Category: quinuclidine

Cheng, Jin-tao published the artcileSynthesis of 1-(mercaptomethyl)cyclopropane acetic acid, Related Products of quinuclidine, the publication is Guangzhou Huagong (2010), 38(6), 92-93, database is CAplus.

1-(Mercaptomethyl) cyclopropane acetic acid, the key intermediate of montelukast, was prepared from 1,1-bis(hydroxymethyl)cyclopropane by ring-formation reaction, cyanation reaction, esterification reaction, aldol reaction, and hydrolytic reaction, with 49.5% overall yield.

Guangzhou Huagong published new progress about 162515-68-6. 162515-68-6 belongs to quinuclidine, auxiliary class Thiol,Carboxylic acid,Aliphatic cyclic hydrocarbon, name is 2-(1-(Mercaptomethyl)cyclopropyl)acetic acid, and the molecular formula is C6H10O2S, Related Products of quinuclidine.

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

Ke, Li-na published the artcileInhibitory effects of benzoic acid and its derivatives on the polyphenoloxidase from the 5^th instar of Pieris rapae L., Recommanded Product: 4-Cyclohexylbenzoic acid, the publication is Xiamen Daxue Xuebao, Ziran Kexueban (2004), 43(6), 856-860, database is CAplus.

The polyphenoloxidase (PPO) is more responsible for enzymic browning during the growth of the insects. It also is involved in the defense reaction and has some certain relation with the immune condition of the insects. The polyphenoloxidase is a metalloenzyme oxidase which catalyzes two distinct reactions of melanin synthesis the hydroxylation of a monophenol and the oxidation of ωmi-diphenol to the corresponding ωmi-quinone. A great number of benzoic acid family compounds can inhibit the enzyme activity for the oxidation of L-DOPA. In the present paper, partial characteristics and inhibitory kinetics of polyphenoloxidase (PPO) from the 5^th instar of Pieris rapae L. were studied. The results show that benzoic acid, p-cyanobenzoic acid, p-hydroxybenzoic acid and p-cyclohexylbenzoic acid were chosen as inhibitors of PPO for the oxidation of L-DOPA. The reactions of these inhibitors with the PPO are reversible with remaining enzyme activity. The IC₅₀ (the inhibitor concentrations leading to 50% activity lost) were estimated to be 14.2, 16.1, 11.3 and 2.1 mmol/L, resp. The inhibitory mechanisms of p-hydroxybenzoic acid is competitive, p-cyanobenzoic acid belongs to be a mixed typed inhibitor while the others are noncompetitive inhibitors. Obviously, p-cyanobenzoic acid is the best inhibitor among the four compounds, so it may have the bright prospect in the future as the biocide.

Xiamen Daxue Xuebao, Ziran Kexueban 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

Costanzo, Michael J. published the artcilePotent, nonpeptide inhibitors of human mast cell tryptase. Investigation of the carboxamide portion of spirocyclic piperidine amides, Quality Control of 20029-52-1, the publication is Letters in Drug Design & Discovery (2008), 5(2), 116-121, database is CAplus.

The authors have explored a series of spirocyclic piperidine amide derivatives with respect to the N-acyl portion (viz. 6) for inhibition of tryptase. Thus, the authors identified analogs (I and II) as potent tryptase inhibitors (IC₅₀ < 10 nM) with excellent selectivity vs. trypsin. Four other interesting compounds in this chem. series had IC₅₀ = 10-20 nM. X-ray cocrystal structures of tryptase complexes with spirocyclic piperidine amides are reported.

Letters in Drug Design & Discovery 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, Quality Control of 20029-52-1.

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

Manabe, Shino published the artcileCharacterization of Antibody Products Obtained through Enzymatic and Nonenzymatic Glycosylation Reactions with a Glycan Oxazoline and Preparation of a Homogeneous Antibody-Drug Conjugate via Fc N-Glycan, COA of Formula: C19H15NO3, the publication is Bioconjugate Chemistry (2019), 30(5), 1343-1355, database is CAplus and MEDLINE.

Glycan engineering of antibodies has received considerable attention. Although various endo-β-N-acetylglucosaminidase mutants have been developed for glycan remodeling, a side reaction has been reported between glycan oxazoline and amino groups. In this study, we performed a detailed characterization for antibody products obtained through enzymic and nonenzymic reactions with the aim of maximizing the efficiency of the glycosylation reaction with fewer side products. The reactions were monitored by an ultraperformance liquid chromatog. system using an amide-based wide-pore column. The products were characterized by liquid chromatog. coupled with tandem mass spectrometry. The side reactions were suppressed by adding glycan oxazoline in a stepwise manner under slightly acidic conditions. Through a combination of an azide-carrying glycan transfer reaction under optimized conditions and a bio-orthogonal reaction, a potent cytotoxic agent monomethyl auristatin E was site-specifically conjugated at N-glycosylated Asn297 with a drug-to-antibody ratio of 4. The prepared antibody-drug conjugate exhibited cytotoxicity against HER2-expressing cells.

Bioconjugate Chemistry published new progress about 1353016-70-2. 1353016-70-2 belongs to quinuclidine, auxiliary class Other Aromatic Heterocyclic,Carboxylic acid,Amide,Inhibitor,Inhibitor, name is Dbco-acid, and the molecular formula is C19H15NO3, COA of Formula: C19H15NO3.

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

Roam, Jacob L. published the artcileA modular, plasmin-sensitive, clickable poly(ethylene glycol)-heparin-laminin microsphere system for establishing growth factor gradients in nerve guidance conduits, HPLC of Formula: 1353016-70-2, the publication is Biomaterials (2015), 112-124, database is CAplus and MEDLINE.

Peripheral nerve regeneration is a complex problem that, despite many advancements and innovations, still has sub-optimal outcomes. Compared to biol. derived acellular nerve grafts and autografts, completely synthetic nerve guidance conduits (NGC), which allow for precise engineering of their properties, are promising but still far from optimal. We have developed an almost entirely synthetic NGC that allows control of soluble growth factor delivery kinetics, cell-initiated degradability and cell attachment. We have focused on the spatial patterning of glial-cell derived human neurotrophic factor (GDNF), which promotes motor axon extension. The base scaffolds consisted of heparin-containing poly(ethylene glycol) (PEG) microspheres. The modular microsphere format greatly simplifies the formation of concentration gradients of reversibly bound GDNF. To facilitate axon extension, we engineered the microspheres with tunable plasmin degradability. ‘Click’ crosslinking chemistries were also added to allow scaffold formation without risk of covalently coupling the growth factor to the scaffold. Cell adhesion was promoted by covalently bound laminin. GDNF that was released from these microspheres was confirmed to retain its activity. Graded scaffolds were formed inside silicone conduits using 3D-printed holders. The fully formed NGC’s contained plasmin-degradable PEG/heparin scaffolds that developed linear gradients in reversibly bound GDNF. The NGC’s were implanted into rats with severed sciatic nerves to confirm in vivo degradability and lack of a major foreign body response. The NGC’s also promoted robust axonal regeneration into the conduit.

Biomaterials published new progress about 1353016-70-2. 1353016-70-2 belongs to quinuclidine, auxiliary class Other Aromatic Heterocyclic,Carboxylic acid,Amide,Inhibitor,Inhibitor, name is Dbco-acid, and the molecular formula is C19H15NO3, HPLC of Formula: 1353016-70-2.

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

Chaudhari, Chandan published the artcileOne-pot synthesis of cyclohexylamine and N-aryl pyrroles via hydrogenation of nitroarenes over the Pd_0.5Ru_0.5-PVP catalyst, Category: quinuclidine, the publication is New Journal of Chemistry (2021), 45(22), 9743-9746, database is CAplus.

The direct synthesis of cyclohexylamine via the hydrogenation of nitrobenzene over monometallic (Pd, Ru or Rh) and bimetallic (Pd_xRu_1-x) catalysts was studied. The Pd_0.5Ru_0.5-PVP catalyst was the most effective catalyst for this reaction. The catalyst can be reused and applied for the synthesis of N-aryl pyrroles I (R = Ph, 4-chlorophenyl, pyridin-3-yl, etc.) and quinoxalines such as 2,3-diphenylquinoxaline and 2,3-diphenyl-1,2,3,4-tetrahydroquinoxaline from nitrobenzenes RNO₂.

New Journal of Chemistry published new progress about 1761-71-3. 1761-71-3 belongs to quinuclidine, auxiliary class Ploymers, name is 4,4-Diaminodicyclohexyl methane, and the molecular formula is C13H26N2, Category: 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

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

Zhang, H. J. published the artcileEffect of Free-Volume Hole Fraction on Dynamic Mechanical Properties of Epoxy Resins Investigated by Pressure-Volume-Temperature Technique, COA of Formula: C13H26N2, the publication is Journal of Physical Chemistry B (2020), 124(9), 1824-1832, database is CAplus and MEDLINE.

Dynamic mech. anal. experiments were carried out to investigate the mech. properties of four types of chem. different epoxy resins. Pressure-volume-temperature (PVT) experiments were performed to determine the free-volume hole fraction (h_PVT) of each epoxy resin using the Simha-Somcynsky lattice-hole theory. Using the Williams-Landel-Ferry equation, the correlations between the relative hole fraction (1 – h_PVT^T_r/h_PVT, where h_PVT^T_r is the hole fraction at a reference temperature T_r) and four typical parameters reflecting dynamic mech. properties [storage modulus (E’), loss modulus (E”), damping factor (tanδ), and complex viscosity (|η*|)] were studied at from T_g(PVT) (the glass transition temperature determined by PVT data) to T_g(PVT) + 100°C. At from T_g(Eonset‘₎ (temperature corresponding to the intersection of the two tangent fitting lines in the E'(T) curve indicating the glassy-state and glass-transition stages) to T_g(PVT) + 100°C, the variations in the four dynamic mech. parameters with a relative hole fraction could be separated into two distinct categories: (i) log[E'(T)] and log[|η*|(T)] decreased linearly to their min. values and then remained nearly unchanged with increasing relative hole fraction, and (ii) log[E”(T)] and log[tanδ(T)] first increased monotonically to their maximum values and then decreased linearly with the increasing relative hole fraction. This study demonstrates that the PVT technique is a feasible and reliable exptl. method to determine the hole fractions of thermoset polymers.

Journal of Physical Chemistry B published new progress about 1761-71-3. 1761-71-3 belongs to quinuclidine, auxiliary class Ploymers, name is 4,4-Diaminodicyclohexyl methane, and the molecular formula is 0, COA of Formula: C13H26N2.

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

Zhang, H. J. published the artcileEffect of free-volume holes on static mechanical properties of epoxy resins studied by positron annihilation and PVT experiments, Quality Control of 1761-71-3, the publication is Polymer (2020), 122225pp., database is CAplus.

The tensile, flexural, and fracture toughness properties of seven chem. different amine-cured epoxy resins were studied. Positron annihilation lifetime and pressure-volume-temperature (PVT) experiments were performed on each epoxy resin to characterize the average size and fraction, resp., of free-volume holes. A neg. correlation between hole fraction and hole size was revealed for these chem. different epoxy resins. Better tensile and flexural mech. properties (higher tensile modulus and lower tensile strain at break; higher flexural modulus, higher flexural strength, and lower flexural strain at break) were clearly observed for epoxy resins with smaller hole size and higher hole fraction. However, no clear relationship between fracture toughness and hole properties was found. The correlations between (tensile and flexural) static mech. properties and hole properties for chem. different epoxy resins should provide guidance for further improvements in the mech. properties of carbon fiber-reinforced polymers.

Polymer published new progress about 1761-71-3. 1761-71-3 belongs to quinuclidine, auxiliary class Ploymers, name is 4,4-Diaminodicyclohexyl methane, and the molecular formula is C18H20N2O12, Quality Control of 1761-71-3.

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