Author: tianli

Wasson, B. K. published the artcileβ-Adrenergic blocking agents. 3-(3-Substituted-amino-2-hydroxypropoxy)-4-substituted-1,2,5-thiadiazoles, Category: alcohols-buliding-blocks, the publication is Journal of Medicinal Chemistry (1972), 15(6), 651-5, database is CAplus and MEDLINE.

A number of 3-(3-substitute-amino-2-hydroxypropoxy)-4-substituted-1,2,5-thiadiazoles were prepared by 3 general procedures: (a) by condensation of the appropriate 3-hydroxy-4-substituted-1,2,5-thiadiazole with epichlorohydrin, then formation of the epoxide, and condensation with an amine, (b) by treatment of 4-chloro-3-(3-substituted-amino-2-hydroxypropoxy)-1,2,5-thiadiazole with a heterocyclic compound containing a secondary N, or (c) by formation of a bromohydrin of a 3-substituted-4-allyloxy-1,2,5-thiadiazole, followed by treatment with an amine. A number of I containing 4-Cl, 4-Et, or 4-EtO such as (+)-3-(3-tert-butylamino-2-hydroxypropoxy)-4-chloro-1,2,5-thiadiazole-HCl [(+)-I, R = Cl, R1 = H, R2 = tert-Bu] [26791-14-0], 3-(3-isopropylamino-2-hydroxypropoxy)-4-ethyl-1,2,5-thiadiazole-HCl (I, R = Et, R1 = H, R2 = iso-Pr) [26670-38-2] and 3-(3-isopropylamino-2-hydroxypropoxy)-4-ethoxy-1,2,5-thiadiazole-HCl (I, R = EtO, R1 = H, R2 = iso-Pr) [26852-60-8] were potent β-adrenergic blocking agents but short acting (ED50 0.023, 0.04 and 0.035 mg/kg i.v., resp., dose required to inhibit by 50% the cardioaccelerator response to 0.12 mg/kg i.v. isoproterenol in the ganglion-blocked anesthetized rat). A number of 1,2,5-thiadiazoles possessing a bulky group in the 4-position were long acting, the outstanding member being (+-)-3-(3-tert-butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole-HCl [(+-)-II -HCl] [26670-02-0] with an ED50 of 0.013. Resolution of (+-)-II showed the bulk of activity resided in the (+)-form, (+)-3-(3-tert-butylamino-2-hydroxypropoxy)-4-morpholino-1,2,5-thiadiazole hydrogen maleate [(+)-II H maleate] [26839-77-0] the ED50 being 0.0066. The optimal activity in the thiadiazoles was achieved by the presence of an iso-Pr or tert-Bu group in the aminoisopropanoloxy side chain and inclusion of a bulky substituent in the 4 position.

Journal of Medicinal Chemistry published new progress about 30165-97-0. 30165-97-0 belongs to alcohols-buliding-blocks, auxiliary class Morpholine,Thiadiazole,Alcohol, name is 4-Morpholino-1,2,5-thiadiazol-3-ol, and the molecular formula is C42H63O3P, Category: alcohols-buliding-blocks.

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

Van Truong, Thien published the artcilePromoting crystallization of intrinsic membrane proteins with conjugated micelles, SDS of cas: 85618-21-9, the publication is Scientific Reports (2020), 10(1), 12199, database is CAplus and MEDLINE.

A new technique for promoting nucleation and growth of membrane protein (MP) crystals from micellar environments is reported. It relies on the conjugation of micelles that sequester MPs in protein detergent complexes (PDCs). Conjugation via amphiphilic [metal:chelator] complexes presumably takes place at the micelle/water interface, thereby bringing the PDCs into proximity, promoting crystal nucleation and growth. We have successfully applied this approach to two light-driven proton pumps: bacteriorhodopsin (bR) and the recently discovered King Sejong 1-2 (KS1-2), using the amphiphilic 4,4′-dinonyl-2,2′-dipyridyl (Dinonyl) (0.7 mM) chelator in combination with Zn²⁺, Fe²⁺, or Ni²⁺ (0.1 mM). Crystal growth in the presence of the [metal-chelator] complexes leads to purple, hexagonal crystals (50-75μm in size) of bR or pink, rectangular/square crystals (5-15μm) of KS1-2. The effects of divalent cation identity and concentration, chelator structure and concentration, ionic strength and pH on crystal size, morphol. and process kinetics, are described.

Scientific Reports 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 C13H19Br2ClN2O, SDS of cas: 85618-21-9.

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

Zhang, Zhuming published the artcileGut-Restricted Selective Cyclooxygenase-2 (COX-2) Inhibitors for Chemoprevention of Colorectal Cancer, COA of Formula: C3H5F3O, the publication is Journal of Medicinal Chemistry (2021), 64(15), 11570-11596, database is CAplus and MEDLINE.

Selective cyclooxygenase (COX)-2 inhibitors have been extensively studied for colorectal cancer (CRC) chemoprevention. Celecoxib has been reported to reduce the incidence of colorectal adenomas and CRC but is also associated with an increased risk of cardiovascular events. Here, we report a series of gut-restricted, selective COX-2 inhibitors characterized by high colonic exposure and minimized systemic exposure. By establishing acute ex vivo ¹⁸F-FDG uptake attenuation as an efficacy proxy, we identified a subset of analogs that demonstrated statistically significant in vivo dose-dependent inhibition of adenoma progression and survival extension in an APC^min/+ mouse model. However, in vitro-in vivo correlation anal. showed their chemoprotective effects were driven by residual systemic COX-2 inhibition, rationalizing their less than expected efficacies and highlighting the challenges associated with COX-2-mediated CRC disease chemoprevention.

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 0, COA of Formula: C3H5F3O.

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

Oliveira, Marilene Silva published the artcileMechanism of Photochemical O-Atom Exchange in Nitrosamines with Molecular Oxygen, SDS of cas: 4543-95-7, the publication is Journal of Organic Chemistry (2015), 80(12), 6119-6127, database is CAplus and MEDLINE.

The detection of an oxygen-atom photoexchange process of N-nitrosamines is reported. The photolysis of four nitrosamines (N-nitrosodiphenylamine 1, N-nitroso-N-methylaniline 2, N-butyl-N-(4-hydroxybutyl)nitrosamine 3, and N-nitrosodiethylamine 4) with UV light was examined in an ¹⁸O₂-enriched atm. in solution HPLC/MS and HPLC-MS/MS data show that ¹⁸O-labeled nitrosamines were generated for 1 and 2. But nitrosamines 3 and 4 do not exchange the ¹⁸O label and instead decomposed to amines and/or imines under the conditions. For 1 and 2, the ¹⁸O atom was found not to be introduced by moisture or by singlet oxygen [¹⁸(¹O₂¹Δ_g)] produced thermally by ¹⁸O-¹⁸O labeled endoperoxide of N,N’-di(2,3-hydroxypropyl)-1,4-naphthalene dipropanamide (DHPN¹⁸O₂) or by visible-light sensitization. A d. functional theory study of the structures and energetics of peroxy intermediates arising from reaction of nitrosamines with O₂ is also presented. A reversible head-to-tail dimerization of the O-nitrooxide to the 1,2,3,5,6,7-hexaoxadiazocane (30 kcal/mol barrier) with extrusion of O=¹⁸O accounts for exchange of the oxygen atom label. The unimol. cyclization of O-nitrooxide to 1,2,3,4-trioxazetidine (46 kcal/mol barrier) followed by a retro [2 + 2] reaction is an alternative, but higher energy process. Both pathways would require the photoexcitation of the nitrooxide.

Journal of Organic Chemistry published new progress about 4543-95-7. 4543-95-7 belongs to alcohols-buliding-blocks, auxiliary class Amine,Aliphatic hydrocarbon chain,Alcohol, name is 4-(Butylamino)butan-1-ol, and the molecular formula is C8H19NO, SDS of cas: 4543-95-7.

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

Clerici, Angelo published the artcileA New One-Pot, Four-Component Synthesis of 1,2-Amino Alcohols: TiCl₃/t-BuOOH-Mediated Radical Hydroxymethylation of Imines, Computed Properties of 101-98-4, the publication is Organic Letters (2008), 10(21), 5063-5066, database is CAplus and MEDLINE.

An amine, an aldehyde, and methanol can be readily assembled in one pot under very mild conditions through a free-radical multicomponent reaction by using an aqueous acidic TiCl₃/t-BuOOH system to afford 1,2-amino alcs. in fair to excellent yields.

Organic Letters 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, Computed Properties of 101-98-4.

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

Ekrami, Ali published the artcileDevelopment and evaluation of Zhumeria majdae essential oil-loaded nanoliposome against multidrug-resistant clinical pathogens causing nosocomial infection, Recommanded Product: cis-3,7-Dimethyl-2,6-Octadien-1-Ol, the publication is Journal of Drug Delivery Science and Technology (2022), 103148, database is CAplus.

In this study, we used Zhumeria majdae essential oil (ZMEO) loaded nanoliposome (NLP) to control several multidrug-resistant clin. pathogens (MDRs) that cause nosocomial infections using thin-layer hydration. Initially, ZMEO was extracted and analyzed by GC-MS, and then NLP-ZMEO was examined with different ratios of ZMEO to lecithin. Based on evaluation of release profile and phys. stability, size distribution, and particle size, using dynamic light scattering (DLS) results, the most stable NLP-ZMEO were prepared from ZMEO to lecithin ratio 1:3 that relative to pure ZMEO presented more potent antioxidant, anti-quorum sensing, and anti-biofilm activities. The morphol. results (AFM and SEM) also agreed with DLS anal. Also, the results of structural properties (DSC and FTIR) approved interaction between ZMEO and NLP. Comparing the cytotoxic effect on fibroblasts cell lines and antibacterial activity (MIC, MBC, and agar disk diffusion method), it was found that the antimicrobial activity in NLP-ZMEO was higher than ZMEO against multidrug-resistant clin. pathogens that cause nosocomial infection. The subcytotoxic values of the tested NLP-ZMEO were higher than MICs and MBCs for MDR bacteria and chlorhexidine doses.

Journal of Drug Delivery Science and Technology published new progress about 106-25-2. 106-25-2 belongs to alcohols-buliding-blocks, auxiliary class Natural product, name is cis-3,7-Dimethyl-2,6-Octadien-1-Ol, and the molecular formula is C10H18O, Recommanded Product: cis-3,7-Dimethyl-2,6-Octadien-1-Ol.

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

Horner, Leopold published the artcileo-Quinones. XXVII. Redox potentials of pyrocatechol derivatives, Recommanded Product: 4-(2,4,4-Trimethylpentan-2-yl)benzene-1,2-diol, the publication is Chemische Berichte (1965), 98(6), 2016-45, database is CAplus.

cf. Ibid. 2009-15; CA 62, 16155a. The polarographically determined standard redox potentials of 121 pyrocatechol derivatives, among them 28 substituted 1′,2′-dihydroxy-6,7-benzotropolones, were reported. The substituent effect on increments corresponding to the redox potential is approx. additive for many substituents. The redox potentials are discussed.

Chemische Berichte 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, Recommanded Product: 4-(2,4,4-Trimethylpentan-2-yl)benzene-1,2-diol.

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

Cozens, F. L. published the artcileSpontaneous carbocation generation on clays, Safety of 9-Phenyl-9H-xanthen-9-ol, the publication is Langmuir (1993), 9(3), 874-6, database is CAplus.

Stable carbocations were generated from arylfluorenols I (R = R¹ = H, Me; R = H, R¹ = Me), phenylxanthenol II, and tritylamine incorporated on smectic montmorillonite. Diffuse reflectance spectra were obtained.

Langmuir published new progress about 596-38-3. 596-38-3 belongs to alcohols-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Benzene,Alcohol, name is 9-Phenyl-9H-xanthen-9-ol, and the molecular formula is C19H14O2, Safety of 9-Phenyl-9H-xanthen-9-ol.

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

Kilcoyne, Michelle published the artcileSurface chemistry and linker effects on lectin-carbohydrate recognition for glycan microarrays, Synthetic Route of 96345-79-8, the publication is Analytical Methods (2012), 4(9), 2721-2728, database is CAplus.

Glycan microarrays are an increasingly utilized tool for anal. of protein-carbohydrate interactions and a variety of glycan-containing mols. and slide chemistries have been used to array carbohydrates on microarray surfaces. Slide surface chem. can have significant impact on the ligand presentation, background noise, spot size and morphol. and reproducibility of the arrayed mols., which in turn impacts upon lectin-carbohydrate recognition. The linker used to attach the carbohydrate to the mol. scaffold is another variable in ligand presentation. To evaluate these effects, three different microarray surface chemistries were arrayed with the same mono- and di-saccharide neoglycoconjugates and natural glycoproteins and incubated with four well-characterized plant lectins. Analogs of three monosaccharide neoglycoconjugates, with two common linkers each, were included in the test group to evaluate the linker effect on lectin recognition. Based on lowest background noise, expected lectin-ligand interaction, good spot morphol. and best reproducibility, the three-dimensional hydrogel slide surface proved most suitable for lectin interrogation of carbohydrate ligands, and the more flexible phenylisothiocyanate linker afforded greater recognition of the carbohydrates by the relevant lectins.

Analytical Methods published new progress about 96345-79-8. 96345-79-8 belongs to alcohols-buliding-blocks, auxiliary class Sugar Units,Gal and Man, name is (2R,3S,4S,5S,6R)-2-(Hydroxymethyl)-6-(4-isothiocyanatophenoxy)tetrahydro-2H-pyran-3,4,5-triol, and the molecular formula is C13H15NO6S, Synthetic Route of 96345-79-8.

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

Gokel, George W. published the artcileSulfur heterocycles. 3. Heterogeneous, phase-transfer, and acid-catalyzed potassium permanganate oxidation of sulfides to sulfones and a survey of their carbon-13 nuclear magnetic resonance spectra, Name: 2-Methyl-2-sulfanylpropan-1-ol, the publication is Journal of Organic Chemistry (1980), 45(18), 3634-9, database is CAplus.

Nineteen low-mol.-weight and heterocyclic sulfides were oxidized by variations of a technique using KMnO₄ and various catalysts. In addition, the NMR spectra of these compounds and other sulfones are reported.

Journal of Organic Chemistry published new progress about 73303-88-5. 73303-88-5 belongs to alcohols-buliding-blocks, auxiliary class Thiol,Aliphatic hydrocarbon chain,Alcohol, name is 2-Methyl-2-sulfanylpropan-1-ol, and the molecular formula is C4H10OS, Name: 2-Methyl-2-sulfanylpropan-1-ol.

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