Tag: M.W=400-450

Gyulai, Orsolya published the artcileOn-line observation of the crystal growth in the case of the non-typical spherical crystallization methods of ambroxol hydrochloride, Safety of trans-4-((2-Amino-3,5-dibromobenzyl)amino)cyclohexanol hydrochloride, the publication is Powder Technology (2018), 144-149, database is CAplus.

Spherical crystallization can be an important technol. step in the production of a solid form active agent. By the production of spherical crystals, direct compression tablet making can be applied to the powder material. This method makes the tableting process quicker, shorter and more economical with reduced amounts of additives and a reduced number of technol. steps. This way, the granulation method can be avoided, which is also advantageous for a moisture sensitive drug. In this paper, we presented Focused Beam Reflectance Measurement (FBRM) studies applied in the case of the non-typical spherical crystallization methods of the active pharmaceutical ingredient ambroxol hydrochloride. Spherical agglomeration and controlled cooling crystallization methods were carried out based on our previous studies regarding these methods and the crystal formation processes were investigated with FBRM probe. Critical agglomeration periods and other mechanisms, such as the breakage of the agglomerates and the precipitation of small particles, were investigated. Chord length values were observed continuously and samples were taken out in certain points of the crystallization Particle size anal. was carried out in each case to obtain information on the particle size enlargement caused by the crystallization methods. With the application of light microscopic anal., aspect ratio and roundness values were also determined to obtain pieces of information on the sphericity-changes of the particles throughout the crystallization and large improvements were presented either for these parameters (aspect ratio from ∼ 1.7 to ∼ 1.3; roundness from ∼ 2.4 to ∼ 1.5) and the mean particle size (from ∼13μm to 120-400μm). Among others, it was revealed that after the spherical agglomeration method (SA), mostly crystal agglomerates were formed, while slow cooling crystallization with alternating temperature profile (ATP) yielded larger and probably harder individual crystals.

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

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

Zhebentyaev, A. I. published the artcileIon-pair thin-layer chromatography of drugs which are quaternary ammonium compound derivatives, Name: N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate, the publication is Farmatsiya (Moscow) (1998), 47(1), 21-22, 27, database is CAplus.

The influence of mobile phase composition on chromatog. development of 12 drugs which are quaternary ammonium compound derivatives (QAD) was studied. Chromatog. development optimal conditions of some QAD using organic solvent and aqueous counter-ion solution mixture were established. Distribution coefficients of investigated GAD in system with different counter-ions was calculated

Farmatsiya (Moscow) 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 C5H6BNO2, Name: N-Benzyl-N,N-dimethyl-2-phenoxyethanaminium 3-hydroxy-2-naphthoate.

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

Pouchain, Laurent published the artcileQuaterthiophenes with Terminal Indeno[1,2-b]thiophene Units as p-Type Organic Semiconductors, Synthetic Route of 239075-02-6, the publication is Journal of Organic Chemistry (2009), 74(3), 1054-1064, database is CAplus and MEDLINE.

Quaterthiophenes 4T, Oct-4T, and Tol-4T based on a central 2,2′-bithiophene core α,ω-terminated with 4,4-unsubstituted and 4,4-disubstituted n-octyl or p-tolyl indeno[1,2-b]thiophene were synthesized by Stille or Miyaura-Suzuki couplings. Compound 4T was also synthesized by an alternative route involving a soluble precursor bearing solubilizing trimethylsilyl groups which were eliminated in the last step. The electronic properties of the compounds were analyzed by cyclic voltammetry, UV-visible absorption and fluorescence emission spectroscopy. Thermal evaporation of 4T and Oct-4T leads to crystalline thin films and UV-visible absorption and x-ray diffraction data for these films suggest that the mols. adopt a quasi-vertical orientation onto the substrate. Strong π-π intermol. interactions were observed for 4T but not for mols. Oct-4T due to the presence of n-octyl chains. Sublimed thin films of Tol-4T show an amorphous character. The characterization of field-effect transistors fabricated from these three materials gave a hole-mobility of 2.2 × 10^-2 cm² V^-1 s^-1 with an on/off ratio of 2.2 × 10⁴ for 4T while no field-effect was observed for Oct-4T and Tol-4T.

Journal of Organic Chemistry 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, Synthetic Route of 239075-02-6.

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

Md, Shadab published the artcileAmbroxol Hydrochloride Loaded Gastro-Retentive Nanosuspension Gels Potentiate Anticancer Activity in Lung Cancer (A549) Cells, Synthetic Route of 23828-92-4, the publication is Gels (2021), 7(4), 243, database is CAplus and MEDLINE.

This study aimed to develop gastro-retentive sustained-release ambroxol (ABX) nanosuspensions utilizing ambroxol-kappa-carrageenan (ABX-CRGK) complexation formulations. The complex was characterized by differential scanning calorimetry, powder x-ray diffractometer, and SEM. The prepared co-precipitate complex was used for the development of the sustained-release formulation to overcome the high metabolic and poor solubility problems associated with ABX. Furthermore, the co-precipitate complex was formulated as a suspension in an aqueous floating gel-forming vehicle of sodium alginate with chitosan, which might be beneficial for targeting the stomach as a good absorption site for ABX. The suspension exhibited rapid floating gel behavior for more than 8 h, thus confirming the gastro-retentive effects. Particle size anal. revealed that the optimum nanosuspension (ABX-NS) had a mean particle size of 332.3 nm. Afterward, the ABX released by the nanoparticles would be distributed to the pulmonary tissue as previously described. Based on extensive pulmonary distribution, the developed nanosuspension-released ABX nanoparticles showed significant cytotoxic enhancement compared to free ABX in A549 lung cancer cells. However, a significant loss of mitochondrial membrane potential (MMP) also occurred. The level of caspase-3 was the highest in the ABX-NS-released particle-treated samples, with a value of 416.6 ± 9.11 pg/mL. Meanwhile, the levels of nuclear factor kappa beta, interleukins 6 and 1 beta, and tumor necrosis alpha (NF-kB, IL-6, IL-1β, and TNF-α, resp.) were lower for ABX-NS compared to free ABX (p < 0.05). In caspase-3, Bax, and p53, levels significantly increased in the presence of ABX-NS compared to free ABX. Overall, ABX-NS produced an enhancement of the anticancer effects of ABX on the A549 cells, and the developed sustained-release gel was successful in providing a gastro-retentive effect.

Gels 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, Synthetic Route of 23828-92-4.

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

Klingstedt, Therese published the artcileSynthesis of a library of oligothiophenes and their utilization as fluorescent ligands for spectral assignment of protein aggregates, Category: alcohols-buliding-blocks, the publication is Organic & Biomolecular Chemistry (2011), 9(24), 8356-8370, database is CAplus and MEDLINE.

Mol. probes for selective identification of protein aggregates are important to advance the understanding of the mol. pathogenesis underlying protein aggregation diseases. Here the authors report the chem. design of a library of anionic luminescent conjugated oligothiophenes (LCOs), which can be utilized as ligands for detection of protein aggregates. Certain mol. requirements were shown to be necessary for detecting (i) early nonthioflavinophilic protein assemblies of Aβ1-42 and insulin preceding the formation of amyloid fibrils and (ii) for obtaining distinct spectral signatures of the two main pathol. hallmarks observed in human Alzheimer’s disease brain tissue (Aβ plaques and neurofibrillary tangles). The authors’ findings suggest that a superior anionic LCO-based ligand should have a backbone consisting of five to seven thiophene units and carboxyl groups extending the conjugated thiophene backbone. Such LCOs will be highly useful for studying the underlying mol. events of protein aggregation diseases and could also be utilized for the development of novel diagnostic tools for these diseases.

Organic & Biomolecular Chemistry 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

Abdelaleem, Eglal A. published the artcileAn Innovative Method, Interference Subtraction, for Determination of Drugs in Syrups in Presence of Potential Interfering Excipients, Product Details of C13H19Br2ClN2O, the publication is Analytical Chemistry Letters (2018), 8(6), 782-793, database is CAplus.

Pharmaceutical dosage forms contain both active ingredients and inactive materials called exipients, most of which cause high interference specially in direct UV-spectrophotometry. This problem is highly obvious in syrups which may contain preservatives, coloring agents, thickening agents and sweetening agents. Thus, there is an urgent need to develop and validate a simple, accurate and selective method named interference subtraction method for determination of drugs in syrups in presence of these excipients without pre-separation by solving this interference. This newly designed method was successfully applied to; Oxybutynin hydrochloride in Detronin syrup, Ambroxol hydrochloride in Muco syrup and Ibuprofen in both Brufen syrup and Megafen N oral suspension. These chosen syrups contain different excipients causing different types of interference. This innovative method was validated according to ICH guidelines. The results obtained by interference subtraction method were statistically compared with those obtained by the official and /or reported methods of the proposed drugs.

Analytical Chemistry Letters 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, Product Details of C13H19Br2ClN2O.

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