Category: alcohols-buliding-blocks

Pein, Wesley L. published the artcileNickel-Catalyzed Ipso-Borylation of Silyloxyarenes via C-O Bond Activation, Application In Synthesis of 27292-49-5, the publication is Organic Letters (2021), 23(12), 4588-4592, database is CAplus and MEDLINE.

The conversion of silyloxyarenes to boronic acid pinacol esters via Ni catalysis is described. In contrast to other borylation protocols of inert C-O bonds, the method is competent in activating the C-O bond of silyloxyarenes in isolated aromatic systems lacking a directing group. The catalytic functionalization of benzyl silyl ethers was also achieved under these conditions. Sequential cross-coupling reactions were achieved by leveraging the orthogonal reactivity of silyloxyarenes, which could then be functionalized subsequently.

Organic Letters 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, Application In Synthesis of 27292-49-5.

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

Liu, Ye published the artcileInfluence of the Electronic Properties of the Ligand on the Photoelectrochemical Behavior of Au₂₅ Nanocluster-Sensitized TiO₂ Photoanode, Category: alcohols-buliding-blocks, the publication is Journal of Physical Chemistry C (2022), 126(4), 1778-1784, database is CAplus.

Atomically precise metal nanoclusters (NCs) have recently emerged as a new class of bifunctional (photoactive and catalytically active) photosensitizers in light energy conversion applications. Despite the size and alloy effects of NCs, no effort has been made to elucidate how the protecting ligand affects the photoelectrochem. of the NC-sensitized photoelectrodes. With a nanoporous TiO₂ array as model support, Au₂₅ NCs protected by various thiol-bearing ligands have been used to prepare four different photoanodes. It is revealed that a subtle change of the ligand from an alkanethiol to an aromatic thiol facilitates the charge transfer between the NC and TiO₂, which in turn improves the photoelectrochem. performance of the corresponding photoanode by at least 6 times. This new insight highlights the importance of the electronic properties of the ligand on the design of more efficient NC-sensitized photoelectrodes.

Journal of Physical Chemistry C 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, Category: alcohols-buliding-blocks.

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

Shugars, Diane C. published the artcileBiophysical characterization of recombinant proteins expressing the leucine zipper-like domain of the human immunodeficiency virus type 1 transmembrane protein gp41, Synthetic Route of 70539-42-3, the publication is Journal of Virology (1996), 70(5), 2982-91, database is CAplus and MEDLINE.

Envelope oligomerization is thought to serve crucial functions during the life cycle of human immunodeficiency virus type 1 (HIV-1). We recently reported that virus entry requires coiled-coil formation of the leucine zipper-like domain of the HIV-1 transmembrane envelope glycoprotein gp41. To determine the oligomeric state mediated by this region of the envelope, we have expressed the zipper motif as a fusion partner with the monomeric maltose-binding protein of Escherichia coli. The biophys. properties of this protein were characterized by velocity and equilibrium sedimentation, size exclusion chromatog., light scattering, and chem. crosslinking analyses. Results indicate that the leucine zipper sequence from HIV-1 is capable of multimerizing much larger and otherwise monomeric proteins into extremely stable tetramers. Recombinant proteins containing an alanine or a serine substitution at a critical isoleucine residue within the zipper region were also generated and similarly analyzed. The alanine- and serine-substituted proteins behaved as tetrameric and monomeric species, resp., consistent with the influence of these same substitutions on the helical coiled-coil structure of synthetic peptide models. On the basis of these findings, we propose that the fusogenic gp41 structure involves tetramerization of the leucine zipper domain which is situated ∼30 residues from the N-terminal fusion peptide sequence.

Journal of Virology 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 C18H12FN, Synthetic Route of 70539-42-3.

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

Ebner, A. published the artcileFunctionalization of AFM Tips and supports for molecular recognition force spectroscopy and recognition imaging, Related Products of alcohols-buliding-blocks, the publication is Methods in Molecular Biology (New York, NY, United States) (2019), 117-151, database is CAplus and MEDLINE.

Linking of sensor mols. (e.g., antibodies) to an AFM tip converts it into a biosensor by which single target mols. (e.g., antigens) can be detected and localized on the sample surface. Moreover, the mechanism of interaction can be studied by force spectroscopy if purified target mols. are linked to an ultra-flat surface, such as mica or silicon (nitride). Rapid imaging of the binding sites and force spectroscopy studies are greatly facilitated if 6-10 nm long polyethylene glycol (PEG) chains are used as flexible tethers between the sensor mol. and the tip. Here, we describe a set of methods by which a variety of proteins, oligonucleotides, or small mols. can be tethered to silicon (nitride) tips or to mica. Methods are included which afford site-specific and oriented coupling of the sensor mols.

Methods in Molecular Biology (New York, NY, United States) 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, Related Products of alcohols-buliding-blocks.

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

Feng, Yi-chao published the artcileApplication analysis of modified Zhike powder combined with ambroxol hydrochloride granules in treatment of chronic cough, Formula: C13H19Br2ClN2O, the publication is Xiandai Zhenduan Yu Zhiliao (2021), 32(6), 850-851, database is CAplus.

Objective: To investigate the application effect of Zhike powder combined with ambroxol hydrochloride granules in the treatment of chronic cough. Methods: A total of 80 patients with chronic cough who were admitted to our hospital from Apr. 2017 to March 2019 were selected and randomly divided into the control group and the observation group, 40 cases in each group. The control group was given ambroxol hydrochloride granules, the observation group was given modified Zhike powder, and both groups were treated for 14 d. The clin. efficacy, cough symptom scores and adverse reactions were compared between the two groups of patients after treatment. Results: After treatment, the total effective rate of the observation group was higher than that of the control group, and the difference was statistically significant (P<0.05). The cough symptom scores of the two groups were lower than those before treatment, and the observation group was lower than the control group, and the difference was statistically significant (P<0.05). There was no significant difference in the incidence of adverse reactions between the two groups (P>0.05). Conclusion: Modified Zhike Powder combined with ambroxol hydrochloride granules can improve the clin. efficacy of patients with chronic cough and relieve cough symptoms, and the medication is safe and worthy of clin. use.

Xiandai Zhenduan Yu Zhiliao 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, Formula: C13H19Br2ClN2O.

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

Fontenelle, Clement Q. published the artcileDesign of fluorinated 5-HT₄R antagonists: Influence of the basicity and lipophilicity toward the 5-HT₄R binding affinities, Product Details of C3H5F3O, the publication is Bioorganic & Medicinal Chemistry (2013), 21(23), 7529-7538, database is CAplus and MEDLINE.

Analogs of potent 5-HT₄R antagonists possessing a fluorinated N-alkyl chain have been synthesized to investigate the effect of the resulting change in basicity and lipophilicity on the affinity and selectivity profile. The authors demonstrate that for this series, the affinity is decreased with decreased basicity of the piperidine’s nitrogen atom. In contrast, the resulting increase in lipophilicity has minimal impact on binding affinity and selectivity. 3,3,3-Trifluoropropyl and derivatives 7-Fluoro-5-[1-(4,4,4-triuorobutyl)piperidin-4yl]methyloxybenzo[h]-1,6-naphthyridine 4,4,4-trifluorobutyl and 7-Fluoro-5-[1-(3,3,3-triuoropropyl)piperidin-4yl]methyloxybenzo[h]-1,6-naphthyridine have shown to bind to the 5-HT₄R while maintaining their pharmacol. profile and selectivity toward other 5-HT receptors.

Bioorganic & 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 C3H5F3O, Product Details of C3H5F3O.

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

Jeffries, Benjamin published the artcileReducing the Lipophilicity of Perfluoroalkyl Groups by CF₂-F/CF₂-Me or CF₃/CH₃ Exchange, Recommanded Product: 3,3,3-Trifluoropropan-1-ol, the publication is Journal of Medicinal Chemistry (2018), 61(23), 10602-10618, database is CAplus and MEDLINE.

Fluorination is commonly employed to optimize bioactivity and pharmaco-kinetic properties of drug candidates. Aliphatic fluorination often reduces the lipophilicity (log P), but polyfluoroalkylation typically increases lipophilicity. Hence, identification of polyfluorinated motifs that nonetheless lead to similar or even reduced lipophilicities is of interest to expand the arsenal of medicinal chem. tools in tackling properties such as compound metabolic stability or off-target selectivity. We show that changing a CF₃-group of a perfluoroalkyl chain to a Me group leads to a drastic reduction in lipophilicity. We also show that changing a C-F bond of a trifluoromethyl group, including when incorporated as part of a perfluoroalkyl group, to a C-Me group, leads to a reduction in log P, despite the resulting chain elongation. The observed lipophilicity trends were identified in fluorinated alkanol models and reproduced when incorporated in analogs of a drug candidate, and the metabolic stability of these motifs was demonstrated.

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 C3H5F3O, Recommanded Product: 3,3,3-Trifluoropropan-1-ol.

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

Linclau, Bruno published the artcileInvestigating the Influence of (Deoxy)fluorination on the Lipophilicity of Non-UV-Active Fluorinated Alkanols and Carbohydrates by a New log P Determination Method, Recommanded Product: 3,3,3-Trifluoropropan-1-ol, the publication is Angewandte Chemie, International Edition (2016), 55(2), 674-678, database is CAplus and MEDLINE.

Property tuning by fluorination is very effective for a number of purposes, and currently increasingly investigated for aliphatic compounds An important application is lipophilicity (log P) modulation. However, the determination of log P is cumbersome for non-UV-active compounds A new variation of the shake-flask log P determination method is presented, enabling the measurement of log P for fluorinated compounds with or without UV activity regardless of whether they are hydrophilic or lipophilic. No calibration curves or measurements of compound masses/aliquot volumes are required. With this method, the influence of fluorination on the lipophilicity of fluorinated aliphatic alcs. was determined, and the log P values of fluorinated carbohydrates were measured. Interesting trends and changes, for example, for the dependence on relative stereochem., are reported.

Angewandte Chemie, International Edition 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 C3H5F3O, Recommanded Product: 3,3,3-Trifluoropropan-1-ol.

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

Li, Zhang published the artcileDesign, synthesis and evaluation of novel diaryl-1,5-diazoles derivatives bearing morpholine as potent dual COX-2/5-LOX inhibitors and antitumor agents, Application In Synthesis of 622-40-2, the publication is European Journal of Medicinal Chemistry (2019), 168-184, database is CAplus and MEDLINE.

In this paper, 41 hybrid compounds containing diaryl-1,5-diazole and morpholine structures, compounds I [R¹ = H, F, Me, etc.; R² = H, F, Cl, etc.; X = O, S] and II [R³ = H, F, MeO, etc.; Y = O, NH; n = 2,3] acting as dual COX-2/5-LOX inhibitors have been designed, synthesized and biol. evaluated. Most of them showed potent antiproliferative activities and COX-2/5-LOX inhibitory in-vitro. Among them, compound II [R³ = CF₃, Y = NH, n = 3] displayed the most potency against cancer cell lines (IC₅₀ = 6.43-10.97 μM for F10, HeLa, A549 and MCF-7 cells), lower toxicity to non-cancer cells than celecoxib (A33: IC₅₀ = 194.01 μM vs.celecoxib: IC₅₀ = 97.87 μM for 293T cells), and excellent inhibitory activities on COX-2 (IC50 = 0.17 μM) and 5-LOX (IC₅₀ = 0.68 μM). Meanwhile, the mol. modeling study was performed to position compound II [R³ = CF₃, Y = NH, n = 3] into COX-2 and 5-LOX active sites to determine the probable binding models. Mechanistic studies demonstrated that compound II [R³ = CF₃, Y = NH, n = 3] could block cell cycle in G2 phase and subsequently induced apoptosis of F10 cells. Furthermore, compound II [R³ = CF₃, Y = NH, n = 3] could significantly inhibit tumor growth in F10-xenograft mouse model, and pharmacokinetic study of compound A33 indicated that it showed better stability in vivo. In general, compound II [R³ = CF₃, Y = NH, n = 3] could be a promising candidate for cancer therapy.

European 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, Application In Synthesis of 622-40-2.

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

Jiang, Biwei published the artcileApplication of carboprost tromethamine combined with modified patch suture in placenta previa postpartum hemorrhage, Application of 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid, the publication is Zhongguo Jiceng Yiyao (2013), 20(4), 533-535, database is CAplus.

The effect of carboprost tromethamine (hemabate) combined with modified patch suture in placenta previa postpartum hemorrhage was observed Sixty-two patients with placenta previa were divided into the control group (30 cases) and treatment group (32 cases). The control group was treated with hemabate, and the treatment group was treated with hemabate combined with modified patch suture. The two groups of intraoperative, postpartum 2 h, 24 h postpartum were compared in bleeding volume and Hb changes. The intraoperative bleeding volume [(321.9±67.8) ml vs (435.9±83.3) ml] and 2h, 24h postpartum bleeding volume [(417.7±68.0) ml vs (539.6±70.4) ml and (485.3±68.5) ml vs (621.0±81.3) ml] of the treatment group were significant less than that of the control group (t=5.926, 6.938, 7.133, all P<0.05). Significant difference in changes of Hb level was also observed between the two groups, though postpartum level was not significantly reduced in the treatment group compared with the control group [(5.0±6.5) g/L vs (-4.0±6.8) g/L] (t=-3.662, P<0.05). Hemabate combined with modified patch suture can be more effective in the prevention of postpartum hemorrhage in placenta previa.

Zhongguo Jiceng Yiyao published new progress about 58551-69-2. 58551-69-2 belongs to alcohols-buliding-blocks, auxiliary class Chiral,Alkenyl,Amine,Aliphatic cyclic hydrocarbon,Ester,Alcohol,Inhibitor,, name is 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid, and the molecular formula is C25H47NO8, Application of 2-Amino-2-(hydroxymethyl)propane-1,3-diol (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((S,E)-3-hydroxy-3-methyloct-1-en-1-yl)cyclopentyl)hept-5-enoic acid.

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