Month: October 2022

In 2020,World Journal of Pharmaceutical Research included an article by Naykodi, Pradnya S.; Bidkar, Shital J.; More, Komal V.; Dighe, Ajinkya D.. Category: alcohols-buliding-blocks. The article was titled 《Taste masking of bitter drugs by using ion exchange resin method》. The information in the text is summarized as follows:

The various organoleptic properties such as taste, smell, texture also these are important factor in development of oral dosage forms. The taste is the major factor that affect the patient compliance and product quality. Acceptability of any dosage form mainly depends over its taste i.e. mouth feel. Drug mol. interact with taste receptor on the tongue to give bitter, sweet or other taste sensation, when they dissolve in saliva. The taste buds shows the sensation of taste by signal transduction from the receptor organs. Now a days most of the potent drugs that are cardiac, analgesic, anti-inflammatory, anti-tubercular, antibacterial, anthalmetics, antimalarial, antiepileptics, anticoagulants, histamine receptor agonist, antithyroids, antineoplastic, antiprotozoal, diuretics, nutritional agents, opioid analgesic, sex hormones, vaccines most of them are bitter in taste. So it become a necessary to develop such a dosage form that is acceptable for its taste by patients especially children or geriatrics. It becomes a challenge for pharmacist to make palatable formulation by masking the bitter taste of the drug. In the part of experimental materials, we found many familiar compounds, such as trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride(cas: 23828-92-4Category: alcohols-buliding-blocks)

trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride(cas: 23828-92-4) is a medication indicated to alleviate chest congestion associated with conditions that include bronchitis, pneumonia, bronchospasm asthma, cough, and allergy.Category: alcohols-buliding-blocks Preclinically, ambroxol, the active ingredient of Mucosolvan, has been shown to increase respiratory tract secretion.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Kadri, Safwen; El Ayed, Mohamed; Mabrouk, Maha; Limam, Ferid; Elkahoui, Salem; Aouani, Ezzedine; Mokni, Meherzia published an article on February 5 ,2019. The article was titled 《Characterization, anti-oxidative effect of grape seed powder and in silico affinity profiling of polyphenolic and extra-phenolic compounds for calpain inhibition》, and you may find the article in Journal of Pharmaceutical and Biomedical Analysis.Safety of rel-(3R,4S,5S,6R)-6-(Hydroxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetraol The information in the text is summarized as follows:

Vitis vinifera grape is a highly cultivated crop and solid wastes generated by the wine industry are largely under exploited. Plentiful studies have intended analyzing the polyphenolic content of grape seeds but characterization of non phenolic compounds is rather scarce. The present study aimed at the selective extraction of lipid, phenolic and aqueous phases from grape seed powder (GSP) in order to establish their intimate composition, as well as their antioxidant and chelating properties underlying partly their biol. effects. Major non phenolic compounds identified in the lipid phase were glyceryl-monostearate and 2-monostearin whereas fructofuranose and sucrose were the most abundant in the aqueous phase. Among the most abundant compounds detected in the various phases, the polyphenol quercetin exhibited the best affinity and free binding energy towards the active site of the calcium-dependent protease calpain. Polyphenols likely constitute the bioactive part of GSP that should be exploited as safe modulators of intracellular signaling which is likely at the basis of their health beneficial effects. Nevertheless other compounds as lipids or sugars should be valorized along with polyphenols to improve their bioavailability into highly protected organs as brain or eye. The experimental process involved the reaction of rel-(3R,4S,5S,6R)-6-(Hydroxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetraol(cas: 54-17-1Safety of rel-(3R,4S,5S,6R)-6-(Hydroxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetraol)

rel-(3R,4S,5S,6R)-6-(Hydroxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetraol(cas: 54-17-1) is oxidized in various tissues under either aerobic or anaerobic conditions through glycolysis; the oxidation reaction produces carbon dioxide, water, and ATP.Safety of rel-(3R,4S,5S,6R)-6-(Hydroxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetraol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Mertins, Kristin; Zapf, Alexander; Beller, Matthias published an article in Journal of Molecular Catalysis A: Chemical. The title of the article was 《Catalytic borylation of o-xylene and heteroarenes via C-H activation》.Name: 2-(3,4-Dimethylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane The author mentioned the following in the article:

Ir and Rh complexes catalyze the borylation of xylene and different heteroarenes using pinacolborane via C-H activation. Various five-membered heterocycles such as thiophene, pyrrole, thionaphthene, and indole derivatives yield the borylated products in moderate to good yields. In general, the reactions proceed with high selectivity to give borylation ortho to the heteroatom. The experimental process involved the reaction of 2-(3,4-Dimethylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane(cas: 401797-00-0Name: 2-(3,4-Dimethylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane)

2-(3,4-Dimethylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane(cas: 401797-00-0) belongs to hydroxy-containing compounds. Hydroxy groups participate in the dehydration reactions that link simple biological molecules into long chains. The joining of a fatty acid to glycerol to form a triacylglycerol removes the −OH from the carboxy end of the fatty acid.Name: 2-(3,4-Dimethylphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Siddiqui, Bina S.; Adil, Qayyum; Begum, Sabira; Siddiqui, Salimuzzaman published an article in Pakistan Journal of Pharmaceutical Sciences. The title of the article was 《Synthesis of alkyl catechols and evaluation of their antibacterial and cytotoxic activity》.Safety of 4-Butylbenzene-1,2-diol The author mentioned the following in the article:

A series of potential biol. active mono-, di- and tetra- alkyl catechols were prepared through Friedel- Crafts alkylation of catechol, and evaluated for their antibacterial and cytotoxic activity. The mono-substituted alkyl derivatives showed maximum antibacterial activity in vitro which increased with the increasing length of the alkyl chains. Primary screening results indicated that all the monoalkyl derivatives except 4- (2-octyl) catechol inhibited the growth of Bordetella bronchoseptica and maximum zones of inhibition were observed in case of monohexyl catechols (both n- and 2-hexyl) and monobenzyl derivative In case of Gram-neg. organisms growth of Klebsiella pneumoniae and Acinetobacter calcoaceticus was inhibited by several derivatives Mono-3-octyl-, monononyl- and monobenzyl catechols markedly inhibited the growth of Kl. pneumoniae. Mono-2-heptyl catechol inhibited the growth of six Gram-neg. bacteria. Min. inhibitory concentration of six most active compounds of the series was determined against Gram-pos. and Gram-neg. organisms; it ranged from > 100 μg/mL to 10μg/mL. The antibacterial activity of catechol was not significant. Cytotoxicity test done by brine shrimp assays showed that the order of cytotoxicity decreases in going from mono- to tetra- alkyl catechols, and among the mono- alkyl products, a decrease in order of cytotoxicity was noted in going from mono-Me catechol (LD50 = 59) to monopentyl catechol (LD50 = 173) after which the order of cytotoxicity gradually increased up to the largest alkyl substituent tested i.e. monononyl catechol (LD50 = 114). Me and Et catechol, which were almost inactive in respect of their antibacterial activity possessed pronounced cytotoxicity as compared to higher homologs. Catechol itself did not show significant cytotoxicity (LD50 = 393.27). The results came from multiple reactions, including the reaction of 4-Butylbenzene-1,2-diol(cas: 2525-05-5Safety of 4-Butylbenzene-1,2-diol)

4-Butylbenzene-1,2-diol(cas: 2525-05-5) 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. Safety of 4-Butylbenzene-1,2-diol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2012,Roughley, Stephen D.; Browne, Helen; Macias, Alba T.; Benwell, Karen; Brooks, Teresa; D’Alessandro, Jalanie; Daniels, Zoe; Dugdale, Sarah; Francis, Geraint; Gibbons, Ben; Hart, Terance; Haymes, Timothy; Kennett, Guy; Lightowler, Sean; Matassova, Natalia; Mansell, Howard; Merrett, Angela; Misra, Anil; Padfield, Anthony; Parsons, Rachel; Pratt, Robert; Robertson, Alan; Simmonite, Heather; Tan, Kiri; Walls, Steven B.; Wong, Melanie published 《Fatty acid amide hydrolase inhibitors. 3: Tetra-substituted azetidine ureas with in vivo activity》.Bioorganic & Medicinal Chemistry Letters published the findings.HPLC of Formula: 18621-18-6 The information in the text is summarized as follows:

Attempts to optimize the human fatty acid amide hydrolase (FAAH) inhibition and physicochem. properties of previously reported tetrasubstituted azetidine urea FAAH inhibitor, VER-156084, are reported. The SAR of a series of analogs and in vivo dose-dependent FAAH inhibition in an anandamide-loading study in rats were determined The experimental part of the paper was very detailed, including the reaction process of Azetidin-3-ol hydrochloride(cas: 18621-18-6HPLC of Formula: 18621-18-6)

Azetidin-3-ol hydrochloride(cas:18621-18-6) is one of azetidine.Azetidines (azacyclobutanes) constitute a well-known class of heterocyclic compounds. Azetidine scaffold has been discovered in several natural products.HPLC of Formula: 18621-18-6 Several pharmacologically important synthetic compounds also contain azetidine ring. Because of inherent ring strain, the synthesis of azetidines is a challenging endeavor.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2018,Ke, Bowen; Ma, Lin; Kang, Ting; He, Wei; Gou, Xueyan; Gong, Deying; Du, Lupei; Li, Minyong published 《In Vivo Bioluminescence Imaging of Cobalt Accumulation in a Mouse Model》.Analytical Chemistry (Washington, DC, United States) published the findings.HPLC of Formula: 1195-59-1 The information in the text is summarized as follows:

As a trace element nutrient, cobalt is critical for both prokaryotes and eukaryotes. In the current study, a turn-on Cobalt Bioluminescent Probe 1 (CBP-1) for the detection of cobalt has been successfully developed based on oxidative C-O bond cleavage. This probe exhibited high selectivity and sensitivity toward cobalt over other analytes. By using CBP-1, the successful in vivo imaging of cobalt accumulation was carried out in a mouse model. Such an ability to determine cobalt in living animals provides a powerful technol. for studying the system distribution, toxic potency, and biol. effect of Co2+. The experimental part of the paper was very detailed, including the reaction process of 2,6-Pyridinedimethanol(cas: 1195-59-1HPLC of Formula: 1195-59-1)

2,6-Pyridinedimethanol(cas: 1195-59-1) belongs to pyridine. Pyridine’s structure is isoelectronic with that of benzene, but its properties are quite different. Pyridine is completely miscible with water, whereas benzene is only slightly soluble. Like all hydrocarbons, benzene is neutral (in the acid–base sense), but because of its nitrogen atom, pyridine is a weak base.HPLC of Formula: 1195-59-1

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2018,Hu, Fang; Yuan, Youyong; Wu, Wenbo; Mao, Duo; Liu, Bin published 《Dual-Responsive Metabolic Precursor and Light-Up AIEgen for Cancer Cell Bio-orthogonal Labeling and Precise Ablation》.Analytical Chemistry (Washington, DC, United States) published the findings.Quality Control of 3,5-Dihydroxybenzaldehyde The information in the text is summarized as follows:

Metabolic glycoengineering of unnatural glycans with bio-orthogonal chem. groups and a subsequent click reaction with fluorescent probes have been widely used in monitoring various bioprocesses. Herein, we developed a dual-responsive metabolic precursor that could specifically generate unnatural glycans with azide groups on the membrane of targeted cancer cells with high selectivity. Moreover, a water-soluble fluorescent light-up probe with aggregation-induced emission (AIE) was synthesized, which turned its fluorescence on upon a click reaction with azide groups on the cancer cell surface, enabling special cancer cell imaging with low background signal. Furthermore, the probe can generate 1O2 upon light irradiation, fulfilling its dual role as an imaging and therapeutic agent for cancer cells. Therefore, the concepts of the cancer-cell-specific metabolic precursor cRGD-S-Ac3ManNAz and the AIE light-up probe are promising in bio-orthogonal labeling and cancer-specific imaging and therapy. The results came from multiple reactions, including the reaction of 3,5-Dihydroxybenzaldehyde(cas: 26153-38-8Quality Control of 3,5-Dihydroxybenzaldehyde)

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.Quality Control of 3,5-Dihydroxybenzaldehyde

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2019,Biochimica et Biophysica Acta, Biomembranes included an article by Sivaramakrishna, D.; Prasad, Muvva D.; Swamy, Musti J.. Name: 2-Aminopropane-1,3-diol. The article was titled 《A homologous series of apoptosis-inducing N-acylserinols: Thermotropic phase behavior, interaction with cholesterol and characterization of cationic N-myristoylserinol-cholesterol-CTAB niosomes》. The information in the text is summarized as follows:

N-Acylserinols (NASOHs) exhibit anti-cancer activity by elevating ceramide levels, and/or by activating proapoptotic effectors. In the present work we investigated the thermotropic phase behavior and supramol. organization of a homologous series of NASOHs (number of C-atoms in the acyl chain, n = 8-18), and the interaction of N-myristoylserinol (NMSOH) with cholesterol, and characterized cationic niosomes made up of NMSOH, cholesterol and cetyltrimethylammonium bromide (CTAB). Differential scanning calorimetric studies revealed that NASOHs exhibit a major chain-melting phase transition in both dry and hydrated states. The thermodn. parameters, transition enthalpy and entropy show linear dependence on the acyl chain length in the dry state, but exhibit odd-even alternation in the hydrated state. Powder X-ray diffraction studies revealed that NASOHs adopt a tilted bilayer structure, wherein the bilayer repeat distances (d-spacings) also showed odd-even alteration, with even-chainlength compounds exhibiting slightly higher d-spacings. Studies on the interaction between NMSOH and cholesterol revealed that both lipids mix well with up to 55 mol% cholesterol, whereas phase separation was observed at higher cholesterol content. The transition enthalpy corresponding to the NMSOH-cholesterol complex increases up to 55 mol% cholesterol and decreases at higher cholesterol content. Presence of the cationic surfactant CTAB affects the phase behavior, fluidity and size of the NMSOH-cholesterol (45,55, mol/mol) niosomes, with unilamellar vesicles of about 85 (±20) nm in diameter being obtained at 10 mol% CTAB. These results provide a thermodn. and structural basis for further investigations on these cationic niosomes towards their use in drug delivery applications, especially for anticancer drugs. After reading the article, we found that the author used 2-Aminopropane-1,3-diol(cas: 534-03-2Name: 2-Aminopropane-1,3-diol)

2-Aminopropane-1,3-diol(cas: 534-03-2) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Name: 2-Aminopropane-1,3-diol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2019,Chemical Communications (Cambridge, United Kingdom) included an article by Liu, Yi-Yin; Liang, Dong; Lu, Liang-Qiu; Xiao, Wen-Jing. Computed Properties of C3H9NO. The article was titled 《Practical heterogeneous photoredox/nickel dual catalysis for C-N and C-O coupling reactions》. The information in the text is summarized as follows:

Efficient C-N and C-O coupling reactions of aryl halides with amines and alcs. have been developed by using the strategy of heterogeneous visible light photoredox and nickel dual catalysis. Obviously, the joint use of inexpensive and bench-stable CdS and nickel salts, together with mild reaction conditions, makes these two transformations attractive for the synthetic community. This heterogeneous dual catalysis system also proved to be successful in the ligand-free catalytic hydroxylation of aryl bromide with water as a nucleophile. The practicality of this protocol is further emphasized by the scaled-up reaction and the reusability of heterogeneous photocatalysts. In the experiment, the researchers used 3-Aminopropan-1-ol(cas: 156-87-6Computed Properties of C3H9NO)

3-Aminopropan-1-ol(cas: 156-87-6) belongs to anime. In organic chemistry, amines are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (NH3), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines).Computed Properties of C3H9NO

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

In 2019,Chemical Communications (Cambridge, United Kingdom) included an article by Bera, Atanu; Sk, Motahar; Singh, Khushboo; Banerjee, Debasis. Product Details of 873-75-6. The article was titled 《Nickel-catalyzed dehydrogenative coupling of aromatic diamines with alcohols: selective synthesis of substituted benzimidazoles and quinoxalines》. The information in the text is summarized as follows:

The first nickel-catalyzed dehydrogenative coupling of primary alcs. and ethylene glycol with aromatic diamines for selective synthesis of mono- and di-substituted benzimidazoles and quinoxalines is reported. The earth-abundant, non-precious and simple NiCl2/1,10-phenanthroline system enables the synthesis of N-heterocycles releasing water and hydrogen gas as byproducts. Mechanistic studies involving deuterium labeling experiments and quant. determination of hydrogen gas evaluation were performed. In the experiment, the researchers used many compounds, for example, (4-Bromophenyl)methanol(cas: 873-75-6Product Details of 873-75-6)

(4-Bromophenyl)methanol(cas: 873-75-6) undergoes three-component reaction with acetylferrocene and arylboronic acid to give ferrocenyl ketones containing biaryls.Product Details of 873-75-6 It undergoes efficient trimethylsilylation reaction with 1,1,1,3,3,3-hexamethyldisilazane in the presence of catalytic amount of aspartic acid in acetonitrile.

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts