Category: alcohols-buliding-blocks

Elam, Christopher published the artcileDiscovery of novel SERCA inhibitors by virtual screening of a large compound library, Name: 2,5-Bis(2,4,4-trimethylpentan-2-yl)benzene-1,4-diol, the publication is European Journal of Medicinal Chemistry (2011), 46(5), 1512-1523, database is CAplus and MEDLINE.

Two screening protocols based on recursive partitioning and computational ligand docking methodologies, resp., were employed for virtual screens of a compound library with 345,000 entries for novel inhibitors of the enzyme sarco/endoplasmic reticulum calcium ATPase (SERCA), a potential target for cancer chemotherapy. A total of 72 compounds that were predicted to be potential inhibitors of SERCA were tested in bioassays and 17 displayed inhibitory potencies at concentrations below 100 μM. The majority of these inhibitors were composed of two Ph rings tethered to each other by a short link of one to three atoms. Putative interactions between SERCA and the inhibitors were identified by inspection of docking-predicted poses and some of the structural features required for effective SERCA inhibition were determined by anal. of the classification pattern employed by the recursive partitioning models.

European Journal of Medicinal Chemistry published new progress about 903-19-5. 903-19-5 belongs to alcohols-buliding-blocks, auxiliary class Benzene,Phenol, name is 2,5-Bis(2,4,4-trimethylpentan-2-yl)benzene-1,4-diol, and the molecular formula is C22H38O2, Name: 2,5-Bis(2,4,4-trimethylpentan-2-yl)benzene-1,4-diol.

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

De Castro Dantas, T. N. published the artcilePreparation of aminoalkylphosphonium salts, Category: alcohols-buliding-blocks, the publication is Phosphorus and Sulfur and the Related Elements (1982), 13(1), 97-105, database is CAplus.

Three synthetic methods gave aminophosphonium salts Ph₃P⁺(CH₂)_nNRR¹ X^– (n = 2-4; R, R¹ = Me, Et, Me₂CH, Ph, PhCH₂). Yields are better with n = 3, but no intramol. stabilization was detected.

Phosphorus and Sulfur and the Related Elements published new progress about 101-98-4. 101-98-4 belongs to alcohols-buliding-blocks, auxiliary class Amine,Benzene,Alcohol, name is 2-(Benzyl(methyl)amino)ethanol, and the molecular formula is C10H15NO, Category: alcohols-buliding-blocks.

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

Huang, Pan published the artcileDiscovery of a Dual Tubulin Polymerization and Cell Division Cycle 20 Homologue Inhibitor via Structural Modification on Apcin, Related Products of alcohols-buliding-blocks, the publication is Journal of Medicinal Chemistry (2020), 63(9), 4685-4700, database is CAplus and MEDLINE.

Apcin is one of the few compounds that have been previously reported as a Cdc20 specific inhibitor, although Cdc20 is a very promising drug target. We reported here the design, synthesis, and biol. evaluations of 2,2,2-trichloro-1-aryl carbamate derivatives as Cdc20 inhibitors. Among these derivatives, compound 9f(I) was much more efficient than the pos. compound apcin in inhibiting cancer cell growth, but it had approx. the same binding affinity with apcin in SPR assays. It is possible that another mechanism of action might exist. Further evidence demonstrated that compound 9f also inhibited tubulin polymerization, disorganized the microtubule network, and blocked the cell cycle at the M phase with changes in the expression of cyclins. Thus, it induced apoptosis through the activation of caspase-3 and PARP. In addition, compound 9f inhibited cell migration and invasion in a concentration-dependent manner. These results provide guidance for developing the current series as potential new anticancer therapeutics.

Journal of Medicinal Chemistry published new progress about 622-40-2. 622-40-2 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Alcohol, name is 2-Morpholinoethanol, and the molecular formula is C6H13NO2, Related Products of alcohols-buliding-blocks.

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

Wongrakpanich, Amaraporn published the artcilePhyllanthus emblica extract-loaded transfersomes for hair follicle targeting: phytoconstituents, characterization, and hair growth promotion, COA of Formula: C5H12O2, the publication is Journal of Oleo Science (2022), 71(7), 1085-1096, database is CAplus and MEDLINE.

Phyllanthus emblica Linn. (PE) has been used to promote hair growth for decades. In this study, dried PE fruit powder was extracted, tested for biol. activities, and loaded into transfersomes for hair follicle targeting. Before lyophilization, PE fruit powder was extracted using 2 solvent systems, water and 30% ethanol. The PE 30% ethanolic extract had higher antioxidant activity and total phenolic content than the PE aqueous extract However, the cytotoxicity of the PE 30% ethanolic extract was higher than that of PE aqueous extract As a result, the PE aqueous extract was analyzed using ultra-performance liquid chromatog. and found that the major component of the PE aqueous extract was gallic acid. Afterward, the PE aqueous extract was tested for its potential to activate the expression of genes involved in hair growth promotion in human keratinocytes. At a non-toxic concentration (10 μg/mL), this extract promoted various growth factors comparable to 1% minoxidil. PE-loaded transfersomes were prepared to deliver the PE aqueous extract to the hair follicle. The particle size and polydispersity index of PE-loaded transfersomes were 228 nm and 0.25, resp. After 3 mo of storage, the particle size at 4°C and 30°C was 218 nm and 241 nm, resp., which was comparable to its initial size. However, at 40°C, the particle size dramatically increased (315 nm). The fluorescent agent, rhodamine B, was used to evaluate the potential of transfersomes to target hair follicles. Rhodamine B transfersomes had better penetration and accumulation in hair follicles than rhodamine B solution To conclude, the PE aqueous extract, mainly composed of gallic acid, can activate hair growth gene expression. The extract can be loaded into hair follicles targeting transfersomes. Thus, PE-loaded transfersomes are a promising delivery system for hair follicle targeting to promote hair growth.

Journal of Oleo Science 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 C5H6N2O2, COA of Formula: C5H12O2.

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

Gladkikh, V. F. published the artcileChanges in the stomach of small laboratory animals after oral administration of naphthamone and diphesyl, COA of Formula: C28H29NO4, the publication is Meditsinskaya Parazitologiya i Parazitarnye Bolezni (1972), 41(4), 423-8, database is CAplus and MEDLINE.

Rats, mice, guinea pigs, and cats, given orally repeated toxic doses of the antihelminthic compounds diphesyl (I) [34987-38-7] and naphthamone [3818-50-6] showed inflammation of the gastric mucosa, proliferation of the superficial squamous epithelium, and hyperkeratosis of the forestomach. These effects were reversible, and were probably due to the hydroxynaphthoate anion in the drugs.

Meditsinskaya Parazitologiya i Parazitarnye Bolezni published new progress about 3818-50-6. 3818-50-6 belongs to alcohols-buliding-blocks, auxiliary class Anti-infection,Antiparasitic, name is N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, and the molecular formula is C28H29NO4, COA of Formula: C28H29NO4.

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

Anagnostou, Athanasius published the artcileErythropoietin has a mitogenic and positive chemotactic effect on endothelial cells, Product Details of C18H20N2O12, the publication is Proceedings of the National Academy of Sciences of the United States of America (1990), 87(15), 5978-82, database is CAplus and MEDLINE.

A dose-dependent proliferative action of human recombinant erythropoietin on human umbilical vein endothelial cells and bovine adrenal capillary endothelial cells was observed Binding studies with radioiodinated recombinant human erythropoietin revealed a large number (≈27,000) of an apparent single class of receptors with an affinity in the 10^-9 M range. Linkage of the radiolabeled ligand to its receptor via a bifunctional crosslinking agent allowed identification of an endothelial cell protein of 45 kilodaltons as the principal receptor associated with this mitogenic effect of erythropoietin. Recombinant human erythropoietin also enhanced the migration of endothelial cells.

Proceedings of the National Academy of Sciences of the United States of America published new progress about 70539-42-3. 70539-42-3 belongs to alcohols-buliding-blocks, auxiliary class pyrrolidine,Ester,Amide,Inhibitor,Inhibitor, name is Bis(2,5-dioxopyrrolidin-1-yl) O,O’-ethane-1,2-diyl disuccinate, and the molecular formula is C18H20N2O12, Product Details of C18H20N2O12.

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

Kim, Seung-Woo published the artcileRobust neuroprotective effects of 2-((2-oxopropanoyl)oxy)-4-(trifluoromethyl)benzoic acid (OPTBA), a HTB/pyruvate ester, in the postischemic rat brain, Synthetic Route of 328-90-5, the publication is Scientific Reports (2016), 31843, database is CAplus and MEDLINE.

Postischemic brain damage in stroke is proceded with complicated pathol. events, and so multimodal drug treatments may offer better therapeutic means for improving clin. outcomes. Here, we report robust neuroprotective effects of a novel compound, 2-((2-oxopropanoyl)oxy)-4-(trifluoromethyl)benzoic acid (OPTBA), a 2-hydroxy-4-trifluoromethyl benzoic acid (HTB, a metabolite of triflusal)-pyruvate ester. I.v. administration of OPTBA (5 mg/kg) 3 or 6 h after middle cerebral artery occlusion (MCAO) in Sprague-Dawley rats reduced infarct volumes to 38.5 ± 11.4% and 46.5 ± 15.3%, resp., of that of MCAO controls, and ameliorated motor impairment and neurol. deficits. Importantly, neuroprotective effects of OPTBA were far greater than those afforded by combined treatment of HTB and pyruvate. Furthermore, OPTBA suppressed microglial activation and proinflammatory cytokine inductions more effectively than HTB/pyruvate co-treatment in the postischemic brain and LPS-treated cortical slice cultures and also attenuated NMDA-induced neuronal death in hippocampal slice cultures. LC-MS anal. demonstrated that OPTBA was hydrolyzed to HTB and pyruvate with a t_1/2 of 38.6 min in blood and 7.2 and 2.4 h in cortex and striatum, resp., and HTB was maintained for more than 24 h both in blood and brain tissue. Together these results indicate OPTBA acts directly and via its hydrolysis products, thus acting as a multimodal neuroprotectant in the postischemic brain.

Scientific Reports published new progress about 328-90-5. 328-90-5 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Carboxylic acid,Benzene,Phenol, name is 2-Hydroxy-4-(trifluoromethyl)benzoic acid, and the molecular formula is C8H5F3O3, Synthetic Route of 328-90-5.

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

Kazmierczak, Andrzej published the artcileMechanism of kinetin-induced death of Vicia faba ssp. minor root cortex cells, Safety of 2-(((9H-Purin-6-yl)amino)methyl)-6-methylphenol, the publication is Scientific Reports (2021), 11(1), 23746, database is CAplus and MEDLINE.

Cell death (CD) may be induced by endogenous or exogenous factors and contributes to all the steps of plant development. This paper presents results related to the mechanism of CD regulation induced by kinetin (Kin) in the root cortex of Vicia faba ssp. minor. To explain the process, 6-(2-hydroxy-3-methylbenzylamino)purine (PI-55), adenine (Ad), 5′-amine-5′-deoxyadenosine (Ado) and N-(2-chloro-4-piridylo)-N′-phenylurea (CPPU) were applied to (i) block cytokinin receptors (CKs) and inhibit the activities of enzymes of CK metabolism, i.e., (ii) phosphoribosyltransferase, (iii) kinases, and (iv) oxidases, resp. Moreover, ethylene glycol-bis(β-aminoethyl ether)-N,N,N′,N′-tetraacetic acid (EGTA), lanthanum chloride (LaCl3), ruthenium red (RRed) and cyclosporine A (CS-A) were applied to (i) chelate extracellular calcium ions (Ca2+) as well as blocks of (ii) plasma-, (iii) endoplasmic reticulum- (ER) membrane Ca2+ ion channels and (iv) mitochondria- (MIT) Ca2+ ions release by permeability transition por (PTP), resp. The measured physiol. effectiveness of these factors was the number of living and dying cortex cells estimated with orange acridine (OA) and ethidium bromide (EB), the amounts of cytosolic Ca2+ ions with chlortetracycline (CTC) staining and the intensity of chromatin and Ca2+-CTC complex fluorescence, resp. Moreover, the role of sorafenib, an inhibitor of RAF kinase, on the vitality of cortex cells and ethylene levels as well as the activities of RAF-like kinase and MEK2 with Syntide-2 and Mek2 as substrates were studied. The results clarified the previously presented suggestion that Kin is converted to appropriate ribotides (5′-monophosphate ribonucleotides), which cooperate with the ethylene and Ca2+ ion signalling pathways to transduce the signal of kinetin-programmed cell death (Kin-PCD). Based on the present and previously published results related to Kin-PCD, the crosstalk between ethylene and MAP kinase signalling, as well as inhibitors of CK receptors and enzymes of their metabolism, is proposed.

Scientific Reports published new progress about 1122579-42-3. 1122579-42-3 belongs to alcohols-buliding-blocks, auxiliary class 5.6_Aromatics,Purines, name is 2-(((9H-Purin-6-yl)amino)methyl)-6-methylphenol, and the molecular formula is C13H13N5O, Safety of 2-(((9H-Purin-6-yl)amino)methyl)-6-methylphenol.

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

Li, Shengke published the artcileSupramolecular Modulation of Antibacterial Activity of Ambroxol by Cucurbit[7]uril, Application of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, the publication is ChemPlusChem (2020), 85(4), 679-683, database is CAplus and MEDLINE.

Supramol. encapsulation by cucurbit[7]uril (CB[7]) was recently demonstrated to provide a simple and efficient method for antibacterial activity regulation of antibiotics. In this work, CB[7] was shown to form binary host-guest complex with ambroxol hydrochloride (ABX), a clin. mucokinetic and expectorant drug, which was reported to exhibit certain antibacterial activity. ¹H NMR titration and isothermal titration calorimetry experiment results suggested that the 4-hydroxyl cyclohexylamine group of ABX was included inside the CB[7] cavity, with a binding constant K_a of (6.69±0.11)×10⁵ M^-1 in phosphate buffered saline (PBS) solution, thermodynamically driven by both enthalpy change and entropy. More importantly, ABX’s inhibitory activity (MIC₅₀) against bacillary strains towards Pseudomonas aeruginosa and Escherichia coli strains was decreased from (5.11±0.31)×10^-6 M^-1 and (2.63±0.34)×10^-5 M^-1 to zero upon encapsulation by CB[7], and was subsequently recovered to almost its original activity when a competitive guest, amantadine hydrochloride, for disassembling CB[7]-ABX complex, was added, suggesting that the antibacterial activity of ABX could be readily “turned off/on” upon its complexation and decomplexation with CB[7].

ChemPlusChem published new progress about 23828-92-4. 23828-92-4 belongs to alcohols-buliding-blocks, auxiliary class Membrane Transporter/Ion Channel,Sodium Channel, name is trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, and the molecular formula is C13H19Br2ClN2O, Application of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride.

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

Mitsudo, Koichi published the artcileSynthesis of 3-Benzo[b]thienyl 3-Thienyl Ether via an Addition-Elimination Reaction and Its Transformation to an Oxygen-Fused Dithiophene Skeleton: Synthesis and Properties of Benzodithienofuran and Its π-Extended Derivatives, Recommanded Product: Thiophen-3-ol, the publication is Organic Letters (2017), 19(11), 2821-2824, database is CAplus and MEDLINE.

The synthesis of 3-benzo[b]thienyl 3-thienyl ether and its dehydrogenative cyclization leading to benzodithienofuran (BDTF; [1]benzothieno[3,2-b]thieno[2,3-d]furan) are described for the first time. Further transformation of BDTF to more π-extended BDTF derivatives and their fundamental phys. properties are also studied.

Organic Letters 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, Recommanded Product: Thiophen-3-ol.

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