Month: October 2022

Esmaeili, Sajjad; Ghobadi, Nazanin; Nazari, Donya; Pourhossein, Alireza; Rasouli, Hassan; Adibi, Hadi; Khodarahmi, Reza published their research in Medicinal Chemistry (Sharjah, United Arab Emirates) in 2021. The article was titled 《Curcumin-based Antioxidant and Glycohydrolase Inhibitor Compounds: Synthesis and In Vitro Appraisal of the Dual Activity Against Diabetes》.Category: alcohols-buliding-blocks The article contains the following contents:

Curcumin, as the substantial constituent of the turmeric plant (Curcuma longa), plays a significant role in the prevention of various diseases, including diabetes. It possesses ideal structure features as an enzyme inhibitor, including a flexible backbone, hydrophobic nature, and several available hydrogen bond (H-bond) donors and acceptors. The present study aimed at synthesizing several novel curcumin derivatives and further evaluation of these compounds for possible antioxidant and anti-diabetic properties along with inhibitory effect against two carbohydrate-hydrolyzing enzymes, α-amylase and α-glucosidase, as these enzymes are therapeutic targets for attenuation of postprandial hyperglycemia. Therefore, curcumin-based pyrido[2,3-d]pyrimidine derivatives were synthesized and identified using an instrumental technique like NMR spectroscopy and then screened for antioxidant and enzyme inhibitory potential. Total antioxidant activity, reducing power assay and 1,1-diphenyl-2- picrylhydrazyl (DPPH•) radical scavenging activity were done to appraise the antioxidant potential of these compounds in vitro. Compounds L6-L9 showed higher antioxidant activity while L4, L9, L12 and especially L8 exhibited the best selectivity index (lowest α-amylase/α-glucosidase inhibition ratio). These antioxidant inhibitors may be potential anti-diabetic drugs, not only to reduce glycemic index but also to limit the activity of the major reactive oxygen species (ROS) producing pathways.3,5-Dihydroxybenzaldehyde(cas: 26153-38-8Category: alcohols-buliding-blocks) was used in this study.

3,5-Dihydroxybenzaldehyde(cas: 26153-38-8) is used as a building block in the synthesis of more complex structures. It is also used in the synthesis of terbutaline, which is an important bronchodilator.Category: alcohols-buliding-blocks

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

HPLC of Formula: 100-55-0In 2021 ,《KF/clinoptilolite NPs: An efficient and heterogeneous catalyst for chemoselective silylation of alcohols and phenols》 appeared in Phosphorus, Sulfur and Silicon and the Related Elements. The author of the article were Oladee, Razieh; Zareyee, Daryoush; Khalilzadeh, Mohammad A.. The article conveys some information:

Potassium fluoride incorporated on clinoptilolite nanoparticles (KF/CP NPs) by ion exchanging is found to be an effective and inexpensive heterogeneous nanocatalyst for chemoselective silylation of alcs. and phenols with 1,1,1,3,3,3-hexamethyldisilazane (HMDS) at room temperature Nano-powder of clinoptilolite (CP) was prepared using a planetary ball mill mech. method and characterized by dynamic light scattering (DLS), X-ray powder diffraction (XRD) and scanning electron microscope (SEM) analyses. Almost all of products were obtained in high yields as well as short reaction times and the catalyst was also reused eight times without loss of its catalytic activity. In the experiment, the researchers used many compounds, for example, 3-Pyridinemethanol(cas: 100-55-0HPLC of Formula: 100-55-0)

3-Pyridinemethanol(cas: 100-55-0) belongs to pyridine. Pyridine derivatives lend themselves to many roles in the spirited field of supramolecular chemistry – whether as the ligand backbone of metal-organic polymers or presiding over the key electronic stations of nanodevices. In biochemistry, pyridine-containing cofactors are necessary nutrients on which our lives depend. HPLC of Formula: 100-55-0

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Safety of 3,5-DihydroxybenzaldehydeIn 2019 ,《Small molecule inhibitors of the BfrB-Bfd interaction decrease Pseudomonas aeruginosa fitness and potentiate fluoroquinolone activity》 appeared in Journal of the American Chemical Society. The author of the article were Punchi Hewage, Achala N. D.; Yao, Huili; Nammalwar, Baskar; Gnanasekaran, Krishna Kumar; Lovell, Scott; Bunce, Richard A.; Eshelman, Kate; Phaniraj, Sahishna M.; Lee, Molly M.; Peterson, Blake R.; Battaile, Kevin P.; Reitz, Allen B.; Rivera, Mario. The article conveys some information:

The iron storage protein bacterioferritin (BfrB) is central to bacterial iron homeostasis. The mobilization of iron from BfrB, which requires binding by a cognate ferredoxin (Bfd), is essential to the regulation of cytosolic iron levels in P. aeruginosa. This paper describes the structure-guided development of small mol. inhibitors of the BfrB-Bfd protein-protein interaction. The process was initiated by screening a fragment library and followed by obtaining the structure of a fragment hit bound to BfrB. The structural insights were used to develop a series of 4-(benzylamino)- and 4-((3-phenylpropyl)amino)-isoindoline-1,3-dione analogs that selectively bind BfrB at the Bfd binding site. Challenging P. aeruginosa cells with the 4-substituted isoindoline analogs revealed a dose-dependent growth phenotype. Further investigation determined that the analogs elicit a pyoverdin hyperprodn. phenotype that is consistent with blockade of the BfrB-Bfd interaction and ensuing irreversible accumulation of iron in BfrB, with concomitant depletion of iron in the cytosol. The irreversible accumulation of iron in BfrB prompted by the 4-substituted isoindoline analogs was confirmed by visualization of BfrB-iron in P. aeruginosa cell lysates separated on native PAGE gels and stained for iron with Ferene S. Challenging P. aeruginosa cultures with a combination of com. fluoroquinolone and our isoindoline analogs results in significantly lower cell survival relative to treatment with either antibiotic or analog alone. Collectively, these findings furnish proof of concept for the usefulness of small mol. probes designed to dysregulate bacterial iron homeostasis by targeting a protein-protein interaction pivotal for iron storage in the bacterial cell. The experimental process involved the reaction of 3,5-Dihydroxybenzaldehyde(cas: 26153-38-8Safety of 3,5-Dihydroxybenzaldehyde)

3,5-Dihydroxybenzaldehyde(cas: 26153-38-8) is a building block. It has been used in the synthesis of 2,4-dimethylbenzoylhydrazones with antileishmanial and antioxidant activities.Safety of 3,5-Dihydroxybenzaldehyde

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

《Application of two advanced derivative spectrophotometric methods for simultaneous estimation of salbutamol sulphate, ambroxol hydrochloride and theophylline in pure and commercial formulations》 was written by Dave, H. N.; Mashru, R. C.. Reference of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride And the article was included in International Journal of Current Pharmaceutical Research in 2022. The article conveys some information:

Two advanced spectrophotometric methods have been proposed for the simultaneous determination of Salbutamol sulfate, Ambroxol hydrochloride and Theophylline in pure and pharmaceutical formulations. The proposed methods exclude the hectic steps of time-consuming sample preparations or purification or separation steps. There is no any spectrophotometric method has been avail for simultaneous estimation of the ternary mixture containing Salbutamol sulfate, Ambroxol hydrochloride and Theophylline. The methods are derivative ratio spectra zero-crossing method and double divisor ratio spectra derivative method resp. Both the methods are found to be rapid, accurate, precise, reliable and economical as well. The developed methods show best results in terms of linearity, accuracy, precision, limit of detection and limit of quantification for standard laboratory mixtures of pure drugs and marketed formulations. The range for Salbutamol sulfate, Ambroxol hydrochloride and Theophyllineare found to be 1-35μg ml-1, 5-35μg ml-1 and 6-60μg ml-1 resp. For the derivative ratio spectra zero-crossing method, the values of the limit of detection are found to be 0.3161μg ml-1, 0.2212μg ml-1 and 0.2910μg ml-1 and the values limit of quantification are found to be 0.9571μg ml-1, 0.7412μg ml-1 and 0.9671μg ml-1 for Salbutamol sulfate, Ambroxol hydrochloride and Theophylline resp. For double divisor ratio spectra derivative method, limit of detection values is found to be 0.3251μg ml-1, 0.2591μg ml-1 and 0.2640μg ml-1 and the limit of quantification values are found to be 0.9870μg ml-1, 0.8650μg ml-1 and 0.8812μg ml-1 for Salbutamol sulfate, Ambroxol hydrochloride and Theophylline resp. The common excipients and additives did not interfere in the determinations of any of the drugs while being analyzed for com. formulations. These two spectrophotometric methods, which determine SS, AH, and THE simultaneously, are simple, specific, accurate, precise, rapidly, and economically, indicating that they can be used routinely in pharmaceutical anal. As a result, derivative spectrophotometry may be used effectively for the simultaneous determination of SS, AH and THE in the combined dosage forms without any prior separation of individual drugs. The experimental process involved the reaction of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride(cas: 23828-92-4Reference of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride)

trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride(cas: 23828-92-4) enhances pulmonary surfactant production and stimulates ciliary activity.Reference of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride It promotes mucus clearance, facilitates expectoration and eases productive cough, allowing patients to breathe.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

《Spontaneous Evolution of the Domain Structure and Dielectric Relaxation in Crystals of Triglycine Sulfate and Rochelle Salt》 was written by Golitsyna, O. M.; Drozhdin, S. N.. Application of 6381-59-5This research focused ontriglycine sulfate rochelle salt dielec relaxation permittivity annealing. The article conveys some information:

Short-term annealing in the paraelec. phase causes an exponential drop in the dielec. permittivity in the ferroelec. phase of triglycine sulfate (TGS) crystals and Rochelle salt crystals. This is due to the spontaneous enlargement of the nonequilibrium domain structure of these crystals. Introducing radiation or impurity defects into a TGS crystal accelerates the processes of dielec. relaxation with their localization near TC only. The results came from multiple reactions, including the reaction of Potassium sodium (2R,3R)-2,3-dihydroxysuccinate tetrahydrate(cas: 6381-59-5Application of 6381-59-5)

Potassium sodium (2R,3R)-2,3-dihydroxysuccinate tetrahydrate(cas: 6381-59-5) is a ferroelectric crystal with a high piezoelectric effect and electromechanical coupling coefficient. Application of 6381-59-5 Potassium sodium tartrate tetrahydrate has been used in the preparation of Lowry reagent for the determination of microsomal protein concentration in rat hepatic microsomes by Lowry method.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

SDS of cas: 1082066-29-2On October 2, 2019 ,《Para-Selective, Iridium-Catalyzed C-H Borylations of Sulfated Phenols, Benzyl Alcohols, and Anilines Directed by Ion-Pair Electrostatic Interactions》 was published in Journal of the American Chemical Society. The article was written by Montero Bastidas, Jose R.; Oleskey, Thomas J.; Miller, Susanne L.; Smith, Milton R.; Maleczka, Robert E.. The article contains the following contents:

Para C-H borylations (CHB) of tetraalkylammonium sulfates [R4N][ArOSO3] (R = n-Pr, Bu) and sulfamates [Bu4N][ArNHSO3] have been achieved using bipyridine-ligated Ir boryl catalysts, 4,4′-R2bpy/[Ir(cod)(OMe)]2/B2pin2, yielding borylated phenols 4-(pinB)-RC6H3OH (R = halo, Me, CN, CF3, CF3O, OMe), together with minor amounts of meta-isomers. Selectivities can be modulated by both the length of the alkyl groups in the tetraalkylammonium cations and the substituents on the bipyridine ligands. Ion pairing, where the alkyl groups of the cation shield the meta C-H bonds in the counteranions, is proposed to account for para selectivity. The 4,4′-dimethoxy-2,2′-bipyridine ligand gave superior selectivities. In the experiment, the researchers used many compounds, for example, (2-Fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methanol(cas: 1082066-29-2SDS of cas: 1082066-29-2)

(2-Fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methanol(cas: 1082066-29-2) belongs to organoboron compounds. Organoboron compounds are versatile intermediates and as such are some of the most important classes of reagents in modern organic chemistry. Organoboron compounds are less toxic than organostannane reagents, and unlike alkynylzinc and magnesium, many organoboron compounds possess remarkable oxidative and thermal stabilities. SDS of cas: 1082066-29-2

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

The author of 《Quality by design approach to develop stability indicating reversed-phase high-performance liquid chromatography method development for ambroxol》 were Ahmad, Sufiyan; Khabiya, Pranit; Au, Tatiya; Bakhshi, Abdurl Raheman. And the article was published in Asian Journal of Pharmaceutical and Clinical Research in 2021. Safety of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride The author mentioned the following in the article:

As per requisition of current regulatory requirements, simple, rapid and sensitive method by 33 factorial quality by design approach was established and validated for Ambroxol (AMB) by reversed-phase high-performance liquid chromatog. (RP-HPLC). A simple RP-HPLC method has been developed and validated with different parameters such as linearity, precision, repeatability, limit of detection (LOD), limit of quantitation (LOQ), accuracy as per International Conference for Harmonisation guidelines (Q2R1). Statistical data anal. was done for data obtained from different aliquots Runs on Agilent Tech. Gradient System with Auto injector, UV diode-array detection and Gradient Detector. Equipped with Reverse Phase (Agilent) C18 column (4.6 mm x 100 mm; 2.5μm), a 20μl injection loop and UV730D Absorbance detector at 244 nm wave length and running chemstation 10.1 software and drugs along with degradants were separated via Methanol: (0.1% orthophosphoric acid) Water (75:25) of pH 3 as mobile phase setting flow rate 0.7 mL/min at ambient temperature the retention time of AMB were found to be 4.85 min. The industrialized method was found linear over the concentration range of 10-50μg/mL for AMB while the LOD and LOQ of AMB was found to be 0.5174-0.2739μg/mL, anal. method that concluded. There are no interfering peaks underperformed degradation conditions. Therefore, a sensitive, robust, accurate, and stability indicating method was developed with high degree of practical utility. In the experimental materials used by the author, we found trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride(cas: 23828-92-4Safety of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride)

trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride(cas: 23828-92-4) is a mucolytic expectorant and a metabolite of bromhexine.Safety of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride It is used in the treatment of respiratory disorders characterized by viscous or excessive mucus.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

The author of 《Iron-catalysed enantioselective Suzuki-Miyaura coupling of racemic alkyl bromides》 were Iwamoto, Takahiro; Okuzono, Chiemi; Adak, Laksmikanta; Jin, Masayoshi; Nakamura, Masaharu. And the article was published in Chemical Communications (Cambridge, United Kingdom) in 2019. Formula: C12H17BO2 The author mentioned the following in the article:

The first iron-catalyzed enantioselective Suzuki-Miyaura coupling reaction has been developed. In the presence of catalytic amounts of FeCl2 and (R,R)-QuinoxP*, lithium arylborates are cross-coupled with tert-Bu α-bromopropionate in an enantioconvergent manner, enabling facile access to various optically active α-arylpropionic acids including several nonsteroidal anti-inflammatory drugs (NSAIDs) of com. importance. (R,R)-QuinoxP* is specifically able to induce chirality when compared to analogous P-chiral ligands that give racemic products, highlighting the critical importance of transmetalation in the present asym. cross-coupling system. In the part of experimental materials, we found many familiar compounds, such as 4,4,5,5-Tetramethyl-2-phenyl-1,3,2-dioxaborolane(cas: 24388-23-6Formula: C12H17BO2)

4,4,5,5-Tetramethyl-2-phenyl-1,3,2-dioxaborolane(cas: 24388-23-6) can be used to prepare sulfinamide derivatives by reacting with diethylaminosulfur trifluoride (DAST) and potassium phenyltrifluoroborate.Formula: C12H17BO2

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

《Theophylline as a Green Catalyst for the Synthesis of 1H-Pyrazolo[1,2-b]phthalazine-5,10-diones》 was written by Mohamadpour, Farzaneh. Name: 3-Hydroxybenzaldehyde And the article was included in Organic Preparations and Procedures International in 2020. The article conveys some information:

A green, readily available, and inexpensive method is developed to synthesize 1H-Pyrazolo[1,2-b]phthalazine-5,10-diones. Theophylline has shown significant potential to be an alternative green catalyst for the synthesis of these valuable heterocyclic compounds In the part of experimental materials, we found many familiar compounds, such as 3-Hydroxybenzaldehyde(cas: 100-83-4Name: 3-Hydroxybenzaldehyde)

3-Hydroxybenzaldehyde(cas: 100-83-4) is used as an ionophore, during the development of an highly selective and sensitive PVC membrane sensor, which can be used as a Tb3+ ion selective electrode.Name: 3-Hydroxybenzaldehyde

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Category: alcohols-buliding-blocksIn 2019 ,《Rapid Solution-Phase Hydrogen/Deuterium Exchange for Metabolite Compound Identification》 was published in Journal of the American Society for Mass Spectrometry. The article was written by Majuta, Sandra N.; Li, Chong; Jayasundara, Kinkini; Kiani Karanji, Ahmad; Attanayake, Kushani; Ranganathan, Nandhini; Li, Peng; Valentine, Stephen J.. The article contains the following contents:

Rapid, solution-phase hydrogen/deuterium exchange (HDX) coupled with mass spectrometry (MS) is demonstrated as a means for distinguishing small-mol. metabolites. HDX is achieved using capillary vibrating sharp-edge spray ionization (cVSSI) to allow sufficient time for reagent mixing and exchange in micrometer-sized droplets. Different compounds are observed to incorporate deuterium with varying efficiencies resulting in unique isotopic patterns as revealed in the MS spectra. Using linear regression techniques, parameters representing contribution to exchange by different hydrogen types can be computed. In this proof-of-concept study, the exchange parameters are shown to be useful in the retrodiction of the amount of deuterium incorporated within different compounds On average, the exchange parameters retrodict the exchange level with ∼ 2.2-fold greater accuracy than treating all exchangeable hydrogens equally. The parameters can be used to produce hypothetical isotopic distributions that agree (± 16% RMSD) with exptl. measurements. These initial studies are discussed in light of their potential value for identifying challenging metabolite species. [Figure not available: see fulltext.]. In the part of experimental materials, we found many familiar compounds, such as 3-Aminopropan-1-ol(cas: 156-87-6Category: alcohols-buliding-blocks)

3-Aminopropan-1-ol(cas: 156-87-6) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Category: alcohols-buliding-blocks

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts