, auxiliary class Carboxylic acid,Benzene, name is 4-Cyclohexylbenzoic acid, and the molecular formula is C13H16O2, Recommanded Product: 4-Cyclohexylbenzoic acid.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Sathyanarayana, Pochampalli published the artcileCopper catalyzed oxygen assisted C(CNOH)-C(alkyl) bond cleavage: a facile conversion of aryl/aralkyl/vinyl ketones to aromatic acids, SDS of cas: 20029-52-1, the publication is Organic & Biomolecular Chemistry (2015), 13(37), 9681-9685, database is CAplus and MEDLINE.

A novel copper-catalyzed aerobic oxidative C(NOH)-C(alkyl) bond cleavage reaction of aryl/aralkyl/vinyl ketones for the synthesis of aromatic/acrylic acids is described. A series of ketones having aryl/aralkyl/vinyl at the one end and Me to any higher alkyl at the other end can be selectively cleaved and converted into the corresponding acids via oxime intermediates.

Organic & Biomolecular Chemistry published new progress about 20029-52-1. 20029-52-1 belongs to quinuclidine, auxiliary class Carboxylic acid,Benzene, name is 4-Cyclohexylbenzoic acid, and the molecular formula is C13H16O2, SDS of cas: 20029-52-1.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Urlam, Murali K. published the artcileDevelopment of new N-arylbenzamides as STAT3 dimerization inhibitors, Computed Properties of 20029-52-1, the publication is MedChemComm (2013), 4(6), 932-941, database is CAplus and MEDLINE.

The O-tosylsalicylamide S3I-201 (10) was used as a starting point for design and synthesis of novel STAT-3 dimerization inhibitors with improved drug-like qualities. The phosphonic acid 12d and salicylic acids 13f, 13g with a shorter amide linker lacking the O-tosyl group had improved STAT-3 inhibitory activity. The equivalent potencies observed by the replacement of phosphonic acid moiety of 12d with 5-amino-2-hydroxybenzoic acid group as in 13f further validates 5-amino-2-hydroxybenzoic acid as a phosphotyrosine mimic. The salicylic acid 13f displayed improved whole cell activity. The focused library of salicylic acids 13 with benzamide linker indicated that hydrophobic heptyl and cyclohexyl are the best tolerated R groups and a biphenyl ether (as the Ar group) significantly contributes to STAT3 inhibitory activity. Our docking studies indicated that the acidic groups of 12d, 13f and 13g interact in the p-Tyr-705 binding site in a broadly similar manner, while the phenoxybenzoyl group and the cyclohexylbenzyl group occupying pY+1 and pY-X hydrophobic pockets resp. The in vitro and cell based potency of 13f warrants further development of this scaffold as STAT3 inhibitors.

MedChemComm published new progress about 20029-52-1. 20029-52-1 belongs to quinuclidine, auxiliary class Carboxylic acid,Benzene, name is 4-Cyclohexylbenzoic acid, and the molecular formula is C18H28B2O4, Computed Properties of 20029-52-1.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Koshel, S. G. published the artcileSynthesis of cyclohexylbenzoic acids by liquid-phase catalytic oxidation of cyclohexyltoluenes, Synthetic Route of 20029-52-1, the publication is Neftekhimiya (1989), 29(2), 257-61, database is CAplus.

Isomeric cyclohexyltoluenes were oxidized by mol. oxygen in glacial AcOH using Co(OAc)₂ as catalyst and AcH as initiator. The reactivity of the cyclohexyltoluene decreased in the order: p– > m– > o-isomer.

Neftekhimiya published new progress about 20029-52-1. 20029-52-1 belongs to quinuclidine, auxiliary class Carboxylic acid,Benzene, name is 4-Cyclohexylbenzoic acid, and the molecular formula is C13H16O2, Synthetic Route of 20029-52-1.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Wang, Yaxin published the artcileVisible-Light-Promoted Site-Specific and Diverse Functionalization of a C(sp³)-C(sp³) Bond Adjacent to an Arene, Synthetic Route of 20029-52-1, the publication is ACS Catalysis (2020), 10(12), 6603-6612, database is CAplus.

A strategy for inert C-C bond functionalization is reported. Site-specific cleavage and functionalization of saturated C(sp3)-C(sp3) bond via a visible-light-induced radical process was achieved. The general features of this reaction are: 1-Both linear and cyclic C(sp3)-C(sp3) bonds with a vicinal arene can be specifically functionalized; 2-One carbon is converted into ketone, and the another can be tunably converted into nitrile, peroxide or halide; 3-The typical conditions includes: 1.0 mol% Ru(bpy)3Cl2, 1.0 or 5.0 equiv of Zhdankin reagent, white CFL (24 W), open flask and room temperature These reactions offer a powerful tool to modify carbon skeletons that are intractable by conventional methods. Good selectivity and functional group tolerance, together with mild and open air conditions make these transformations valuable and attractive.

ACS Catalysis published new progress about 20029-52-1. 20029-52-1 belongs to quinuclidine, auxiliary class Carboxylic acid,Benzene, name is 4-Cyclohexylbenzoic acid, and the molecular formula is C9H10O3S, Synthetic Route of 20029-52-1.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Yang, Ya-Jun published the artcileDesign, synthesis and biological evaluation of dipeptides as novel non-covalent 20S proteasome inhibitors, Recommanded Product: 4-Cyclohexylbenzoic acid, the publication is Journal of Asian Natural Products Research (2021), 23(5), 436-451, database is CAplus and MEDLINE.

Based on the interaction modes of the natural 20S proteasome inhibitors , we have previously discovered a dipeptide . To explore the SAR around compound , we designed and synthesized a series of dipeptides () with a fragment-based strategy. Among them, nine compounds showed significant inhibitory activities against the chymotrypsin-like activity of human 20S proteasome with IC₅₀ values at the submicromolar level, which were comparable or even superior to the parent compound Meanwhile, they displayed no significant inhibition against trypsin-like and caspase-like activities of 20S proteasome. The results suggested the feasibility to design dipeptides as novel and potent 20S proteasome inhibitors.

Journal of Asian Natural Products Research published new progress about 20029-52-1. 20029-52-1 belongs to quinuclidine, auxiliary class Carboxylic acid,Benzene, name is 4-Cyclohexylbenzoic acid, and the molecular formula is C12H14IN, Recommanded Product: 4-Cyclohexylbenzoic acid.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider

Li, Jian-Jun published the artcileCu-Catalyzed C-H Alkenylation of Benzoic Acid and Acrylic Acid Derivatives with Vinyl Boronates, Application of 4-Cyclohexylbenzoic acid, the publication is Organic Letters (2020), 22(12), 4692-4696, database is CAplus and MEDLINE.

An efficient Cu-catalyzed C-H alkenylation with acyclic and cyclic vinyl boronates was realized for the first time under mild conditions. The scope of the vinyl borons and the compatibility with functional groups including heterocycles are superior than Pd-catalyzed C-H coupling with vinyl borons, providing a reliable access to multisubstituted alkenes and dienes. Subsequent hydrogenation of the product from the internal vinyl borons will lead to installation of secondary alkyls.

Organic Letters published new progress about 20029-52-1. 20029-52-1 belongs to quinuclidine, auxiliary class Carboxylic acid,Benzene, name is 4-Cyclohexylbenzoic acid, and the molecular formula is C13H16O2, Application of 4-Cyclohexylbenzoic acid.

Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider