Tag: M.W=350-400

Choudhari, Alap A. published the artcileMicroencapsulation of solid dispersions of felodipine and characterization of release mechanism, HPLC of Formula: 72509-76-3, the main research area is felodipine microencapsulation sustained release solid dispersion.

The study was aimed at increase the solubility of poorly soluble drug Felodipine and formulating it in sustained release dosage form. Solid dispersion of drug was prepared using Poly vinyl pyrollidone (PVP) and hydroxyl Pr Me cellulose (HPMC) as inert hydrophilic carriers by kneading method. A 17-fold increase in dissolution rate of Felodipine was observed with solid dispersion prepared with HPMC. Optimized solid dispersion was further characterized by Powder X-ray diffraction (PXRD) which suggest transformation of crystalline Felodipine in amorphous form and Fourier transform IR spectroscopy (FTIR) suggesting no possible interaction. Sustained release microcapsules of Felodipine were formulated using Et cellulose (EC) and Eudragit RL 100 (EDRL) as coating material with solid dispersion of Felodipine as core by emulsion solvent evaporation method. Gelatin was used as microencapsulating agent employing coacervation-phase separation technique. Microcapsules from all the batches were found to discrete, spherical and free flowing and % entrapment efficiency was found to be in range of 88% to 96%. All the batches of microcapsules showed sustained release curve in pH 7.4 phosphate buffer up to eight hours with microcapsules prepared with gelatin giving Felodipine release up to 86% after 8 h. XRD pattern studies of the microcapsules made of gelatin showed drug still present in the amorphous form and thus maintaining its solubility in the microcapsule system.

International Journal of Drug Development & Research published new progress about Amorphous materials. 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, HPLC of Formula: 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jiang, Ling published the artcileApplication of Enzymatic Promiscuity in Pharmaceutical Synthesis: Papain-catalyzed One-pot Synthesis of 1,4-Dihydropyridine Calcium Channel Antagonists and Derivatives, Computed Properties of 72509-76-3, the main research area is aryl aldehyde acetoacetate aminocrotonate papain catalyst three component reaction; phenyl dihydropyridine dicarboxylate preparation green chem.

A new method for the synthesis of 1,4-dihydropyridine(1,4-DHP) calcium channel antagonists felodipine, nitrendipine and their derivatives via papain-catalyzed three-component reactions of aldehyde, Me acetoacetate and Et 3-aminocrotonate was developed. Operational simplicity, mild reaction conditions and eco-friendliness are the key features of this protocol.

Chemical Research in Chinese Universities published new progress about Aryl aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Computed Properties of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Zhengyong published the artcileUltrasonic extraction and nebulization in real-time coupled with carbon fiber ionization mass spectrometry for rapid screening of the synthetic drugs adulterated into herbal products, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is ultrasonic extraction nebulization direct analysis carbon fiber ionization; screening drug adulterated herbal product; Carbon fiber ionization; Direct analysis; Herbal products; Rapid screening; Synthetic drugs; Ultrasonic extraction and nebulization in real-time.

Ultrasonic extraction and nebulization in real-time/carbon fiber ionization mass spectrometry (UEN/CFI-MS) was developed to screen the synthetic drugs adulterated into herbal products such as antidiabetic drug, antihypertensive drug, and hypolipidemic drug. Recently, ambient ionization MS techniques have achieved great advance for rapid anal. of sample surface. However, direct anal. of the analytes inside samples remains a challenge due to a lack of effective online sample extraction procedures. Owing to disappointing desorption efficiency, analytes inside the sample suffer from low detecting sensitivity when applying ambient ionization MS techniques. In this study, online ultrasonic extraction combined with carbon fiber ionization was used for real-time extraction, nebulization and detection of the analytes inside samples. The ultrasonic atomizer could produce a high-frequency vibration to realize online extraction and nebulization of sample. Then, the produced sample droplets could be immediately ionized by the carbon fiber ionization mass spectrometry. UEN/CFI-MS has shown great compatibility to solvents and compounds with a wide range of polarity and has few limitations for the shape of sample. UEN/CFI-MS was successfully applied for the rapid screening of synthetic drugs adulterated into herbal products. Among 37 batches of herbal products, 1 batch of Chinese patent medicine and 6 batches of dietary supplements were detected to be adulterated with the synthetic chems. without labeling.

Analytica Chimica Acta published new progress about Carbon fibers Role: NUU (Other Use, Unclassified), USES (Uses). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Jiang, Ling published the artcileMechanochemical enzymatic synthesis of 1,4-dihydropyridine calcium antagonists and derivatives, Application In Synthesis of 72509-76-3, the main research area is Lipozyme ball milling dihydropyridine calcium antagonists.

BACKGROUND : Enzyme promiscuity has attracted significant attention from chemists and biochemists in recent years. However, long reaction time and use of toxic organic solvents limit its applications for industrial processes. 1,4-Dihydropyridine (1,4-DHP) calcium antagonists are recommended for the first line treatment of hypertension. Although some chem. protocols for the preparation of 1,4-DHP calcium antagonists have been developed, enzymic synthesis of these compounds still remains uncovered. RESULTS : Solvent-free quick synthesis of 1,4-DHP calcium antagonists felodipine, nitrendipine, nifedipine and nemadipine B and their derivatives was achieved by Lipozyme RM IM (triacylglycerol acylhydrolase, EC3.1.1.3)-catalyzed multicomponent reactions of aromatic aldehyde, alkyl acetoacetate and alkyl 3-aminocrotonate under ball-milling conditions. The products were obtained in moderate yields (up to 86.8%) and the influence of reaction conditions including catalyst loading, grinding auxiliary and grinding frequency was investigated. CONCLUSION : The protocol successfully overcame some longstanding problems in the field of enzymic promiscuity research, such as long reaction time and use of harmful organic solvents, and demonstrated the potential application value of promiscuous enzyme-catalyzed reactions under ball-milling conditions for pharmaceutical synthesis. © 2019 Society of Chem. Industry.

Journal of Chemical Technology and Biotechnology published new progress about Pharmaceutical natural products (1,4-Dihydropyridine calcium). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Application In Synthesis of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ormerod, Kiel G. published the artcileRegulation of excitation-contraction coupling at the Drosophila neuromuscular junction, Safety of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is Drosophila neuromuscular junction excitation contraction coupling; drosophila; neuromuscular junction; synapse.

The Drosophila neuromuscular system is widely used to characterize synaptic development and function. However, little is known about how specific synaptic alterations effect neuromuscular transduction and muscle contractility, which ultimately dictate behavioral output. Here we develop and use a force transducer system to characterize excitation-contraction coupling at Drosophila larval neuromuscular junctions (NMJs), examining how specific neuronal and muscle manipulations disrupt muscle contractility. Muscle contraction force increased with motoneuron stimulation frequency and duration, showing considerable plasticity between 5 and 40 Hz and saturating above 50 Hz. Endogenous recordings of fictive contractions revealed average motoneuron burst frequencies of 20-30 Hz, consistent with the system operating within this plastic range of contractility. Temperature was also a key factor in muscle contractility, as force was enhanced at lower temperatures and dramatically reduced with increasing temperatures Pharmacol. and genetic manipulations of critical components of Ca2+ regulation in both pre- and postsynaptic compartments affected the strength and time course of muscle contractions. A screen for modulators of muscle contractility led to identification and characterization of the mol. and cellular pathway by which the FMRFa peptide, TPAEDFMRFa, increases muscle performance. These findings indicate Drosophila NMJs provide a robust system to correlate synaptic dysfunction, regulation and modulation to alterations in excitation-contraction coupling. Key points : Larval muscle contraction force increases with stimulation frequency and duration, revealing substantial plasticity between 5 and 40 Hz. Fictive contraction recordings demonstrate endogenous motoneuron burst frequencies consistent with the neuromuscular system operating within the range of greatest plasticity. Genetic and pharmacol. manipulations of critical components of pre- and postsynaptic Ca2+ regulation significantly affect the strength and time course of muscle contractions. A screen for modulators of the excitation-contraction machinery identified a FMRFa peptide, TPAEDFMRFa and its associated signalling pathway, that dramatically increases muscle performance. Drosophila serves as an excellent model for dissecting components of the excitation-contraction coupling machinery.

Journal of Physiology (Oxford, United Kingdom) published new progress about Actins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Safety of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

S’ari, Mark published the artcileLow dose scanning transmission electron microscopy of organic crystals by scanning moire fringes, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is STEM scanning moire fringes organic crystals; Bright field STEM; Dose-limited resolution; Low dose; Organic crystals; Scanning moiré fringes.

In the pharmaceutical industry, it is important to determine the effects of crystallization and processes, such as milling, on the generation of crystalline defects in formulated products. Conventional transmission electron microscopy and scanning transmission electron microscopy (STEM) can be used to obtain information on length scales unobtainable by other techniques, however, organic crystals are extremely susceptible to electron beam damage. This work demonstrates a bright field (BF) STEM method that can increase the information content per unit specimen damage by the use of scanning moire fringes (SMFs). SMF imaging essentially provides a magnification of the crystal lattice through the interference between closely aligned lattice fringes and a scanning lattice of similar spacing. The generation of SMFs is shown for three different organic crystals with varying electron beam sensitivity, theophylline, furosemide and felodipine. The electron fluence used to acquire the BF-STEM for the most sensitive material, felodipine was approx. 3.5 e-/Å2. After one addnl. scan of felodipine (total fluence of approx. 7.0 e-/Å2), the SMFs were no longer visible due to extensive damage caused to the crystal. Irregularity in the SMFs suggested the presence of defects in all the organic crystals. Further effort is required to improve the data anal. and interpretation of the resulting SMF images, allowing more information regarding the crystal structure and defects to be extracted

Micron published new progress about Crocidolite asbestos Role: ANT (Analyte), ANST (Analytical Study). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Application of 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Itsumi, Momoe published the artcileHigh-throughput screen identifies 5-HT receptor as a modulator of AR and a therapeutic target for prostate cancer, Name: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is antitumor AR modulator 5HT receptor therapeutic target prostate cancer; 5-hydroxytryptamine receptor; androgen receptor; high-throughput screen; prostate cancer; protein kinase A.

Background : Eradication of persistent androgen receptor (AR) activity in castration-resistant prostate cancer may be a promising strategy to overcome castration resistance. We aimed to identify novel compounds that inhibit AR activity and could be potential therapeutic agents for prostate cancer. Methods : A high-throughput screening system involving cell lines stably expressing AR protein and AR-responsive luciferase was employed for the 1260 compound library. Mol. and antitumor effects on candidate pathways that interacted with AR signaling were examined in prostate cancer cells expressing AR. Results : The high-throughput screening identified various potential compounds that interfered with AR signaling through known and novel pathways. Among them, a 5-hydroxytryptamine 5A (5-HT5A) receptor antagonist suppressed AR activity through protein kinase A signaling, which was confirmed by 5-HT5A receptor knockdown. Consistently, 5-HT5A receptor inhibitors showed cytotoxic effects toward prostate cancer cells. Conclusions : Taken together, this study identifies 5-HT5A receptor as a promising therapeutic target for prostate cancer via its interaction with AR signaling.

Prostate (Hoboken, NJ, United States) published new progress about 5-HT receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Name: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Abuhassan, Qamar published the artcileSmall scale in vitro method to determine a bioequivalent equilibrium solubility range for fasted human intestinal fluid, COA of Formula: C18H19Cl2NO4, the main research area is bioequivalent equilibrium solubility human intestinal fluid; Aprepitant; Carvedilol; Fasted simulated intestinal fluid; Felodipine; Fenofibrate; Griseofulvin; Indomethacin; Intestinal solubility; Naproxen; Oral absorption; Phenytoin; Piroxicam; Probucol; Simulated intestinal fluid; Solubility; Tadalafil; Zafirlukast.

Drug solubility is a key parameter controlling oral absorption, but intestinal solubility is difficult to assess in vitro. Human intestinal fluid (HIF) aspirates can be applied but they are variable, difficult to obtain and expensive. Simulated intestinal fluids (SIF) are a useful surrogate but multiple recipes are available and the optimum is unknown. A recent study characterised fasted HIF aspirates using a multi-dimensional approach and determined nine bioequivalent SIF media recipes that represented over ninety percent of HIF compositional variability. In this study these recipes have been applied to determine the equilibrium solubility of twelve drugs (naproxen, indomethacin, phenytoin, piroxicam, aprepitant, carvedilol, zafirlukast, tadalafil, fenofibrate, griseofulvin, felodipine, probucol) previously investigated using a statistical design of experiment (DoE) approach. The bioequivalent solubility measurements are statistically equivalent to the previous DoE, enclose literature solubility values in both fasted HIF and SIF, and the solubility range is less than the previous DoE. These results indicate that the system is measuring the same solubility space as literature systems with the lower overall range suggesting improved equivalence to in vivo solubility, when compared to DoEs. Three drugs (phenytoin, tadalafil and griseofulvin) display a comparatively narrow solubility range, a behavior that is consistent with previous studies and related to the drugs’ mol. structure and properties. This solubility behavior would not be evident with single point solubility measurements. The solubility results can be analyzed using a custom DoE to determine the most statistically significant factor within the media influencing solubility This approach has a lower statistical resolution than a formal DoE and is not appropriate if determination of media factor significance for solubilisation is required. This study demonstrates that it is possible to assess the fasted intestinal equilibrium solubility envelope using a small number of bioequivalent media recipes obtained from a multi-dimensional anal. of fasted HIF. The derivation of the nine bioequivalent SIF media coupled with the lower measured solubility range indicate that the solubility results are more likely to reflect the fasted intestinal solubility envelope than previous DoE studies and highlight that intestinal solubility is a range and not a single value.

European Journal of Pharmaceutics and Biopharmaceutics published new progress about Bile salts Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, COA of Formula: C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Shutao published the artcileFelodipine enhances aminoglycosides efficacy against implant infections caused by methicillin-resistant Staphylococcus aureus, persisters and biofilms, Synthetic Route of 72509-76-3, the main research area is felodipine aminoglycoside methicillin resistant Staphylococcus aureus biofilm; Aminoglycosides; Felodipine; Implant infection; Methicillin-resistant Staphylococcus aureus; Persisters.

Methicillin-resistant Staphylococcus aureus (MRSA), biofilms, and persisters are three major factors leading to recurrent and recalcitrant implant infections. Although antibiotics are still the primary treatment for chronic implant infections in clin., only few drugs are effective in clearing persisters and formed biofilms. Here, felodipine, a dihydropyridine calcium channel blocker, was reported for the first time to have antibacterial effects against MRSA, biofilm, and persisters. Even after continuous exposure to sub-lethal concentrations of felodipine, bacteria are less likely to develop resistance. Besides, low doses of felodipine enhances the antibacterial activity of gentamicin by inhibiting the expression of protein associated with aminoglycoside resistance (aacA-aphD). Next, biofilm eradication test and persisters killing assay suggested felodipine has an excellent bactericidal effect against formed biofilms and persisters. Furthermore, the result of protein profiling, and quant. metabonomics anal. indicated felodipine reduce MRSA virulence (agrABC), biofilm formation and TCA cycle. Then, mol. docking showed felodipine inhibit the growth of persisters by binding to the H pocket of ClpP protease, which could lead to substantial protein degradation Furthermore, murine infection models suggested felodipine in combination with gentamicin alleviate bacterial burden and inflammatory response. In conclusion, low dose of felodipine might be a promising agent for biomaterial delivery to enhance aminoglycosides efficacy against implant infections caused by MRSA, biofilm, and persisters.

Bioactive Materials published new progress about 16S rRNA Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Synthetic Route of 72509-76-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mango, Katalin published the artcileCYP2B6 allelic variants and non-genetic factors influence CYP2B6 enzyme function, Related Products of pyridine-derivatives, the main research area is CYP2B6 allele genotype phenotype amoxicillin clavulanic acid cyclophosphamide.

Human CYP2B6 enzyme although constitutes relatively low proportion (1-4%) of hepatic cytochrome P 450 content, it is the major catalyst of metabolism of several clin. important drugs (efavirenz, cyclophosphamide, bupropion, methadone). High interindividual variability in CYP2B6 function, contributing to impaired drug-response and/or adverse reactions, is partly elucidated by genetic polymorphisms, whereas non-genetic factors can significantly modify the CYP2B6 phenotype. The influence of genetic and phenoconverting non-genetic factors on CYP2B6-selective activity and CYP2B6 expression was investigated in liver tissues from Caucasian subjects (N = 119). Strong association was observed between hepatic S-mephenytoin N-demethylase activity and CYP2B6 mRNA expression (P < 0.0001). In less than one third of the tissue donors, the CYP2B6 phenotype characterized by S-mephenytoin N-demethylase activity and/or CYP2B6 expression was concordant with CYP2B6 genotype, whereas in more than 35% of the subjects, an altered CYP2B6 phenotype was attributed to phenoconverting non-genetic factors (to CYP2B6-specific inhibitors and inducers, non-specific amoxicillin + clavulanic acid treatment and chronic alc. consumption, but not to the gender). Furthermore, CYP2B6 genotype-phenotype mismatch still existed in one third of tissue donors. In conclusion, identifying potential sources of CYP2B6 variability and considering both genetic variations and non-genetic factors is a pressing requirement for appropriate elucidation of CYP2B6 genotype-phenotype mismatch. Scientific Reports published new progress about Alcohols Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 72509-76-3 belongs to class pyridine-derivatives, name is 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C18H19Cl2NO4, Related Products of pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem