Month: December 2022

Dey, Nilanjan published the artcileHeparin triggered dose dependent multi-color emission switching in water: a convenient protocol for heparinase I estimation in real-life biological fluids, Category: pyridine-derivatives, the main research area is heparin heparinase I fluorescence probe color change.

Oligo(p-phenylenevinylene) based bis-pyridinium derivatives show ‘ratiometric’ detection of heparin in water. For the first time, we present a dose-dependent, multi-color emission switching in the presence of heparin. The reversible self-assembly of probes with heparin as the stimulus is also exploited for the screening of heparinase I enzyme.

Chemical Communications (Cambridge, United Kingdom) published new progress about Blood analysis. 36437-30-6 belongs to class pyridine-derivatives, name is 1,1-Di-n-octyl-4,4-bipyridinium Dibromide, and the molecular formula is C26H42Br2N2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Chen, Liuxi published the artcileEvaluation of polysaccharide-based chiral stationary phases in modern SFC-MS/MS for enantioselective bioanalysis., Product Details of C18H19Cl2NO4, the main research area is polysaccharide chiral stationary phase supercritical fluid chromatog mass spectrometry; supercritical fluid chromatog tandem mass spectrometry polysaccharide; SFC–MS/MS; chiral bioanalysis; chiral stationary phase; enantiomer; enantioselective bioanalysis; supercritical fluid chromatography.

Aim: The applicability of polysaccharide-based chiral stationary phases in modern supercritical fluid chromatog. (SFC)-MS/MS for chiral bioanal. was evaluated. Materials & methods: Ten popular polysaccharide-based chiral stationary phases (CSPs) were tested using a set of 23 drugs against three cosolvents. The effect of temperature and backpressure on separation was examined Results: The recommended order of CSPs for screening was determined Methanol with 0.1% NH4OH is proven to be the first choice of cosolvent. Temperature of 40°C and backpressure of 10 or 15 MPa are recommended starting conditions. Phospholipid elution profiles on the polysaccharide-based CSPs were reported for the first time under SFC conditions. Conclusion: A simplified screening protocol with straightforward method optimization approaches was generated for SFC chiral assay development in a reasonable time frame with a high success rate.

Bioanalysis published new progress about Blood analysis. 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, Product Details of C18H19Cl2NO4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Guillemoto, Q. published the artcileTransfer of trace organic compounds in an operational soil-aquifer treatment system assessed through an intrinsic tracer test and transport modelling, Related Products of pyridine-derivatives, the main research area is trace organic compound transport modeling soil aquifer treatment system; Degradation; Reactive transport model; Soil-aquifer treatment; Sorption; Trace Organic Compounds.

Soil Aquifer Treatment (SAT) can provide supplementary treatment of trace organic compounds (TrOCs) such as pharmaceutical and industrial compounds present in Secondary Treated Wastewater (STWW). Concern on presence of unregulated TrOCs in natural systems has raised recently as well as the interest in SAT systems for remediation. The present study quantifies, at the field scale over35 m of lateral groundwater flow, the effectiveness of the Agon-Coutainville SAT system (Manche, Normandy, France) for TrOCs removal by sorption and biodegradation through monitoring of seven TrOCs (oxazepam, carbamazepine, benzotriazole, tolyltriazole, caffeine, paracetamol, ibuprofen) and major inorganic compounds as intrinsic tracers in STWW and groundwater during a 34-day STWW infiltration experiment during operational use of the SAT. Cationic exchanges and mixing between groundwater and STWW during the experiment were highlighted by major ions and geochem. simulations. Due to the low thickness of the unsaturated zone, a 1D anal. solution of the advection-dispersion equation (ADE) was applied on chloride data. Chloride was used as conservative intrinsic tracer to calibrate the horizontal flow and transport parameters such as the aquifer dispersion coefficient (D) and the average pore water velocity (ν) allowing estimation of the groundwater residence time. Transport and attenuation of the TrOCs were simulated assuming first-order degradation constant (μ) and linear retardation coefficient (R), calibrated to simulate the observed temporal changes in the breakthrough of TrOCs. Sorption was found to play a role in the transport of TrOCs, notably for oxazepam with a higher linear retardation coefficient value of 2.2, whereas no significant differences of retardation were observed for carbamazepine, tolyltriazole, benzotriazole (1.37, 1.35, 1.36 resp.). Estimated first order degradation rate constants, between 0.03d-1 for carbamazepine and 0.09d-1 for tolyltriazole, were generally high compared to the literature, possibly due to favorable redox conditions and important microbial activities within the system. This study provides evidence of the efficiency of the Agon-Coutainville SAT system for the removal of TrOCs.

Science of the Total Environment published new progress about Biodegradation. 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

Tu, Xijuan published the artcileMiniaturized salting-out assisted liquid-liquid extraction combined with disposable pipette extraction for fast sample preparation of neonicotinoid pesticides in bee pollen, SDS of cas: 21190-89-6, the main research area is neonicotinoid pesticide bee pollen pipet salting out liquid extraction; HPLC; bee pollen; disposable pipette extraction; neonicotinoid pesticides; salting-out assisted liquid-liquid extraction; sample preparation.

As the main source of nutrients for the important pollinator honeybee, bee pollen is crucial for the health of the honeybee and the agro-ecosystem. In the present study, a new sample preparation procedure has been developed for the determination of neonicotinoid pesticides in bee pollen. The neonicotinoid pesticides were extracted using miniaturized salting-out assisted liquid-liquid extraction (mini-SALLE), followed by disposable pipet extraction (DPX) for the clean-up of analytes. Effects of DPX parameters on the clean-up performance were systematically investigated, including sorbent types (PSA, C18, and silica gel), mass of sorbent, loading modes, and elution conditions. In addition, the clean-up effect of classical dispersive solid-phase extraction (d-SPE) was compared with that of the DPX method. Results indicated that PSA-based DPX showed excellent clean-up ability for the high performance liquid chromatog. (HPLC) anal. of neonicotinoid pesticides in bee pollen. The proposed DPX method was fully validated and demonstrated to provide the advantage of simple and rapid clean-up with low consumption of solvent. This is the first report of DPX method applied in bee pollen matrix, and would be valuable for the development of a fast sample preparation method for this challenging and important matrix.

Molecules published new progress about Apis mellifera. 21190-89-6 belongs to class pyridine-derivatives, name is Ethyl 6-chloropicolinate, and the molecular formula is C8H8ClNO2, SDS of cas: 21190-89-6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Yan, Hongling published the artcileA comprehensive investigation on the chemical diversity and efficacy of different parts of Ligusticum chuanxiong, Formula: C17H18N2O6, the main research area is analysis phthalide fibrous root stem leaf Ligusticum.

Ligusticum chuanxiong Hort.(CX) is a medicinal and edible plant with a wide range of constituents of biol. interest. Since the biomass of the non-medicinal parts of CX is huge, discarding them will cause a waste of resources. To expand the medicinal uses of CX, we comprehensively investigated the chem. diversity and efficacy of its different parts (rhizomes, fibrous roots, stems and leaves). 75 compounds in the volatile oil and 243 compounds in the methanol extracts (including 95 phthalides) obtained from CX were characterized by GC-MS and UHPLC/Q-Orbitrap MS anal., resp. Of 95 phthalides, 14 potential new compounds and 5 phthalide trimers were identified from CX for the first time. Phthalide monomers were more abundant in rhizomes and fibrous roots, and phthalide dimers or even phthalide trimers mainly in stems and leaves. By multivariate and univariate analyses, 22 and 24 different compounds were found in the volatile oils and the methanol extracts, resp. In the bioactivity evaluation of different parts, stems and leaves showed the best antioxidant activity, fibrous roots showed the strongest vasodilator activity, and rhizomes showed the most significant anticoagulant activity, which was related to the different metabolites in different parts. Ultimately, this work revealed the similarities and differences of phytochems. and bioactivities in different anatomical parts of CX. It might provide helpful evidence for the rational application of non-medicinal resources.

Food & Function published new progress about Anticoagulants. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Formula: C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Levin, Gabriel published the artcileNifedipine versus ritodrine during external cephalic version procedure: a case control study, Product Details of C17H18N2O6, the main research area is nifedipine ritodrine external cephalic version procedure; Amniotic fluid index; breech; external cephalic version; nifedipine; ritodrine.

Published series regarding interventions for facilitating external cephalic version (ECV) have concluded that parenterally administered beta-stimulant tocolytics, increased ECV success rate and reduced the number of cesarean sections. However, there were insufficient data regarding calcium channel blockers to provide good evidence regarding its efficacy. Given the paucity of literature, we aimed to compare the efficacy of nifedipine to that of ritodrine on ECV success rates. This is a retrospective case control study of prospectively collected data of patients who underwent ECV between Jan. 2012 and Dec. 2013 at Bikur Cholim Medical Center and Hadassah-Hebrew University Medical Center in Jerusalem, Israel. Patient undergoing ECV with tocolysis by ritodrine were compared with those using nifedipine as tocolysis. Patients were matched in a one-to-one ration by parity and placental location. Overall, 148 women received ritodrine and 148 women received nifedipine before ECV procedure. Overall success rate was higher among the ritodrine group (82.4 vs. 63.5%, p> .001). Among nulliparous and among parous, success rate was higher in the ritodrine group (78.9 vs. 57.9 and 88.6 vs. 73.5%, p = .001, p = .04, resp.). Vaginal delivery rate was higher among the ritodrine group (86.5 vs 68.9%, p >.001). Cesarean delivery rate was 31.1% for the nifedipine group vs. 13.5% in the ritodrine group (p > .001). Number needed to treat to benefit (NNTb) 5.7 (95% confidence interval 3.7-12.1). Overall, 216 of 296 (72.9%) of ECV were successful. Ritodrine was associated with higher success rates as compared with nifedipine (56.5 vs. 32.5%, p > .001). In a multivariate anal., ritodrine tocolytic therapy was independently associated higher ECV success rates as compared to nifedipine (OR 4.54, 95% CI 2.38-9.09). Higher amniotic fluid index (OR 1.16, 95% CI 1.05-1.28) and nulliparity (OR 0.16, 95% CI 0.08-0.30) were addnl. independent predictors of ECV outcome. Ritodrine significantly improve the success of ECV compared with nifedipine. Both drugs are shown to be safe.

Journal of Maternal-Fetal & Neonatal Medicine published new progress about Amniotic fluid. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, Product Details of C17H18N2O6.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hargrave, Karl D. published the artcileNovel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones, Product Details of C6H7ClN2, the main research area is pyridobenzodiazepinone HIV1 reverse transcriptase inhibition; dipyridodiazepinone HIV1 reverse transcriptase inhibition; AIDS inhibitor pyridobenzodiazepinone dipyridodiazepinone.

Novel pyrido[2,3-b][1,4]benzodiazepinones, pyrido[2,3-b][1,5]benzodiazepinones, and dipyrido[3,2-b:2′,3′-e][1,4]diazepinones e.g., I (X = N, X1 = CH; X = CH; X1 = N) and II inhibited human immunodeficiency virus type 1 reverse transcriptase in vitro at concentrations as low as 35 nM. In all three series, small substituents (e.g., Me, Et, Ac) are preferred at the lactam nitrogen, whereas slightly larger alkyl moieties (e.g., Et, cyclopropyl) are favored at the other (N-11) diazepinone nitrogen. In general, lipophilic substituents are preferred on the A ring, whereas substitution on the C ring generally reduces potency relative to the corresponding compounds with no substituents on the aromatic ring. Maximum potency is achieved with Me substitution at the position ortho to the lactam nitrogen atom; however, in this case an unsubstituted lactam nitrogen is preferred. Addnl. substituents on the A ring can be readily tolerated. II (BI-RG-587) is a potent (IC50 = 84 nM) and selective non-nucleoside inhibitor of HIV-1 reverse transcriptase, and has been chosen for preclin. development. II is noncytotoxic except at high doses and effective against all clin. isolates of HIV-1, including those which are AZT-resistant. It is specific for HIV-1, ineffective against HIV-2, inactive against simian and feline reverse transcriptase, and does not inhibit DNA polymerases.

Journal of Medicinal Chemistry published new progress about AIDS (disease). 133627-45-9 belongs to class pyridine-derivatives, name is 2-Chloro-4-methylpyridin-3-amine, and the molecular formula is C6H7ClN2, Product Details of C6H7ClN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Pagano, Nicholas published the artcileAn integrated chemical biology approach reveals the mechanism of action of HIV replication inhibitors, Computed Properties of 71255-09-9, the main research area is dihydropyrimidinone derivative preparation antiviral HIV replication reverse transcriptase inhibitor; Dihydropyrimidinone; Flow chemistry; HIV; Microreactors; Multistep synthesis; NNRTI; Resistant virus activity.

Continuous flow (microfluidic) chem. was employed to prepare a small focused library of dihydropyrimidinone (DHPM) derivatives Compounds in this class have been reported to exhibit activity against the human immunodeficiency virus (HIV), but their mol. target had not been identified. The authors tested the initial set of DHPMs in phenotypic assays providing a hit (4-(2-(4-(3-hydroxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidin-5-yl)thiazol-4-yl)benzonitrile (1i)) that inhibited the replication of the human immunodeficiency virus HIV in cells. Flow chem.-driven optimization of 1i led to the identification of HIV replication inhibitors such as (4-(2-(4-(4-hydroxyphenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidin-5-yl)thiazol-4-yl)benzonitrile (1l)) with cellular potency comparable with the clin. drug nevirapine (NVP). Mechanism of action (MOA) studies using cellular and biochem. assays coupled with 3D fingerprinting and in silico modeling demonstrated that these drug-like probe compounds exert their effects by inhibiting the viral reverse transcriptase polymerase (RT). This led to the design and synthesis of the novel DHPM (3-methyl-4-(2-(6-methyl-4-(1-methyl-1H-indol-2-yl)-2-oxo-1,2,3,4-tetrahydropyrimidin-5-yl)thiazol-4-yl)benzonitrile (1at)) that inhibits the replication of drug resistant strains of HIV. The authors’ work demonstrates that combining flow chem.-driven analog refinement with phenotypic assays, in silico modeling and MOA studies is a highly effective strategy for hit-to-lead optimization applicable to the discovery of future therapeutic agents.

Bioorganic & Medicinal Chemistry published new progress about AIDS (disease). 71255-09-9 belongs to class pyridine-derivatives, name is 2-Methoxynicotinaldehyde, and the molecular formula is C7H7NO2, Computed Properties of 71255-09-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Singh, Bharpoor published the artcileMouth dissolving tablets: an innovative deviation in drug delivery system, Recommanded Product: 3-Ethyl 5-methyl 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, the main research area is mouth dissolving tablet drug delivery system mental disability.

The main aim of novel drug delivery system is to develop a dosage form which is easy to administer, free from side effects, exhibit immediate release and offer enhanced bioavailability for better patient compliance. To achieve such results oral drug delivery system, preferably, tablets are the most widely accepted dosage forms which offer numerous advantages. Beside those advantages, Dysphagia is the most common disadvantage of conventional tablets which is associated with number of conditions like sudden exposure of allergies, mental disability, motion sickness, unconsciousness, unavailability of water etc. To get rid from these problems several innovative drug delivery systems have been developed like Mouth Dissolving Tablets (MDT′s) which dissolve in saliva within a few seconds, when put on tongue. These tablets can be administered anywhere and anytime, without the need of water and are thus quite suitable for children, elderly and mentally disabled patients.

Journal of Pharmaceutical Sciences and Research published new progress about AIDS (disease). 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

Restini, Carolina Baraldi A. published the artcileVascular reactivity stimulated by TMA and TMAO: Are perivascular adipose tissue and endothelium involved?, SDS of cas: 21829-25-4, the main research area is TMA TMAO perivascular adipose tissue endothelium; Aorta; Flavin-monooxygenase 3 (FMO3); Perivascular adipose tissue (PVAT); Trimethylamine (TMA); Trimethylamine N-oxide (TMAO); Vascular endothelium.

Trimethylamine (TMA), formed by intestinal microbiota, and its Flavin-Monooxygenase 3 (FMO3) product Trimethylamine-N-Oxide (TMAO), are potential modulators of host cardiometabolic phenotypes. High circulating levels of TMAO are associated with increased risk for cardiovascular diseases. We hypothesized that TMA/TMAO could directly change the vascular tone. Perivascular adipose tissue (PVAT) helps to regulate vascular homeostasis and may also possess FMO3. Thoracic aorta with(+) or without(-) PVAT, also + or – the endothelium (E), of male Sprague Dawley rats were isolated for measurement of isometric tone in response to TMA/TMAO (1nM-0.5 M). Immunohistochem. (IHC) studies were done to identify the presence of FMO3. TMA and TMAO elicited concentration-dependent arterial contraction. However, at a maximally achievable concentration (0.2 M), contraction stimulated by TMA was of a greater magnitude (141.5 ± 16% of maximum phenylephrine contraction) than that elicited by TMAO (19.1 ± 4.03%) with PVAT and endothelium intact. When PVAT was preserved, TMAO-induced contraction was extensively reduced the presence (19.1 ± 4.03%) vs. absence of E (147.2 ± 20.5%), indicating that the endothelium plays a protective role against TMAO-induced contraction. FMO3 enzyme was present in aortic PVAT, but the FMO3 inhibitor methimazole did not affect contraction stimulated by TMA in aorta + PVAT. However, the L-type calcium channel blocker nifedipine reduced TMA-induced contraction by ∼50% compared to the vehicle. Though a high concentration of these compounds was needed to achieve contraction, the findings that TMA-induced contraction was independent of PVAT and E and mediated by nifedipine-sensitive calcium channels suggest metabolite-induced contraction may be physiol. important.

Pharmacological Research published new progress about Adipose tissue. 21829-25-4 belongs to class pyridine-derivatives, name is Dimethyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate, and the molecular formula is C17H18N2O6, SDS of cas: 21829-25-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem