Tag: M.W=400-450

Bhatnagar, Madhu published the artcileThe in vitro effects of anthelmintics on phosphatases of sheep nodular worm, Recommanded Product: N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, the publication is Indian Journal of Parasitology (1987), 11(2), 201-3, database is CAplus.

When tested in vitro, piperazine at 10 and 50 μg/mL inhibited acid phosphatase by 3.6 and 14.96%, resp., and activated alk. phosphatase by 2.35 and 5.9%, resp. Treatment with bephenium hydroxynaphoate at 10 and 50 μg/mL, inhibited acid phosphatase by 11.56 and 58.5%, resp., and increased alk. phosphatase by 11.8 and 55.3%, resp. Mebendazole at 10 and 50 μg/mL inhibited acid phosphatase by 64.6 and 93.87%, resp., and activated alk. phosphatase by 31.5 and 85.5%, resp. Thus, mebendazole showed the max inhibition of acid phosphatase and piperazine the least.

Indian Journal of Parasitology 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, Recommanded Product: N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate.

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

Gladkikh, V. F. published the artcileChanges in the stomach of small laboratory animals after oral administration of naphthamone and diphesyl, COA of Formula: C28H29NO4, the publication is Meditsinskaya Parazitologiya i Parazitarnye Bolezni (1972), 41(4), 423-8, database is CAplus and MEDLINE.

Rats, mice, guinea pigs, and cats, given orally repeated toxic doses of the antihelminthic compounds diphesyl (I) [34987-38-7] and naphthamone [3818-50-6] showed inflammation of the gastric mucosa, proliferation of the superficial squamous epithelium, and hyperkeratosis of the forestomach. These effects were reversible, and were probably due to the hydroxynaphthoate anion in the drugs.

Meditsinskaya Parazitologiya i Parazitarnye Bolezni 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

Li, Shengke published the artcileSupramolecular Modulation of Antibacterial Activity of Ambroxol by Cucurbit[7]uril, Application of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, the publication is ChemPlusChem (2020), 85(4), 679-683, database is CAplus and MEDLINE.

Supramol. encapsulation by cucurbit[7]uril (CB[7]) was recently demonstrated to provide a simple and efficient method for antibacterial activity regulation of antibiotics. In this work, CB[7] was shown to form binary host-guest complex with ambroxol hydrochloride (ABX), a clin. mucokinetic and expectorant drug, which was reported to exhibit certain antibacterial activity. ¹H NMR titration and isothermal titration calorimetry experiment results suggested that the 4-hydroxyl cyclohexylamine group of ABX was included inside the CB[7] cavity, with a binding constant K_a of (6.69±0.11)×10⁵ M^-1 in phosphate buffered saline (PBS) solution, thermodynamically driven by both enthalpy change and entropy. More importantly, ABX’s inhibitory activity (MIC₅₀) against bacillary strains towards Pseudomonas aeruginosa and Escherichia coli strains was decreased from (5.11±0.31)×10^-6 M^-1 and (2.63±0.34)×10^-5 M^-1 to zero upon encapsulation by CB[7], and was subsequently recovered to almost its original activity when a competitive guest, amantadine hydrochloride, for disassembling CB[7]-ABX complex, was added, suggesting that the antibacterial activity of ABX could be readily “turned off/on” upon its complexation and decomplexation with CB[7].

ChemPlusChem 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 of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride.

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

Shuto, Ayumi published the artcileπ-Extended Planarized Triphenylboranes with Thiophene Spacers, Application of 5,5′-Bis(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2,2′-bithiophene, the publication is Organic Letters (2013), 15(24), 6234-6237, database is CAplus and MEDLINE.

Planarized triphenylboranes extended with thiophene or bithiophene spacers were synthesized, which showed intense fluorescences in solution and reversible redox waves for reduction in cyclic voltammetry. Organic light-emitting diodes (OLEDs) using these compounds as an electron-transporting material were fabricated.

Organic Letters 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 C17H19N3O6, Application of 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

Krotov, A. I. published the artcileActivity of some quaternary salts of β-aryloxyethylaralkylammonium during the infection of mice by Nippostrongylus brasiliensis, Application In Synthesis of 3818-50-6, the publication is Meditsinskaya Parazitologiya i Parazitarnye Bolezni (1968), 37(3), 361-4, database is CAplus.

Some quaternary salts of β-aryloxyethylaralkylammonium were synthesized and tested in Nippostrongylus braziliensis exptl. infection in mice. The anthelmintic drug naphthamone (N-(β-phenoxyethyl)-N,N-dimethyl-N-benzylammonium β-hydroxynaphthoate) served as a standard. Changes in the cation portion of the napthamone mol. by introduction of various substitutes (e.g. CHO, OH) in the phenoxygroup, or substitution of the latter by the naphthoxy group, gave inactive compounds Introduction of naphthyl, imidazolyl, and other groups instead of the benzyl group results in reduction of the activity, whereas the presence of the thenyl group preserved the activity. The most active compound was bephenium salicylate; bephenium α-bromo-β-hydroxynaphthoate was inactive.

Meditsinskaya Parazitologiya i Parazitarnye Bolezni 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, Application In Synthesis of 3818-50-6.

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

Dore, J. C. published the artcileInformation processing manipulation of developed formulas for structure-activity relation studies. Application to antiparasitic drugs, Computed Properties of 3818-50-6, the publication is Journal de Pharmacie de Belgique (1990), 45(6), 375-84, database is CAplus.

A method is described for structure-activity relationship studies using algorithms based on mol. connectivity matrixes of atoms, bonds, chem. functional groups, and mol. fragments. Common features of a group of different compounds with the same pharmacol. activity can be determined with this method. A network (Prim’s tree) relating chem. structures to activities can be designed from the data obtained. New compounds placed in the network can be tested for their expected activities. The method was applied to a group of 50 antiparasitic drugs.

Journal de Pharmacie de Belgique 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, Computed Properties of 3818-50-6.

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

Monton, Chaowalit published the artcileCharacterization of crosslinked hard gelatin capsules for a structural assembly of elementary osmotic pump delivery system, Recommanded Product: trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, the publication is Journal of Pharmaceutical Investigation (2019), 49(6), 655-665, database is CAplus.

The objective of this study was to characterize the crosslinked hard gelatin capsules (HGCs) for use as a structural assembly of elementary osmotic pumps (EOP). HGCs were crosslinked in formaldehyde vapor for 6, 12, and 24 h. Weight loss after immersing in various mediums, water soluble protein fraction, loss on drying, and formaldehyde residue were investigated. Fourier transform IR (FTIR) spectra were used to detect the crosslinking formation. The EOP capsules were prepared for delivery of diltiazem hydrochloride (DIL HCl) and ambroxol hydrochloride (AMB HCl), which are freely and sparingly water soluble drugs, resp. Physicochem. stability of storage crosslinked HGC shells was investigated. All crosslinked HGC shells were water insoluble FTIR spectra exhibited intermediate lysine methylol and arginine methylol peaks. Storage time increased, moisture content increased and formaldehyde residue decreased. The developing EOP capsules were more appropriate for delivery of high water soluble rather than low water soluble drug. EOP capsule contained 100 mg DIL HCl using HGCs crosslinked for 12 h provided release profiles for 12 h with a lag time of 2.6-3.1 h. It was also found that DIL HCl EOP capsules prepared using crosslinked HGC shells stored for 90 days maintained the similar drug release profiles. AMB HCl EOP capsules exhibited low drug release. In summary, the crosslinked HGCs were applicable as a structural assembly of the osmotic controlled drug delivery system.

Journal of Pharmaceutical Investigation 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, Recommanded Product: trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride.

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

Manjunatha, N. K. published the artcileSolid state and Computational studies of Ambroxol hydrochloride drug, COA of Formula: C13H19Br2ClN2O, the publication is Chemical Data Collections (2020), 100377, database is CAplus.

The title compound Ambroxol hydrochloride salt or 4-[(2-amino-3, 5-dibromophenyl) Me amino] cyclohexan-1-olhydrochloride (A) have been crystallized, characterized using FT-IR and confirmed by single crystal X-ray diffraction method. In addition, the intercontacts in the crystal structure are analyzed using Hirshfeld surfaces computational method. The A crystallizes in a monoclinic crystal system (space group C2/c) with cell parameters a = 25.1946(14) Å, b = 15.5139(9) Å, c = 8.1636(5) Å, β = 94.664(6)°, V = 3180.3(3) ų and Z = 8. An intermol. interaction of the type O-H… O, N-H… Cl, C-H… Br, C-H… Cg and C-Br… Cg stabilizes the crystal structure. The intercontacts in the crystal structures are visualized using 2D finger print plots. The electrostatic potential surfaces and topol. surfaces (shape index (S) and curvedness (C)) are plotted over the Hirshfeld surfaces to identify the potentials (pos. and neg.) and mol. surface topol., resp. Intercontacts are evaluated for the propensity of forming contacts in the crystal packing by enrichment ration (E) values. The presence of C-Br… Br-C intermol. interactions are confirmed using E values and is categorized as Type I halogen…halogen intermol. interactions.

Chemical Data Collections 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

Pieckowski, Michal published the artcileCombination of large volume sample stacking with polarity switching and cyclodextrin electrokinetic chromatography (LVSS-PS-CDEKC) for the determination of selected preservatives in pharmaceuticals, Recommanded Product: trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, the publication is Talanta (2020), 120673, database is CAplus and MEDLINE.

In this study, a large volume sample stacking (LVSS) with polarity switching (PS) and cyclodextrin electrokinetic chromatog. (CDEKC) method has been developed for the simultaneous separation and determination of 8 preservatives: methylparaben (MP), ethylparaben (EP), propylparaben (PP), butylparaben (BP), isobutylparaben (IBP), sorbic acid (SA), benzoic acid (BA), p-hydroxybenzoic acid (PHBA) in pharmaceuticals. The effects of some typical parameters such as sample volume, applied voltage, composition and pH of the running buffer and organic modifier concentration were examined and optimized. Moreover, the impact of type and concentration of cyclodextrin as electrolyte modifiers was also investigated. The detection limits of analytes for the elaborated LVSS-PS-CDEKC method were found to be in 0.8-5 ng mL^-1 range, which were around 500 times lower than normal CDEKC without preconcentration technique. All analytes were completely resolved in less than 11 min in an uncoated fused-silica capillary of 75μm internal diameter (I.D) x 50 cm length. The electrophoretic separation was performed in a 2 mM α-cyclodextrin and 25 mM tetraborate system (pH = 9.3) with an applied voltage of 25 kV. The established method was validated and confirmed to be applicable for the determination of the preservatives in a quality control of pharmaceuticals.

Talanta 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, Recommanded Product: trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride.

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

Gangireddy, Ramana published the artcileDesign and evaluation of gastroretentive floating matrix tablets of ambroxol hydrochloride, COA of Formula: C13H19Br2ClN2O, the publication is International Journal of Pharmacy and Biological Sciences (2019), 9(2), 1386-1396, database is CAplus.

Gastro retentive drug delivery is a special approach which remains in the gastric region for a prolonged period to increase gastric residence time and also have the advantage of site-specific drug delivery especially in the upper gastrointestinal tract (GIT) for local or systemic effects. Ambroxol hydrochloride is a systemically active mucolytic agent with a half-life of 3-4 h. It acts by breakdown of acid muco polysaccharide fibers which make the sputum thinner and less viscous as long as treatment is maintained and therefore more easily sputum was removed by coughing. The main aim of the present work is to develop the oral controlled release floating matrix tablets of Ambroxol hydrochloride by direct compression method, using various hydrophilic polymers such as HPMCK100M, Carbopol971P, Polyethylene oxide. FT-IR studies revealed that there was no incompatibility between the drug and polymers used. All the formulations remained buoyant without any disintegration. The formulations F4, F9, F15 have shown the extended drug release close to that of marketed formulation for a period of 12 h. To ascertain the mechanism of drug release in-vitro data was fitted into various release kinetic models like zero order, first order, Higuchi and Peppas. The values indicated the non-fickian diffusion with slow erosion of polymer matrix followed by drug diffusion and resulted in linear drug release profile over a prolonged period of time.

International Journal of Pharmacy and Biological 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