Tag: M.W=400-450

Musdal, Yaman published the artcileFDA-approved drugs and other compounds tested as inhibitors of human glutathione transferase P1-1, HPLC of Formula: 3818-50-6, the publication is Chemico-Biological Interactions (2013), 205(1), 53-62, database is CAplus and MEDLINE.

Glutathione transferase P1-1 (GST P1-1) is often overexpressed in tumor cells and is regarded as a contributor to their drug resistance. Inhibitors of GST P1-1 are expected to counteract drug resistance and may therefore serve as adjuvants in the chemotherapy of cancer by increasing the efficacy of cytostatic drugs. Finding useful inhibitors among compounds used for other indications would be a shortcut to clin. applications and a search for GST P1-1 inhibitors among approved drugs and other compounds was therefore conducted. We tested 1040 FDA-approved compounds as inhibitors of the catalytic activity of purified human GST P1-1 in vitro. We identified chlorophyllide, merbromine, hexachlorophene, and ethacrynic acid as the most effective GST P1-1 inhibitors with IC₅₀ values in the low micromolar range. For comparison, these compounds were even more potent in the inhibition of human GST A3-3, an enzyme implicated in steroid hormone biosynthesis. In distinction from the other inhibitors, which showed conventional inhibition patterns, the competitive inhibitor ethacrynic acid elicited strong kinetic cooperativity in the glutathione saturation of GST P1-1. Apparently, ethacrynic acid serves as an allosteric inhibitor of the enzyme. In their own right, the compounds investigated are less potent than desired for adjuvants in cancer chemotherapy, but the structures of the most potent inhibitors could serve as leads for the synthesis of more efficient adjuvants.

Chemico-Biological Interactions 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, HPLC of Formula: 3818-50-6.

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

Remonen, Tommi published the artcileEthylenedithio end-capped oligothiophenes (bEDTnT); dimer, trimer and tetramer, Recommanded Product: 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, the publication is Synthetic Metals (1999), 101(1-3), 107-108, database is CAplus.

Two new ethylenedithio substituted thiophenes (I; R = H, Br) have been synthesized. Starting from I (R = Br), oligomers II (n = 0, 1, 2) were synthesized. Their cyclic voltammetric behavior and electronic structure (by UV-Vis) have been recorded. Low oxidation potentials and small differences between first and second oxidation potential were found. In the UV-Vis spectra large red shifts compared to other end-capped oligomers were observed

Synthetic Metals published new progress about 239075-02-6. 239075-02-6 belongs to alcohols-buliding-blocks, auxiliary class Thiophene,Boronic acid and ester,Boronate Esters, name is 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, and the molecular formula is C20H28B2O4S2, Recommanded Product: 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene.

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

Del Grosso, Alessandro published the artcileSimple inexpensive boron electrophiles for direct arene borylation, Computed Properties of 239075-02-6, the publication is Chemical Communications (Cambridge, United Kingdom) (2011), 47(46), 12459-12461, database is CAplus and MEDLINE.

Borenium ions, stabilized by coordination of hindered aromatic amines, were shown to act as reactive electrophiles for direct borylation of activated arenes and heterocyclic compounds, such as indoles and thiophenes. 2,6-Lutidine complex of dichloroborenium, [2,6-Me₂C₅H₃N·BCl₂][AlCl₄] was isolated and characterized by single-crystal x-ray diffraction, featuring low degree of π-bonding and high electrophilicity. Friedel-Crafts-type reaction of ArH with BCl₃, catalyzed by AlCl₃ in the presence of N,N-dimethyltoluidine or 2,6-lutidine as borenium stabilizing agents, followed by esterification with 2.2-3 equiv of pinacol, gave pinacolboronates ArBpin (Ar = 1-TIPS-3-pyrrolyl, 1-methyl-3-indolyl, 2,2′-bithiophen-5-yl, thieno[3,2-b]thien-2-yl, 4-(phenyl)(p-tolyl)aminophenyl, etc.). Electrophilic direct borylation is facilitated, and arene substrate scope enhanced, by using electrophiles derived from inexpensive reagents; specifically an amine, BCl₃ and AlCl₃.

Chemical Communications (Cambridge, United Kingdom) published new progress about 239075-02-6. 239075-02-6 belongs to alcohols-buliding-blocks, auxiliary class Thiophene,Boronic acid and ester,Boronate Esters, name is 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, and the molecular formula is C20H28B2O4S2, Computed Properties of 239075-02-6.

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

Lee, Sie Huey published the artcileInhaled mucoactive particles with tailored architecture for enhanced aerodynamicity, stability and efficacy, Application In Synthesis of 23828-92-4, the publication is International Journal of Pharmaceutics (Amsterdam, Netherlands) (2019), 118740, database is CAplus and MEDLINE.

In respiratory and genetic disorders such as asthma, chronic obstructive pulmonary disease (COPD), chronic bronchitis and cystic fibrosis (CF), the lungs produce excess mucus, resulting in a thickened mass, which clogs up the airways and reduces airflow. Consequently, breathing becomes more difficult. Medications that break down the structure of mucus will be especially useful in managing the early symptoms of these diseases and preventing their progression into the more severe forms. This work therefore seeks to develop an inhaled mucoactive dry powder formulation that is efficacious on multiple fronts. As an innovative step, sodium chloride was used to tailor the surface architecture of ambroxol hydrochloride particles, such that the resulting angular features on the surfaces contributed to the creation of corrugated particles with enhanced aerodynamicity. The optimized spray-dried powder particles were of respirable-size (d₅₀ of 2.85 ± 0.15 μm) and moderately corrugated. When the crystalline powder was dispersed via an Aerolizer inhaler at 60 L/min, it gave a fine particle fraction (FPF) of ∼31%, which was a ten-fold improvement over the unmodified species (i.e. ambroxol hydrochloride alone). Tests on artificial sputum medium (ASM) showed that the optimized formulation was potentially useful in liquefying the mucus, which favorably pointed towards the effectiveness of the formulation. In addition, the formulation was also stable to moisture ingress (up to ∼60% RH) and had good flowability. Hence, the advent of angular adjuvant sodium chloride particles in a mucoactive formulation conferred a three-fold benefit to the product: (1) Improved aerodynamicity and flowability, (2) Enhanced moisture stability and (3) Synergistic mucolytic properties.

International Journal of Pharmaceutics (Amsterdam, Netherlands) 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 In Synthesis of 23828-92-4.

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

El-Sayed, Heba M. published the artcileQuality by Design Strategy for Simultaneous HPLC Determination of Bromhexine HCl and Its Metabolite Ambroxol HCl in Dosage Forms and Plasma, Application In Synthesis of 23828-92-4, the publication is Chromatographia (2020), 83(9), 1075-1085, database is CAplus.

Abstract: The quality by design strategy was applied for the simultaneous chromatog. quantification of a binary mixture of bromhexine HCl and its pharmacol. active metabolite ambroxol HCl in dosage forms as well as in human plasma. In this study, five independent parameters were screened by fractional factorial design to specify the critical ones. The optimal conditions were determined by a response surface methodol. using a central composite design. Response surface methodol. enabled the best separation in minimal run time, as well as, prediction of separation and retention parameters with min. error. Separation and quantitation were carried out on BDS Hypersil C₈ (250 × 4.6 mm, 5μm) RP-column at 1.1 mL min^-1 flow rate, 25 mM of KH₂PO₄ (pH 3.5) in aqueous mobile phase, 65% MeOH, 210 nm wavelength of detection and 10μL injection volume After optimization of the chromatog. parameters, validation of the method was achieved according to ICH guidelines. Linearity ranged from 0.195 to 100μg mL^-1 ambroxol HCl, and 0.391-100μg mL^-1 bromhexine HCl, with R² values of 0.9998 and 0.9999 and limits of detection of 0.098 and 0.195μg mL^-1, resp. Recovery results ranged from 98.06 to 100.18 and 97.88 to 100.68 for bromhexine HCl and ambroxol HCl, resp., with RSD less than 1.80.

Chromatographia 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 In Synthesis of 23828-92-4.

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

Lee, Junghoon published the artcileSiloxane-Based Hybrid Semiconducting Polymers Prepared by Fluoride-Mediated Suzuki Polymerization, Computed Properties of 239075-02-6, the publication is Angewandte Chemie, International Edition (2015), 54(15), 4657-4660, database is CAplus and MEDLINE.

Siloxane-containing materials are a large and important class of organic-inorganic hybrids. In this report, a practical variation of the Suzuki polymerization to generate semiconducting polymeric hybrids based on siloxane units, which proceeds under essentially nonbasic conditions, is presented. This method generates solution-processable poly(diketopyrrolopyrrole-alt-benzothiadiazole) (PDPPBT-Si) consisting of the hybrid siloxane substituents, which could not be made using conventional methods. PDPPBT-Si exhibits excellent ambipolar transistor performance with well-balanced hole and electron FET mobilities. The siloxane-containing DPP-thiophene polymer classes (PDPP3T-Si and PDPP4T-Si), synthesized by this method, exhibit high hole mobility of up to 1.29 cm² V^-1 s^-1. This synthetic approach should provide access to a variety of novel siloxane-containing conjugated semiconductor classes by using a variety of aryldihalides and aryldiboronic acids/esters.

Angewandte Chemie, International Edition published new progress about 239075-02-6. 239075-02-6 belongs to alcohols-buliding-blocks, auxiliary class Thiophene,Boronic acid and ester,Boronate Esters, name is 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, and the molecular formula is C20H28B2O4S2, Computed Properties of 239075-02-6.

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

Panther, Lydia A. published the artcileSolvent-Free Synthesis of Core-Functionalised Naphthalene Diimides by Using a Vibratory Ball Mill: Suzuki, Sonogashira and Buchwald-Hartwig Reactions, Category: alcohols-buliding-blocks, the publication is Chemistry – A European Journal (2022), 28(49), e202201444, database is CAplus and MEDLINE.

Herein, the core functionalisation of N,N’-bis(2-ethylhexyl)-2,6-dibromo-1,4,5,8-naphthalenetetracarboxylic acid by using Suzuki, Sonogashira and Buchwald-Hartwig coupling reactions were reported. The products of these reactions are important building blocks in many areas of organic electronics including organic light-emitting diodes (OLEDs), organic field-effect transistors (OFETs) and organic photovoltaic cells (OPVCs). The reactions proceed in as little as 1 h, use com. available palladium sources (frequently Pd(OAc)₂) and were tolerant to air and atm. moisture. Furthermore, the real-world potential of this green VBM protocol was demonstrated by the double Suzuki coupling of a monobromo(NDI) residue to a bis(thiophene) pinacol ester. The resulting dimeric NDI species has been demonstrated to behave as an electron acceptor in functioning OPVCs.

Chemistry – A European Journal published new progress about 239075-02-6. 239075-02-6 belongs to alcohols-buliding-blocks, auxiliary class Thiophene,Boronic acid and ester,Boronate Esters, name is 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, and the molecular formula is C20H28B2O4S2, Category: alcohols-buliding-blocks.

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

Mutalik, G. S. published the artcileComparative clinical trial of bitoscanate, bephenium hydroxynaphthoate, and tetrachlorethylene in hookworm infection, COA of Formula: C28H29NO4, the publication is Indian Journal of Medical Sciences (1972), 26(11), 718-22, database is CAplus and MEDLINE.

Bitoscanate (I) [4044-65-9] (200-300 mg/day) decreased fecal egg counts by 98% and cured 15 of 23 patients with hookworm whereas bephenium hydroxynaphthoate [3818-50-6] (2.4 g) decreased fecal egg count by 76% and cured 3 of 23 patients and tetrachloroethylene [127-18-4] (3 mL) decreased egg counts by 89% and cured 5 of 23 patients. Mild and transient gastrointestinal reactions were obsd with all 3 drugs but most frequently with bitoscanate.

Indian Journal of Medical Sciences 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

Panchale, Wrushali A. published the artcileSimultaneous estimation of salbutamol sulphate and ambroxol HCl from their combined dosage form by UV-VIS spectroscopy using simultaneous equation method, COA of Formula: C13H19Br2ClN2O, the publication is GSC Biological and Pharmaceutical Sciences (2020), 13(3), 127-134, database is CAplus.

A simple UV-Vis Spectrophometric method was developed for the simultaneous determination of salbutamol sulfate and ambroxol HCl (AMB) from their combined dosage form. The method employs formation and solving of simultaneous equation using 242 nm and 272 nm as two anal. wavelengths (λMax of the drugs) of detection. Both the drugs obeyed Beer-Lambert’s law over the concentration range 1-50μg/mL for salbutamol sulfate and 10-50μg/mL for ambroxol HCl, resp. The developed method was validated for Accuracy, Precision, Limit of Detection and Limit of Quantification as per ICH guidelines and results of anal. were validated statistically.

GSC Biological and Pharmaceutical Sciences 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, COA of Formula: C13H19Br2ClN2O.

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

He, Meilian published the artcileDetermination of ambroxol hydrochloride in human plasma by ultra high performance liquid chromatography-tandem mass spectrometry and bioequivalence evaluation of its preparation, Related Products of alcohols-buliding-blocks, the publication is Sepu (2018), 36(11), 1099-1104, database is CAplus and MEDLINE.

A rapid, simple and sensitive ultra high performance liquid chromatog.-tandem mass spectrometry (UHPLC-MS/MS) method was developed for the determination of ambroxol hydrochloride in human plasma, and bioequivalence of its preparation was evaluated. The 50 μL-plasma sample was treated with methanol for protein precipitation, while ambroxol-d5 was used as an internal standard (IS). The separation was carried out on a Waters XBridge BEH C18 column (50 mm × 2.1 mm, 2.5 μm) by gradient elution at a flow rate of 0.4 mL/min, with 0.1% (volume/volume) formic acid aqueous solution and methanol containing 0.1% (volume/volume) formic acid as the mobile phases. The analyte was detected using an electrospray ionization source in pos. ion multiple reaction monitoring (MRM) mode. The calibration curves were linear in the range of 2-400 ng/mL (r = 0.998). The intra- and inter-run accuracies were 97.1-108.7%, and the intra- and inter-run precisions were 1.0-5.6%. The method was applied to the determination of the plasma concentration of the six healthy subjects after the oral administration of 30 mg of test and reference preparations The bioavailability was (102.3 ± 14.8)%. The 90% confidence intervals of the test preparation’s pharmacokinetic parameters were 80.0-125.0% of the reference preparation’s corresponding parameters. Thus, it is proved that the test preparation and reference preparation are bioequivalent.

Sepu 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, Related Products of alcohols-buliding-blocks.

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