Author: tianli

Salaciak, Kinga published the artcileSynthesis and evaluation of the antidepressant-like properties of HBK-10, a novel 2-methoxyphenylpiperazine derivative targeting the 5-HT1A and D2 receptors, Application In Synthesis of 96-20-8, the publication is Pharmaceuticals (2021), 14(8), 744, database is CAplus and MEDLINE.

The increasing number of patients reporting depressive symptoms requires the design of new antidepressants with higher efficacy and limited side effects. As our previous research showed, 2-methoxyphenylpiperazine derivatives are promising candidates to fulfill these criteria. In this study, we aimed to synthesize a novel 2-methoxyphenylpiperazine derivative, HBK-10, and investigate its in vitro and in vivo pharmacol. profile. After assessing the affinity for serotonergic and dopaminergic receptors, and serotonin transporter, we determined intrinsic activity of the compound at the 5-HT1A and D2 receptors. Next, we performed behavioral experiments (forced swim test, tail suspension test) to evaluate the antidepressant-like activity of HBK-10 in naive and corticosterone-treated mice. We also assessed the safety profile of the compound We showed that HBK-10 bound strongly to 5-HT1A and D2 receptors and presented antagonistic properties at these receptors in the functional assays. HBK-10 displayed the antidepressant-like effect not only in naive animals, but also in the corticosterone-induced mouse depression model, i.e., chronic administration of HBK-10 reversed corticosterone-induced changes in behavior. Moreover, the compound′s sedative effect was observed at around 26-fold higher doses than the antidepressant-like ones. Our study showed that HBK-10 displayed a favorable pharmacol. profile and may represent an attractive putative treatment candidate for depression.

Pharmaceuticals published new progress about 96-20-8. 96-20-8 belongs to alcohols-buliding-blocks, auxiliary class Amine,Aliphatic hydrocarbon chain,Alcohol, name is 2-Aminobutan-1-ol, and the molecular formula is C4H11NO, Application In Synthesis of 96-20-8.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Jain, Isha published the artcileIndium(III)-Catalyzed Synthesis of Primary Carbamates and N-Substituted Ureas, Related Products of alcohols-buliding-blocks, the publication is Synlett (2022), 33(1), 93-97, database is CAplus.

An indium triflate-catalyzed synthesis of primary carbamates RXC(O)NH₂ [R = i-Bu, Bn, Ph, etc.; X= O, N] from alcs. and urea as an ecofriendly carbonyl source was developed. Various linear, branched, and cyclic alcs. were converted into the corresponding carbamates in good to excellent yields. This method also provided access to N-substituted ureas by carbamoylation of amines. All the products were obtained by simple filtration or crystallization, without the need for chromatog. purification Mechanistic investigations suggested that the carbamoylation reaction proceeded through activation of urea by O-coordination with indium, followed by nucleophilic attack by the alc. or amine on the carbonyl center of urea. The inexpensive and easily available starting materials and catalyst, the short reaction times, and the ease of product isolation highlighted the inherent practicality of the developed method.

Synlett published new progress about 111-29-5. 111-29-5 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic hydrocarbon chain,Alcohol,Ploymers, name is Pentane-1,5-diol, and the molecular formula is C5H12O2, Related Products of alcohols-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Lamani, Manjunath published the artcilePiperidine and piperazine inhibitors of fatty acid amide hydrolase targeting excitotoxic pathology, Product Details of C10H13NO2, the publication is Bioorganic & Medicinal Chemistry (2019), 27(23), 115096, database is CAplus and MEDLINE.

FAAH inhibitors offer safety advantages by augmenting the anandamide levels “on demand” to promote neuroprotective mechanisms without the adverse psychotropic effects usually seen with direct and chronic activation of the CB1 receptor. FAAH is an enzyme implicated in the hydrolysis of the endocannabinoid N-arachidonoylethanolamine (AEA), which is a partial agonist of the CB1 receptor. Herein, we report the discovery of a new series of highly potent and selective carbamate FAAH inhibitors and their evaluation for neuroprotection. The new inhibitors showed potent nanomolar inhibitory activity against human recombinant and purified rat FAAH, were selective (>1000-fold) against serine hydrolases MGL and ABHD6 and lacked any affinity for the cannabinoid receptors CB1 and CB2. Evaluation of FAAH inhibitors 9(I) and 31(II) using the in vitro competitive activity-based protein profiling (ABPP) assay confirmed that both inhibitors were highly selective for FAAH in the brain, since none of the other FP-reactive serine hydrolases in this tissue were inhibited by these agents. Our design strategy followed a traditional SAR approach and was supported by mol. modeling studies based on known FAAH cocrystal structures. To rationally design new mols. that are irreversibly bound to FAAH, we have constructed “precovalent” FAAH-ligand complexes to identify good binding geometries of the ligands within the binding pocket of FAAH and then calculated covalent docking poses to select compounds for synthesis. FAAH inhibitors I and II were evaluated for neuroprotection in rat hippocampal slice cultures. In the brain tissue, both inhibitors displayed protection against synaptic deterioration produced by kainic acid-induced excitotoxicity. Thus, the resultant compounds produced through rational design are providing early leads for developing therapeutics against seizure-related damage associated with a variety of disorders.

Bioorganic & Medicinal Chemistry published new progress about 27292-49-5. 27292-49-5 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Benzene,Phenol, name is 3-Morpholinophenol, and the molecular formula is C10H13NO2, Product Details of C10H13NO2.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Nakamura, Masaharu published the artcileDevelopment of silicon-containing bis-phenol derivatives as androgen receptor antagonists: Selectivity switching by C/Si exchange, SDS of cas: 57044-25-4, the publication is Bioorganic & Medicinal Chemistry (2013), 21(7), 1643-1651, database is CAplus and MEDLINE.

The authors previously reported that bis-phenol derivatives, including LG190178, possess not only vitamin D receptor (VDR) agonistic activity, but also androgen receptor (AR) antagonistic activity. Here, the authors describe the design, synthesis and evaluation of silicon-containing bis-phenol derivatives, with the objective of obtaining increased selectivity toward VDR or AR. The authors found that replacement of the quaternary carbon in the bis-phenol skeleton with silicon increased AR-antagonistic activity and reduced VDR-agonistic activity, i.e., the AR selectivity of the silicon-containing compounds was higher than that of corresponding carbon compounds To the authors’ knowledge, this is the first report of nuclear receptor (NR) selectivity switching by sila-substitution (C/Si exchange). Among the compounds synthesized, AR-selective ligand (I) exhibited more potent anti-androgenic activity (IC₅₀ = 0.072 μM) than hydroxyflutamide, a well-known androgen antagonist (IC₅₀ = 1.4 μM), in SC-3 cell proliferation assay. These results suggest that sila-substitution is a useful approach for structural development of selective AR ligands.

Bioorganic & Medicinal Chemistry published new progress about 57044-25-4. 57044-25-4 belongs to alcohols-buliding-blocks, auxiliary class Epoxides,Chiral,Aliphatic hydrocarbon chain,Alcohol, name is (R)-Oxiran-2-ylmethanol, and the molecular formula is C3H6O2, SDS of cas: 57044-25-4.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Chatterjee, Sayanti published the artcileHydroxylamine-Derived Reagent as a Dual Oxidant and Amino Group Donor for the Iron-Catalyzed Preparation of Unprotected Sulfinamides from Thiols, Computed Properties of 4410-99-5, the publication is Angewandte Chemie, International Edition (2021), 60(2), 758-765, database is CAplus and MEDLINE.

An iron catalyzed reaction for the selective transformation of thiols (-SH) to sulfinamides (-SONH₂) by a direct transfer of -O and free -NH₂ groups has been developed. The reaction operates under mild conditions using a bench stable hydroxylamine derived reagent, exhibits broad functional group tolerance, is scalable and proceeds without the use of any precious metal catalyst or addnl. oxidant. This novel, practical reaction leads to the formation of two distinct new bonds (S=O and S-N) in a single step to chemoselectively form valuable, unprotected sulfinamide products. Preliminary mechanistic studies implicate the role of the alc. solvent as an oxygen atom donor.

Angewandte Chemie, International Edition published new progress about 4410-99-5. 4410-99-5 belongs to alcohols-buliding-blocks, auxiliary class Thiol,Benzene, name is 2-Phenylethanethiol, and the molecular formula is C8H10S, Computed Properties of 4410-99-5.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Dindarloo Inaloo, Iman published the artcileN-Arylation of (hetero)arylamines using aryl sulfamates and carbamates via C-O bond activation enabled by a reusable and durable nickel(0) catalyst, Safety of Thiophen-3-ol, the publication is New Journal of Chemistry (2020), 44(31), 13266-13278, database is CAplus.

An effective and general aryl amination protocol has been developed using a magnetically recoverable Ni(0) based nanocatalyst. This new stable catalyst was prepared on Fe₃O₄@SiO₂ modified by EDTA and investigated by FT-IR, EDX, TEM, XRD, DLS, FE-SEM, XPS, NMR, TGA, VSM, ICP and elemental anal. techniques. The reaction proceeded via carbon-oxygen bond cleavage of (hetero)aryl carbamates and sulfamates under simple and mild conditions without the use of any external ligands. This method demonstrated functional group tolerance in the N-arylation of various nitrogen-containing compounds as well as aliphatic amines, anilines, pyrroles, pyrazoles, imidazoles, indoles, and indazoles with good to excellent yields. Furthermore, the catalyst could be easily recovered by using an external magnetic field and directly reused at least six times without notable reduction in its activity.

New Journal of Chemistry published new progress about 17236-59-8. 17236-59-8 belongs to alcohols-buliding-blocks, auxiliary class Thiophene,Alcohol, name is Thiophen-3-ol, and the molecular formula is C4H4OS, Safety of Thiophen-3-ol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Horie, Masaki published the artcileCyclopentadithiophene based polymers; a comparison of optical, electrochemical and organic field-effect transistor characteristics, SDS of cas: 239075-02-6, the publication is Journal of Materials Chemistry (2010), 20(21), 4347-4355, database is CAplus.

A series of cyclopentadithiophene based polymers have been synthesized by oxidative polymerization or palladium-catalyzed coupling reactions. Polymers have been prepared with backbones containing benzothiadiazole, benzoxadiazole, 2,2′-bithiophene, Ph and fluorene units. The backbone structure is shown to have a large effect on the film morphol., and the optical and electrochem. properties in solution and the solid state. We show that the polymer composition can be used to tune the band gap over the entire visible spectrum. Spin-coated films of these polymers have been used as the active layer of organic field effect transistors and hole mobilities up to 3.7 × 10^-3 cm² V^-1 s^-1 have been measured under ambient conditions.

Journal of Materials Chemistry published new progress about 239075-02-6. 239075-02-6 belongs to alcohols-buliding-blocks, auxiliary class Thiophene,Boronic acid and ester,Boronate Esters, name is 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, and the molecular formula is C20H28B2O4S2, SDS of cas: 239075-02-6.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Tomic, L. published the artcileTris(dipivaloyemethanato)holmium induced NMR shifts, Recommanded Product: 1-Methylcyclobutan-1-ol, the publication is Croatica Chemica Acta (1971), 267-9, database is CAplus.

The NMR of 1-methylcyclobutanol and 1-octanol were studied by means of complexes of Ho and Pr with 2,2,6,6-tetramethyl-3,5-heptanedione (DPM). The complex Ho(DPM)3 is a more powerful NMR shift reagent than Eu(DPM)3 and Pr(DPM)3, but introduces considerably stronger line broadening, spin-spin splittings being observable only for the most distant protons from the coordination site.

Croatica Chemica Acta published new progress about 20117-47-9. 20117-47-9 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic cyclic hydrocarbon,Alcohol, name is 1-Methylcyclobutan-1-ol, and the molecular formula is C17H18N2O6, Recommanded Product: 1-Methylcyclobutan-1-ol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Vorcakova, Katarina published the artcileSynthesis and characterization of new inhibitors of cholinesterases based on N-phenylcarbamates: In vitro study of inhibitory effect, type of inhibition, lipophilicity and molecular docking, Formula: C12H20O6, the publication is Bioorganic Chemistry (2018), 280-289, database is CAplus and MEDLINE.

Based on current treatment of Alzheimer’s disease, where the carbamate inhibitor Rivastigmine is used, two series of carbamate derivatives were prepared: (i) N-phenylcarbamates with addnl. carbamate group and (ii) N-phenylcarbamates with monosaccharide moiety. All compounds were tested for the inhibitory effect on both of the cholinesterases, elec. eel acetylcholinesterase (eeAChE) and butyrylcholinesterase from equine serum (eqBChE) and the inhibitory activity (expressed as IC₅₀ values) was compared with that of the established drugs Galanthamine and Rivastigmine. The compounds with two carbamate groups revealed higher inhibitory efficiency on both cholinesterases in compared with monosaccharide derived carbamates and with Rivastigmine. The significant decrease of inhibitory efficiency on eqBChE (also for eeAChE but in less manner) was observed after deacetalization of monosaccharide. Moreover, the type of inhibitory mechanism of five chosen compounds was studied. It was found, that compounds with two carbamate groups act presumably via a mixed inhibitory mechanism and the compounds with monosaccharide moiety act as noncompetitive inhibitors. The lipophilicity of tested compounds was determined using partition coefficient Specific positions of the inhibitors in the binding sites of cholinesterases were determined using mol. modeling and the results indicate the importance of phenylcarbamate orientation in the catalytic gorges of both enzymes.

Bioorganic Chemistry published new progress about 20880-92-6. 20880-92-6 belongs to alcohols-buliding-blocks, auxiliary class Other Aliphatic Heterocyclic,Chiral,Alcohol, name is ((3aS,5aR,8aR,8bS)-2,2,7,7-Tetramethyltetrahydro-3aH-bis([1,3]dioxolo)[4,5-b:4′,5′-d]pyran-3a-yl)methanol, and the molecular formula is C8H10S, Formula: C12H20O6.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts

Jana, Rabindranath published the artcileStructural transition dynamics of biologically active flavins in alkylglucoside surfactants aggregates, Application of (2R,3S,4S,5R,6S)-2-(Hydroxymethyl)-6-(octylthio)tetrahydro-2H-pyran-3,4,5-triol, the publication is Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy (2020), 117346, database is CAplus and MEDLINE.

The photophysics and structural transition dynamics of a bio-active flavin lumichrome (LM) entrapped in two sugars based neutral surfactants are reported. Sugar-based surfactants, which were used for research purpose are potential environmentally friendly, green alternative amphiphilic surface active substance compared to other kinds of common surfactants. Here, two alkyl glucoside surfactants n-octyl-β-D-glucopyranoside (OBG) and n-octyl-β-D-thioglucopyranoside (OBTG) were used. This work was carried out by using steady-state absorption and fluorescence emission spectroscopy along with time-resolved fluorescence emission techniques. Photophysics of LM was modulated several folds in these two sugar-based neutral micelles. LM exhibits excitation and emission wavelength dependent fluorescence properties in these two sugars based neutral micelles. LM confined in the micellar environments exhibited structural transition dynamism, i.e. different kinds of conformers are equilibrated. Herein, different conformers of LM are identified and explained with the help of spectroscopic methods. From the fluorescence anisotropy measurement, the rotational relaxation time of LM in OBG micelle was more compared to that in OBTG micelle, which indicates that the LM mol. faced much more constrained environment in OBG micellar media.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy published new progress about 85618-21-9. 85618-21-9 belongs to alcohols-buliding-blocks, auxiliary class Tetrahydropyran,Chiral,sulfides,Alcohol, name is (2R,3S,4S,5R,6S)-2-(Hydroxymethyl)-6-(octylthio)tetrahydro-2H-pyran-3,4,5-triol, and the molecular formula is C14H28O5S, Application of (2R,3S,4S,5R,6S)-2-(Hydroxymethyl)-6-(octylthio)tetrahydro-2H-pyran-3,4,5-triol.

Referemce:
https://en.wikipedia.org/wiki/Alcohol,
Alcohols – Chemistry LibreTexts