Tag: M.W=200-250

Barr, Rita published the artcileElectron donation to the plasma membrane redox system of cultured carrot cells stimulates proton release, Synthetic Route of 1139-46-4, the publication is Biochimica et Biophysica Acta, Bioenergetics (1990), 1017(1), 91-5, database is CAplus and MEDLINE.

Membrane-permeable electron donors, duroquinol, diphenylcarbazide, pyrocatechol, and tert-octylcatechol, promoted both reduction of an impermeant electron acceptor and proton transport with cultured carrot cells. These cells were preloaded with electron donors for 15, 30, 45, and 60 min. Aliquots of cells were removed at various times, washed free of excess electron donors and assayed for their effect on transplasma membrane redox with impermeable hexacyanoferrate (HCF III) as the electron acceptor and for simultaneous H⁺ excretion in the presence of hexacyanoferrate. All four electron donors stimulated HCF III reduction and associated H⁺ excretion. Below a rate of hexacyanoferrate reduction of 6 μmol/g dry weight per min, the ratios of H⁺/e^– were between 0.3 and 1 with low concentrations (0.1 mM) of the added electron donors. When hexacyanoferrate reduction exceeded 6 μmol/g dry weight per min, H⁺ release began to cascade to give ratios of 1 to 3, suggesting activation of an H⁺-ATPase or a proton transporter. This behavior by cultured carrot cells indicates that a certain threshold of proton concentration in a limited membrane domain must be reached in order for the proton channel to be opened.

Biochimica et Biophysica Acta, Bioenergetics published new progress about 1139-46-4. 1139-46-4 belongs to alcohols-buliding-blocks, auxiliary class Benzene,Phenol, name is 4-(2,4,4-Trimethylpentan-2-yl)benzene-1,2-diol, and the molecular formula is C14H22O2, Synthetic Route of 1139-46-4.

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

Peiro Cadahia, Jorge published the artcileSynthesis and Evaluation of Hydrogen Peroxide Sensitive Prodrugs of Methotrexate and Aminopterin for the Treatment of Rheumatoid Arthritis, COA of Formula: C14H21BO3, the publication is Journal of Medicinal Chemistry (2018), 61(8), 3503-3515, database is CAplus and MEDLINE.

A series of novel hydrogen peroxide sensitive prodrugs I (11–13; R = H, Me, F) of methotrexate (MTX) and aminopterin (AMT) were synthesized and evaluated for therapeutic efficacy in mice with collagen induced arthritis (CIA) as a model of chronic rheumatoid arthritis (RA). The prodrug strategy selected is based on ROS-labile 4-methylphenylboronic acid promoieties linked to the drugs via a carbamate linkage or a direct C-N bond. Activation under pathophysiol. concentrations of H₂O₂ proved to be effective, and prodrug candidates were selected in agreement with relevant in vitro physicochem. and pharmacokinetic assays. Selected candidates showed moderate to good solubility, high chem. and enzymic stability, and therapeutic efficacy comparable to the parent drugs in the CIA model. Importantly, the prodrugs displayed the expected safer toxicity profile and increased therapeutic window compared to MTX and AMT while maintaining a comparable therapeutic efficacy, which is highly encouraging for future use in RA patients.

Journal of Medicinal Chemistry published new progress about 1370732-71-0. 1370732-71-0 belongs to alcohols-buliding-blocks, auxiliary class Boronic acid and ester, name is (3-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methanol, and the molecular formula is C14H21BO3, COA of Formula: C14H21BO3.

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

Johnson, Wilbur Jr. published the artcileSafety assessment of alkyl glyceryl ethers as used in cosmetics, Formula: C11H24O3, the publication is International Journal of Toxicology (2013), 32(5S), 5S-21S, database is CAplus and MEDLINE.

A review. Alkyl glyceryl ethers function mostly as skin-conditioning agents in cosmetic products applied to the skin and hair. The Cosmetic Ingredient Review expert panel reviewed the available animal toxicity and clin. data, including the low dermal absorption, and concluded that the alkyl glyceryl ethers are safe in the present practices of use and concentration described in this safety assessment.

International Journal of Toxicology published new progress about 70445-33-9. 70445-33-9 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic Chain, name is 3-((2-Ethylhexyl)oxy)propane-1,2-diol, and the molecular formula is C11H24O3, Formula: C11H24O3.

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

Rashidi, Masih published the artcileThe selective cleavage of lignin aliphatic C-O linkages by solvent-assisted fast pyrolysis (SAFP), HPLC of Formula: 70110-65-5, the publication is Journal of Inclusion Phenomena and Macrocyclic Chemistry (2019), 94(3-4), 297-307, database is CAplus.

We report the effect of an organic solvent on the selective cleavage of individual lignin model compounds and lignin C-O linkages during the fast thermal pyrolysis of lignin. During this process, it was possible to lower the aliphatic hydroxyl contents of lignin, along with increasing the amount of single and double bonded aliphatics. It was found that the addition of solvent during fast pyrolysis of lignin lowered the mol. weight distribution of the obtained bio-oil (�49-52% decrease) and at the same time inhibited the formation of a high amount of char. A detailed study of the cleavage of complex model compounds using Ethanol-Assisted Fast Pyrolysis (EAFP) revealed that the aliphatic hydroxyl groups and etheric linkages are very reactive during this process. By the use of deuterated lignin model compounds and solvent, it was then possible to elucidate the mechanism for cleavage of lignin in the EAFP process that involves the formation of a transition state between solvent and oxygen bonds of lignin. This transition state involves the cleavage of etheric bonds by the in situ transfer of hydrogen from ethanol to this linkage.

Journal of Inclusion Phenomena and Macrocyclic Chemistry published new progress about 70110-65-5. 70110-65-5 belongs to alcohols-buliding-blocks, auxiliary class Benzene,Alcohol,Ether,Benzene Compounds, name is 2-Phenoxy-1-phenylpropane-1,3-diol, and the molecular formula is C15H16O3, HPLC of Formula: 70110-65-5.

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

Crane, F. L. published the artcileStimulation of photosynthesis by carbonyl compounds and chelators, Application In Synthesis of 1139-46-4, the publication is Biochemical and Biophysical Research Communications (1977), 74(4), 1362-8, database is CAplus and MEDLINE.

A number of carbonyl compounds including HCO3-, ethylene carbonate, dimethyl carbonate, propylene carbonate, bis(pentamethylene)urea, and glycidol, and several chelators were tested for their effect on photosynthetic reactions in isolated spinach chloroplasts. Carbonyl compounds inhibited the DCMU-insensitive silicomolybdate reduction by photosystem II but stimulated the O evolution associated with ferricyanide reduction in the presence of DBMIB and the H2O �methylviologen reaction. Many chelators behaved in the same manner except 1,10-phenanthroline which showed the opposite effect. The carbonyl compounds did not uncouple because they stimulated the proton gradients associated with noncyclic photophosphorylation, whereas some chelators, such as bathocuproine or bathophenanthroline inhibited the proton gradients 100%. Electron transport in the presence of ADP and inorganic phosphate showed a stimulation of rates beyond that obtained in presence of an uncoupler. The data are discussed in terms of inhibition of cyclic electron flow around photosystem II which leads to increased electron transport rates toward photosystem I.

Biochemical and Biophysical Research Communications published new progress about 1139-46-4. 1139-46-4 belongs to alcohols-buliding-blocks, auxiliary class Benzene,Phenol, name is 4-(2,4,4-Trimethylpentan-2-yl)benzene-1,2-diol, and the molecular formula is C14H22O2, Application In Synthesis of 1139-46-4.

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

Nemeth, Ansley M. published the artcileStructure-Function Studies on IMD-0354 Identifies Highly Active Colistin Adjuvants, Synthetic Route of 328-90-5, the publication is ChemMedChem (2020), 15(2), 210-218, database is CAplus and MEDLINE.

Infections caused by multidrug-resistant (MDR) bacteria, particularly Gram-neg. bacteria, are an escalating global health threat. Often clinicians are forced to administer the last-resort antibiotic colistin; however, colistin resistance is becoming increasingly prevalent, giving rise to the potential for a situation in which there are no treatment options for MDR Gram-neg. infections. The development of adjuvants that circumvent bacterial resistance mechanisms is a promising orthogonal approach to the development of new antibiotics. We recently disclosed that the known IKK-β inhibitor IMD-0354 potently suppresses colistin resistance in several Gram-neg. strains. In this study, we explore the structure-activity relationship (SAR) between the IMD-0354 scaffold and colistin resistance suppression, and identify several compounds with more potent activity than the parent against highly colistin-resistant strains of Acinetobacter baumannii and Klebsiella pneumoniae.

ChemMedChem 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

Thorsteinson, Nels published the artcileIn silico identification of anthropogenic chemicals as ligands of zebrafish sex hormone binding globulin, Quality Control of 1139-46-4, the publication is Toxicology and Applied Pharmacology (2009), 234(1), 47-57, database is CAplus and MEDLINE.

Anthropogenic compounds with the capacity to interact with the steroid-binding site of sex hormone binding globulin (SHBG) pose health risks to humans and other vertebrates including fish. Building on studies of human SHBG, the authors have applied in silico drug discovery methods to identify potential binders for SHBG in zebrafish (Danio rerio) as a model aquatic organism. Computational methods, including; homol. modeling, mol. dynamics simulations, virtual screening, and 3D QSAR anal., successfully identified 6 non-steroidal substances from the ZINC chem. database that bind to zebrafish SHBG (zfSHBG) with low-micromolar to nanomolar affinities, as determined by a competitive ligand-binding assay. The authors also screened 80,000 com. substances listed by the European Chems. Bureau and Environment Canada, and 6 non-steroidal hits from this in silico screen were tested exptl. for zfSHBG binding. All 6 of these compounds displaced the [³H]5α-dihydrotestosterone used as labeled ligand in the zfSHBG screening assay when tested at a 33 μM concentration, and 3 of them (hexestrol, 4-tert-octylcatechol, and dihydrobenzo(a)pyren-7(8H)-one) bind to zfSHBG in the micromolar range. The study demonstrates the feasibility of large-scale in silico screening of anthropogenic compounds that may disrupt or highjack functionally important protein:ligand interactions. Such studies could increase the awareness of hazards posed by existing com. chems. at relatively low cost.

Toxicology and Applied Pharmacology published new progress about 1139-46-4. 1139-46-4 belongs to alcohols-buliding-blocks, auxiliary class Benzene,Phenol, name is 4-(2,4,4-Trimethylpentan-2-yl)benzene-1,2-diol, and the molecular formula is C18H17N5O3, Quality Control of 1139-46-4.

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

Zhao, Xin published the artcilePolyols with several kinds of Chinese herbal medicine extracts of the anticorrosion composite applied in cosmetics, Formula: C11H24O3, the publication is Guangzhou Huagong (2013), 41(24), 70-72, database is CAplus.

A kind of the anti-corrosion composite containing polyols and several kinds of extracts of Chinese herbal medicine in combination were studied. By use of this kind of compound with combination, a novel cosmetics using antiseptic combination was provided, and the results showed that the combination and the vast majority of cosmetics raw material compatibility were very good, with broad-spectrum antimicrobial activity, which can effectively inhibit gram neg. bacteria, gram-pos. bacteria, yeast and mold, and its bacteriostatic ability was not influenced by surface active agent in cosmetics.

Guangzhou Huagong published new progress about 70445-33-9. 70445-33-9 belongs to alcohols-buliding-blocks, auxiliary class Aliphatic Chain, name is 3-((2-Ethylhexyl)oxy)propane-1,2-diol, and the molecular formula is C15H14O3, Formula: C11H24O3.

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

Valle, M. published the artcileAccess of HTB, main metabolite of triflusal, to cerebrospinal fluid in healthy volunteers, Application of 2-Hydroxy-4-(trifluoromethyl)benzoic acid, the publication is European Journal of Clinical Pharmacology (2005), 61(2), 103-111, database is CAplus and MEDLINE.

Triflusal has been shown to exert neuroprotective effects by downregulating mols. considered responsible for the development of Alzheimer’s disease (AD). The aim of this study was to develop a population pharmacokinetic model to characterize plasma and cerebrospinal fluid (CSF) pharmacokinetics of the main active metabolite of triflusal-HTB (2-hydroxy-4-trifluoro-methylbenzoic acid)-in healthy volunteers. Data from two studies were combined. Study A: subjects received single oral doses of triflusal 900 mg. Triflusal and HTB plasma concentrations were extensively measured. Study B: triflusal 600 mg once daily was administered orally for 14 days. HTB plasma and CSF concentrations were determined in healthy volunteers. Population pharmacokinetic modeling was performed using NONMEM. A one-compartmental model with rapid first-order absorption for triflusal and first-order formation of HTB best described plasma concentrations Triflusal elimination rate constant was 50 times faster than that estimated for the metabolite. CSF concentrations of HTB ranged between 0.011 μg/mL and 0.341 μg/mL. A CSF-plasma partition coefficient of 0.002 and a k_e0 value of 0.059 h^-1 were estimated by means of population modeling. In the present study in healthy volunteers, HTB penetrated into the CSF in a range of concentrations exptl. proven to have protective effects in AD. These concentrations suggest that triflusal could be used in the treatment of central nervous system diseases in doses similar to those used in cardiovascular diseases. Access to the CSF compartment was characterized by a slow equilibrium rate constant and a low CSF-plasma partition coefficient

European Journal of Clinical Pharmacology 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 C10H14BNO4S, Application of 2-Hydroxy-4-(trifluoromethyl)benzoic acid.

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

Lopez-Periago, A. published the artcileImpregnation of a biocompatible polymer aided by supercritical CO₂: Evaluation of drug stability and drug-matrix interactions, Safety of 2-Hydroxy-4-(trifluoromethyl)benzoic acid, the publication is Journal of Supercritical Fluids (2009), 48(1), 56-63, database is CAplus.

Poly(Me methacrylate) (PMMA) was loaded with 2-acetyloxy-4-(trifluoromethyl) benzoic acid (triflusal) by a supercritical carbon dioxide (scCO₂) impregnation method. The main objective of this work was to provide information for the infusion of additives into nonporous polymeric substrates for design of sustained release systems. Chem. and H-bonding interactions between the matrix and the infused drug were evaluated together with the impregnated drug stability. The composition of the obtained systems was characterized by ¹H magnetic nuclear resonance and liquid chromatog. The microstructure of the impregnated matrix was studied using thermal anal. The affinity of the solute to the polymer was explored via attenuated total reflection (ATR)-FTIR and Raman spectroscopies. Finally, an in vitro elution method coupled with high-performance liquid chromatog. was used to evaluate the release behavior of prepared formulations. Loadings of ca. 20 weight% of active agent in PMMA were obtained, while the drug crystallization was avoided. From a pharmaceutical point of view, the impregnated samples had an excellent potential for the preparation of sustained formulations, since the delivery profiles were consistent with keeping stable levels of the drug over a long period of time.

Journal of Supercritical Fluids 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, Safety of 2-Hydroxy-4-(trifluoromethyl)benzoic acid.

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