Author: tianli

Musachio, Elize Aparecida Santos published the artcileSex-specific changes in oxidative stress parameters and longevity produced by Bisphenol F and S compared to Bisphenol A in Drosophila melanogaster, Name: 4,4′-Sulfonyldiphenol, the publication is Comparative Biochemistry and Physiology, Part C: Toxicology & Pharmacology (2022), 109329, database is CAplus and MEDLINE.

Female and male Drosophila melanogaster were exposed sep. for seven days to Bisphenol A (BPA), Bisphenol F (BPF), and Bisphenol S (BPS) at concentrations of 0.25, 0.5, and 1 mM. We observed that males exposed to 0.5 and 1 mM BPS showed lower catalase (CAT) activity and higher superoxide dismutase (SOD) and reactive species (RS); CAT activity decreased for BPF 0.5 and 1 mM. Nevertheless, BPA 0.5 and 1 mM decreased CAT activity, increased RS and lipid peroxidation (LPO), and reduced mitochondrial viability. None of the bisphenols altered the cell viability of male flies, although BPA 0.5 and 1 mM reduced longevity. In female flies, BPA and BPS 0.5 and 1 mM increased RS and LPO levels and decreased CAT activity and glutathione-S-transferase (GST), which may have contributed to lower mitochondrial and cell viability. Furthermore, BPS decreased SOD activity at the 1 mM concentration, and BPA reduced the SOD activity at concentrations of 0.5 and 1 mM. In the BPF 1 mM group, there was a reduction in GST activity and an increase in RS and LPO levels. The toxicol. effects were different between sexes, and BPA was more harmful than BPF and BPS in male flies. Thus, our findings showed that females were more susceptible to oxidative cell damage when exposed to BPA and BPS than to BPF, and daily exposure to BPA and BPS at all concentrations reduced female longevity, as well as in BPF 1 mM.

Comparative Biochemistry and Physiology, Part C: Toxicology & Pharmacology published new progress about 80-09-1. 80-09-1 belongs to alcohols-buliding-blocks, auxiliary class Ploymers, name is 4,4′-Sulfonyldiphenol, and the molecular formula is C12H10O4S, Name: 4,4′-Sulfonyldiphenol.

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

Abendrot, Michal published the artcileZinc(II) complexes of amino acids as new active ingredients for anti-acne dermatological preparations, Formula: C11H24O3, the publication is International Journal of Molecular Sciences (2021), 22(4), 1641, database is CAplus and MEDLINE.

Zinc compounds have a number of beneficial properties for the skin, including antimicrobial, sebostatic and demulcent activities. The aim of the study was to develop new anti-acne preparations containing zinc-amino acid complexes as active ingredients. Firstly, the cytotoxicity of the zinc complexes was evaluated against human skin fibroblasts (1BR.3.N cell line) and human epidermal keratinocyte cell lines, and their antimicrobial activity was determined against Cutibacterium acnes. Then, zinc complexes of glycine and histidine were selected to create original gel formulations. The stability (by measuring pH, d. and viscosity), microbiol. purity (referring to PN-EN ISO standards) and efficacy of the preservative system (according to Ph.Eur. 10 methodol.) for the preparations were evaluated. Skin tolerance was determined in a group of 25 healthy volunteers by the patch test. The preparations containing zinc(II) complexes with glycine and histidine as active substances can be topically used in the treatment of acne skin due to their high antibacterial activity against C. acnes and low cytotoxicity for the skin cells. Dermatol. recipes have been appropriately composed; no irritation or allergy was observed, and the preparations showed high microbiol. purity and physicochem. stability.

International Journal of Molecular Sciences 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

Zhang, Yong-Kang published the artcileBenzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate, Name: 3-Ethylazetidin-3-ol hydrochloride, the publication is Journal of Medicinal Chemistry (2017), 60(13), 5889-5908, database is CAplus and MEDLINE.

Carboxamide pyrazinyloxy benzoxaboroles were investigated with the goal to identify a mol. with satisfactory antimalarial activity, physicochem. properties, pharmacokinetic profile, in vivo efficacy, and safety profile. This optimization effort discovered 46, which met our target candidate profile. Compound 46 had excellent activity against cultured Plasmodium falciparum, and in vivo against P. falciparum and P. berghei in infected mice. It exhibited good PK properties in mice, rats, and dogs. It was highly active against the other 11 P. falciparum strains, which are mostly resistant to chloroquine and pyrimethamine. The rapid parasite in vitro reduction and in vivo parasite clearance profile of 46 were similar to those of artemisinin and chloroquine, two rapid-acting antimalarials. It was nongenotoxic in an Ames assay, an in vitro micronucleus assay, and an in vivo rat micronucleus assay when dosed orally up to 2000 mg/kg. The combined properties of this novel benzoxaborole support its progression to preclin. development.

Journal of Medicinal Chemistry published new progress about 935668-00-1. 935668-00-1 belongs to alcohols-buliding-blocks, auxiliary class Azetidine,Salt,Alcohol, name is 3-Ethylazetidin-3-ol hydrochloride, and the molecular formula is C18H35NO, Name: 3-Ethylazetidin-3-ol hydrochloride.

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

Zhang, Yong-Kang published the artcileBenzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate, COA of Formula: C3H5F3O, the publication is Journal of Medicinal Chemistry (2017), 60(13), 5889-5908, database is CAplus and MEDLINE.

Carboxamide pyrazinyloxy benzoxaboroles were investigated with the goal to identify a mol. with satisfactory antimalarial activity, physicochem. properties, pharmacokinetic profile, in vivo efficacy, and safety profile. This optimization effort discovered 46, which met our target candidate profile. Compound 46 had excellent activity against cultured Plasmodium falciparum, and in vivo against P. falciparum and P. berghei in infected mice. It exhibited good PK properties in mice, rats, and dogs. It was highly active against the other 11 P. falciparum strains, which are mostly resistant to chloroquine and pyrimethamine. The rapid parasite in vitro reduction and in vivo parasite clearance profile of 46 were similar to those of artemisinin and chloroquine, two rapid-acting antimalarials. It was nongenotoxic in an Ames assay, an in vitro micronucleus assay, and an in vivo rat micronucleus assay when dosed orally up to 2000 mg/kg. The combined properties of this novel benzoxaborole support its progression to preclin. development.

Journal of Medicinal Chemistry published new progress about 2240-88-2. 2240-88-2 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Aliphatic hydrocarbon chain,Alcohol, name is 3,3,3-Trifluoropropan-1-ol, and the molecular formula is C18H34N4O5S, COA of Formula: C3H5F3O.

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

Schlimpen, Fabian published the artcileα-Tertiary Propargylamine Synthesis via KA²-Type Coupling Reactions under Solvent-Free Cu^I-Zeolite Catalysis, Application of 2-Aminobutan-1-ol, the publication is Journal of Organic Chemistry (2021), 86(23), 16593-16613, database is CAplus and MEDLINE.

The potential of copper(I)-zeolite catalysis was evaluated in the three-component KA²-coupling mediated synthesis of α-tertiary propargylamines. Authors’ archetypal copper(I)-doped zeolite CuI-USY proved to be efficient under ligand- and solvent-free conditions at 80°. Usable up to four times, this catalytic material enables the coupling of diverse ketones, alkynes, and amines with a broad functional group tolerance. A decarboxylative and a desilylative version, resp., involving an alkynoic acid and trimethylsilylacetylene as alkyne surrogates, was also set up to bypass selectivity issues and/or to access α-tertiary propargylamines that are unattainable under standard KA² conditions. Interestingly, the KA²-type coupling reactions were successfully linked to other Cu^I-catalyzed reactions, thus resulting in sequential one-pot processes under full Cu^I-USY catalysis.

Journal of Organic Chemistry 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 of 2-Aminobutan-1-ol.

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

Cecchi, Patrizio published the artcileGas-phase protonation of spiropentane. A novel entry into the C₅H₉⁺ potential energy surface, Safety of 1-Methylcyclobutan-1-ol, the publication is Journal of the American Chemical Society (1993), 115(22), 10338-47, database is CAplus.

The structures, stabilities, and isomerization patterns of C₅H₉⁺ ions arising from the gas-phase protonation of spiropentane have been investigated by nuclear-decay, radiolytic, and FT-ICR techniques combined with ab initio calculations The exptl. and theor. results are consistent with the initial formation of a corner-protonated spiropentane intermediate 17, whose lifetime in the gas phase exceeds 7 × 10^-9 s. This local C₅H₉⁺ min. is separated from the ca. 30 kcal mol^-1 more stable cyclopentyl cation as well as from dimethylallyl open-chain isomers by significant energy barriers. Persistence of 17 in the gas phase does not find any correspondence in solution Solvation and ion-pairing effects may explain the failure to detect C₅H₉⁺ structures retaining the spirobicyclic framework of spiropentane in the condensed phase.

Journal of the American Chemical Society 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 C5H10O, Safety of 1-Methylcyclobutan-1-ol.

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

Koczurkiewicz-Adamczyk, Paulina published the artcileCinnamic acid derivatives as chemosensitising agents against DOX-treated lung cancer cells – Involvement of carbonyl reductase 1, SDS of cas: 96-20-8, the publication is European Journal of Pharmaceutical Sciences (2020), 105511, database is CAplus and MEDLINE.

Doxorubicin (DOX) therapy is limited by both cancer cells resistance and cardiotoxicity. DOX biotransformation to doxorubicinol (DOXol) by reductases enzymes (mainly by CBR1; carbonyl reductase 1) is a key process responsible for DOX adverse effects development. Thus, inhibition of CBR1 can increase the therapeutic effect of DOX. In the present study, we used a group of new synthesized cinnamic acid (CA) derivatives to improve the effectiveness and safety profile of DOX therapy against cancer cells in vitro. The possible mechanism of CBR1 inhibition was simulated by mol. modeling studies. The kinetics of DOX reduction in the presence of active CA derivatives were measured in cytosols. The chemosensitizing activity of CA derivatives including proapoptotic, anti-invasiveness activity were investigated in A549 lung cancer cell line. In our research 7 from 16 tested CA derivatives binded to the active site of CBR1 enzyme and improved DOX stability by inhibition of DOXol formation. Co-treatment of A549 cells with active CA derivatives and DOX induced cells apoptosis by activation of caspase cascade. At the same time we observed decrease of invasive properties (cell migration and transmigration assays) and the rearangments of F-actin cytoskeleton in CA derivatves + DOX treated cells. Meanwhile, control, human lung fibroblasts stay realtivelly unvulnerable and viable. New synthesized CA derivatives may inhibit the activity of CBR1 leading to the stabilization of DOX therapeutic levels in cancer cells and to protect the myocardium against DOXol cytotoxic effect. Favorable physicochem. properties supported by a safety profile and multidirectional chemosensitizing activity render CA derivatives a promising group for the development of agent useful in combined therapy.

European Journal of Pharmaceutical Sciences 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, SDS of cas: 96-20-8.

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

Borrel, Julien published the artcileCopper-Catalyzed Oxyalkynylation of C-S Bonds in Thiiranes and Thietanes with Hypervalent Iodine Reagents, Recommanded Product: (R)-Oxiran-2-ylmethanol, the publication is Organic Letters (2020), 22(2), 422-427, database is CAplus and MEDLINE.

We report the oxyalkynylation of thiiranes and thietanes using ethynylbenziodoxolone reagents (EBXs) to readily access functionalized building blocks bearing an alkynyl, a benzoate, and an iodide group. The reaction proceeds with high atom efficiency most likely through an alkynyl-episulfonium intermediate. The transformation is copper-catalyzed and compatible with a large array of thiiranes and thietanes.

Organic Letters 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, Recommanded Product: (R)-Oxiran-2-ylmethanol.

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

Timko, Lukas published the artcileSynthesis, physicochemical properties and biological activities of novel alkylphosphocholines with foscarnet moiety, Name: 2-Morpholinoethanol, the publication is Bioorganic Chemistry (2020), 104224, database is CAplus and MEDLINE.

A series of alkylphosphocholines with foscarnet moiety was synthesized. The structure of these zwitterionic amphiphiles was modified in both polar and non-polar parts of surfactant mol. Investigations of physicochem. properties are represented by the determination of critical micelle concentration, the surface tension value at the cmc and the surface area per surfactant head group utilizing surface tension measurements. Hydrodynamic diameter of surfactant micelles was determined using the dynamic light scattering technique. Alkylphosphocholines exhibit significant cytotoxic, anticandidal (Candida albicans) and antiamoebal (Acanthamoeba spp. T4 genotype) activity. The relationship between the structure, physicochem. properties and biol. activity of the tested compounds revealed that lipophilicity has a significant influence on biol. activity of the investigated surfactants. More lipophilic alkylphosphocholines with octadecyl chains show cytotoxic activity against cancer cells which is higher than that of the compounds with shorter alkyl chains. The opposite situation was observed in case of anticandidal and antiamoebal activity of these surfactants. The most active compounds were found to have pentadecyl chains. The foscarnet analog of miltefosine C15-PFA-C showed the highest anticandidal activity. The min. value of anticandidal activity of this compound is 1,4μM thus representing the highest anticandidal activity found within the group of alkylphosphocholines.

Bioorganic 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 C22H38O2, Name: 2-Morpholinoethanol.

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

Bahrami, Mohammadreza published the artcileA review of new adsorbents for separation of BTEX biomarkers, Related Products of alcohols-buliding-blocks, the publication is Biomedical Chromatography (2021), 35(9), e5131, database is CAplus and MEDLINE.

A review. The biomarker anal. of benzene, toluene, ethylbenzene and xylene (BTEXs) in biol. samples is the primary technique for evaluating these compounds in occupational and environmental exposures. The BTEX biomarkers are widely used to study the BTEX distribution in the environment and workplaces. Liquid-liquid extraction and solid-phase liquid extraction are among the most commonly used conventional methods to analyze biol. indexes of BTEXs. New methods have been proposed to analyze BTEX biomarkers using novel adsorbents such as sol-gel composite nanotubes, molecularly imprinted polymers and metal-organic frameworks, which are based on the application of needle trap devices, microextraction by packed sorbent, and solid-phase microextraction techniques. This paper provides an overview of new methods since 2015 regarding applying microextraction methods based on new adsorbents and analyzing BTEX biomarker compounds for occupational and environmental exposures. The results were compared with the liquid-phase microextraction methods recommended for urinary BTEX biomarkers.

Biomedical Chromatography published new progress about 90-64-2. 90-64-2 belongs to alcohols-buliding-blocks, auxiliary class Carboxylic acid,Benzene,Alcohol,Natural product, name is 2-Hydroxy-2-phenylacetic acid, and the molecular formula is C8H8O3, Related Products of alcohols-buliding-blocks.

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