Day: October 21, 2022

Mei, Tian-Sheng; Patel, Harshkumar H.; Sigman, Matthew S. published the artcile< Enantioselective construction of remote quaternary stereocentres>, Name: (R)-4-(tert-Butyl)-2-(5-(trifluoromethyl)pyridin-2-yl)-4,5-dihydrooxazole, the main research area is trisubstituted alkenyl alc arylboronic acid palladium relay Heck arylation; aryl carbonyl compound quaternary carbon substituted stereoselective preparation.

Small mols. that contain all-carbon quaternary stereocenters-carbon atoms bonded to four distinct carbon substituents-are found in many secondary metabolites and some pharmaceutical agents. The construction of such compounds in an enantioselective fashion remains a long-standing challenge to synthetic organic chemists. In particular, methods for synthesizing quaternary stereocenters that are remote from other functional groups are underdeveloped. Here we report a catalytic and enantioselective intermol. Heck-type reaction of trisubstituted-alkenyl alcs. with aryl boronic acids. This method provides direct access to quaternary all-carbon-substituted β-, γ-, δ-, ε- or ζ-aryl carbonyl compounds, because the unsaturation of the alkene is relayed to the alc., resulting in the formation of a carbonyl group. The scope of the process also includes incorporation of pre-existing stereocenters along the alkyl chain, which links the alkene and the alc., in which the stereocenter is preserved. The method described allows access to diverse mol. building blocks containing an enantiomerically enriched quaternary center.

Nature (London, United Kingdom) published new progress about Alkenyl alcohols Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 1428537-19-2 belongs to class pyridine-derivatives, and the molecular formula is C13H15F3N2O, Name: (R)-4-(tert-Butyl)-2-(5-(trifluoromethyl)pyridin-2-yl)-4,5-dihydrooxazole.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Acharjee, Animesh; Rakshit, Atanu; Chowdhury, Suman; Datta, Indukamal; Barman, Milan Krishna; Ali, Ansar Md.; Saha, Bidyut published the artcile< Micellar catalysed oxidation of hydrophobic fatty alcohol in aqueous medium>, Synthetic Route of 123-03-5, the main research area is octanol micellar catalyst oxidation mechanism kinetics.

Oxidation of a hydrophobic fatty alc. was carried out under pseudo 1st order reaction condition in aqueous micellar medium efficiently. In addition to the dissolution of alc. micelles are found to catalyze the oxidation reaction. Use of promoters further enhanced the rate of the reaction with almost instant completion of the reaction via the formation of active oxidants (AO+). The product was confirmed by IR and NMR study. Fluorescence studies and DLS measurements were done to confirm the formation of AO+. NMR studies were carried out to establish the interaction between the surfactants and 1-Octanol. Calculated activation parameters (ΔH≠, ΔS≠) also support the exptl. findings.

Journal of Molecular Liquids published new progress about Activation enthalpy. 123-03-5 belongs to class pyridine-derivatives, and the molecular formula is C21H38ClN, Synthetic Route of 123-03-5.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Heusler, Arne; Fliege, Julian; Wagener, Tobias; Glorius, Frank published the artcile< Substituted Dihydropyridine Synthesis by Dearomatization of Pyridines>, Synthetic Route of 329214-79-1, the main research area is dihydropyridine preparation regioselective; pyridine triflic anhydride dearomatization trimethylamine borane; phenyl chloroformate pyridine dearomatization trimethylamine borane; boranes; chemoselectivity; nitrogen heterocycles; reduction; synthetic methods.

The synthesis of a broad variety of N-substituted 1,4-dihydropyridines I [R = H, 3-Me, 3,5-di-Br, etc.; R1 = Tf, CO2Ph] and 1,2-dihydropyridines II [R2 = F, Cl, CF3, Ph, SPh; R3 = H, F, trimethylsilyl] by very mild and selective reduction with amine borane was reported for the first time.

Angewandte Chemie, International Edition published new progress about Dearomatization. 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Synthetic Route of 329214-79-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Palasek, B.; Puszko, A.; Biedrzycka, Z.; Sicinska, W.; Witanowski, M. published the artcile< Nitrogen NMR shieldings of 2-amino-5-nitro-6-methylpyridines>, Application In Synthesis of 22280-62-2, the main research area is aminonitromethylpyridine NMR shielding.

Nitrogen NMR shieldings (chem. shifts) of 2-amino-5-nitro-6-methylpyridine derivatives are assessed from the point of view of substituent-induced effects under conditions where alkyl, aryl, nitro, and nitroso moieties are substituents at the amino nitrogen. The nitro nitrogen shielding reveals only little variation upon varying the substituents, and this seems to indicate that steric hindrance which is likely to force the nitro group out of the plane of the aromatic ring reduces the π-electron conjugation with the latter, and with the amino group as well. On the other side, the pyridine nitrogen shielding shows large effects of substituents at the amino moiety, which suggests a significant conjugation between the ring and the amino group. The latter effects produce a remarkable deshielding of the pyridine nitrogen in the case of nitro and nitroso substituents at the amino group.

Spectroscopy (Amsterdam) published new progress about NMR (nuclear magnetic resonance). 22280-62-2 belongs to class pyridine-derivatives, and the molecular formula is C6H7N3O2, Application In Synthesis of 22280-62-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zheng, Ke; Iqbal, Sarah; Hernandez, Pamela; Park, HaJeung; LoGrasso, Philip V.; Feng, Yangbo published the artcile< Design and Synthesis of Highly Potent and Isoform Selective JNK3 Inhibitors: SAR Studies on Aminopyrazole Derivatives>, Electric Literature of 56622-54-9, the main research area is aminopyrazole JNK3 enzyme inhibitor preparation structure neurodegeneration.

The c-jun N-terminal kinase 3 (JNK3) is expressed primarily in the brain. Numerous reports have shown that inhibition of JNK3 is a promising strategy for treatment of neurodegeneration. The optimization of aminopyrazole-based JNK3 inhibitors with improved potency, isoform selectivity, and pharmacol. properties by structure-activity relationship (SAR) studies utilizing biochem. and cell-based assays, and structure-based drug design is reported. These inhibitors had high selectivity over JNK1 and p38α, minimal cytotoxicity, potent inhibition of 6-OHDA-induced mitochondrial membrane potential dissipation and ROS generation, and good drug metabolism and pharmacokinetic (DMPK) properties for iv dosing. 26n was profiled against 464 kinases and was found to be highly selective hitting only seven kinases with >80% inhibition at 10 μM. Moreover, 26n showed good solubility, good brain penetration, and good DMPK properties. Finally, the crystal structure of 26k in complex with JNK3 was solved at 1.8 Å to explore the binding mode of aminopyrazole based JNK3 inhibitors.

Journal of Medicinal Chemistry published new progress about Drug metabolism. 56622-54-9 belongs to class pyridine-derivatives, and the molecular formula is C7H10N2, Electric Literature of 56622-54-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Fang, Lei; Zhao, Zitong; Wang, Jue; Xiao, Ping; Sun, Xiangshi; Ding, Yaping; Zhang, Pengcheng; Wang, Dangge; Li, Yaping published the artcile< Light-controllable charge-reversal nanoparticles with polyinosinic-polycytidylic acid for enhancing immunotherapy of triple negative breast cancer>, SDS of cas: 2127-03-9, the main research area is charge reversal nanoparticle polyinosinic polycytidylic acid delivery cancer immunotherapy; Cancer immunotherapy; Charge-reversal; Nanoparticles; Photodynamic therapy; Polyinosinic-polycytidylic acid; ROS-responsive; Triple negative breast cancer; Tumor microenvironment.

Nucleic acid drugs are highly applicable for cancer immunotherapy with promising therapeutic effects, while targeting delivery of these drugs to disease lesions remains challenging. Cationic polymeric nanoparticles have paved the way for efficient delivery of nucleic acid drugs, and achieved stimuli-responsive disassembly in tumor microenvironment (TME). However, TME is highly heterogeneous between individuals, and most nanocarriers lack active-control over the release of loaded nucleic acid drugs, which will definitely reduce the therapeutic efficacy. Herein, we have developed a light-controllable charge-reversal nanoparticle (LCCN) with controlled release of polyinosinic-polycytidylic acid [Poly(I:C)] to treat triple neg. breast cancer (TNBC) by enhanced photodynamic immunotherapy. The nanoparticles keep suitably pos. charge for stable loading of Poly(I:C), while rapidly reverse to neg. charge after near-IR light irradiation to release Poly(I:C). LCCN-Poly(I:C) nanoparticles trigger effective phototoxicity and immunogenic cell death on 4T1 tumor cells, elevate antitumor immune responses and inhibit the growth of primary and abscopal 4T1 tumors in mice. The approach provides a promising strategy for controlled release of various nucleic acid-based immune modulators, which may enhance the efficacy of photodynamic immunotherapy against TNBC.

Acta Pharmaceutica Sinica B published new progress about Antitumor agents. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, SDS of cas: 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Fontaine, Fanny; Hequet, Arnaud; Voisin-Chiret, Anne-Sophie; Bouillon, Alexandre; Lesnard, Aurelien; Cresteil, Thierry; Jolivalt, Claude; Rault, Sylvain published the artcile< First identification of boronic species as novel potential inhibitors of the Staphylococcus aureus NorA efflux pump>, Synthetic Route of 832735-54-3, the main research area is boron compound transport protein NorA Staphylococcus.

Overexpression of efflux pumps is an important mechanism of bacterial resistance that results in the extrusion of antimicrobial agents outside the bacterial cell. Inhibition of such pumps appears to be a promising strategy that could restore the potency of existing antibiotics. The NorA efflux pump of Staphylococcus aureus confers resistance to a wide range of unrelated substrates, such as hydrophilic fluoroquinolones, leading to a multidrug-resistance phenotype. Here, 150 heterocyclic boronic species were evaluated for their activity against susceptible and resistant strains of S. aureus. Twenty-four hit compounds, although inactive when tested alone, were found to potentiate ciprofloxacin activity by a 4-fold increase at concentrations ranging from 0.5 to 8 μg/mL against S. aureus 1199B, which overexpresses NorA. Boron-free analogs showed no biol. activity, thus revealing that the boron atom is crucial for biol. activity. This work describes the first reported efflux pump inhibitory activity of boronic acid derivatives

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 832735-54-3 belongs to class pyridine-derivatives, and the molecular formula is C18H22BNO3, Synthetic Route of 832735-54-3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hameed P, Shahul; Patil, Vikas; Solapure, Suresh; Sharma, Umender; Madhavapeddi, Prashanti; Raichurkar, Anandkumar; Chinnapattu, Murugan; Manjrekar, Praveena; Shanbhag, Gajanan; Puttur, Jayashree; Shinde, Vikas; Menasinakai, Sreenivasaiah; Rudrapatana, Suresh; Achar, Vijayashree; Awasthy, Disha; Nandishaiah, Radha; Humnabadkar, Vaishali; Ghosh, Anirban; Narayan, Chandan; Ramya, V. K.; Kaur, Parvinder; Sharma, Sreevalli; Werngren, Jim; Hoffner, Sven; Panduga, Vijender; Kumar, C. N. Naveen; Reddy, Jitendar; Kumar KN, Mahesh; Ganguly, Samit; Bharath, Sowmya; Bheemarao, Ugarkar; Mukherjee, Kakoli; Arora, Uma; Gaonkar, Sheshagiri; Coulson, Michelle; Waterson, David; Sambandamurthy, Vasan K.; de Sousa, Sunita M. published the artcile< Novel N-Linked Aminopiperidine-Based Gyrase Inhibitors with Improved hERG and in Vivo Efficacy against Mycobacterium tuberculosis>, Safety of 5-Fluoropyridine-2,3-diamine, the main research area is aminopiperidinyl quinolone naphthyridone Mycobacterium tuberculosis bactericide DNA gyrase inhibitor.

DNA gyrase is a clin. validated target for developing drugs against Mycobacterium tuberculosis (Mtb). Despite the promise of fluoroquinolones (FQs) as anti-tuberculosis drugs, the prevalence of pre-existing resistance to FQs is likely to restrict their clin. value. We describe a novel class of N-linked aminopiperidinyl alkyl quinolones and naphthyridones that kills Mtb by inhibiting the DNA gyrase activity. The mechanism of inhibition of DNA gyrase was distinct from the fluoroquinolones, as shown by their ability to inhibit the growth of fluoroquinolone-resistant Mtb. Biochem. studies demonstrated this class to exert its action via single-strand cleavage rather than double-strand cleavage, as seen with fluoroquinolones. The compounds are highly bactericidal against extracellular as well as intracellular Mtb. Lead optimization resulted in the identification of potent compounds with improved oral bioavailability and reduced cardiac ion channel liability. Compounds from this series are efficacious in various murine models of tuberculosis (e.g., compound I).

Journal of Medicinal Chemistry published new progress about Antibacterial agents. 212268-13-8 belongs to class pyridine-derivatives, and the molecular formula is C5H6FN3, Safety of 5-Fluoropyridine-2,3-diamine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Buttelmann, Bernd; Alanine, Alexander; Bourson, Anne; Gill, Ramanjit; Heitz, Marie-Paule; Mutel, Vincent; Pinard, Emmanuel; Trube, Gerhard; Wyler, Rene published the artcile< 2-(3,4-Dihydro-1H-isoquinolin-2yl)-pyridines as a novel class of NR1/2B subtype selective NMDA receptor antagonists>, Related Products of 79055-59-7, the main research area is NMDA receptor antagonist structure activity relationship design.

Recently, we disclosed 4-aminoquinolines as structurally novel NR1/2B subtype selective NMDA receptor antagonists. We would now like to report our findings on structurally related pyridine analogs. The SAR developed in this series resulted in the discovery of high affinity antagonists which are selective (vs α1 and M1 receptors) and active in vivo.

Bioorganic & Medicinal Chemistry Letters published new progress about Drug design. 79055-59-7 belongs to class pyridine-derivatives, and the molecular formula is C6H7BrN2, Related Products of 79055-59-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Rui-Qian; Liu, Zhan-Qing; Luo, Yan-Ling; Xu, Feng; Chen, Ya-Shao published the artcile< Tri-stimuli responsive carbon nanotubes covered by mesoporous silica graft copolymer multifunctional materials for intracellular drug delivery>, Application In Synthesis of 2127-03-9, the main research area is carbon silica graft copolymer multifunctional material intracellular drug delivery.

To overcome premature drug leakage and instability in drug delivery systems, we designed tri-stimuli responsive multiwalled carbon nanotubes covered by mesoporous silica graft poly(N-isopropylacrylamide-block-poly(2-(4-formylbenzoyloxy)) Et methacrylate) multifunctional materials via disulfide linkages (MWCNTs@MSN-s-s-g-PNIPAM-b-PFBEMA). The multifunctional materials could covalently bind and phys. load anticancer drug doxorubicin (DOX), and exhibited pH-, temperature- and reductant-induced multi-stimuli responsiveness, significantly enhancing drug loading capacity and improving the release dynamics of drug. The DOX-loaded multifunctional materials exhibited the optimal release behavior in cancer environments compared with in normal cells upon simultaneously triggered by these stimuli. It meant that the MWCNTs@MSN-s-s-g-PNIPAM-b-PFBEMA could serve as efficient gatekeepers to control the mesopore on-off and thus to modulate drug release. The multifunctional materials were proved to be low toxic, whereas the DOX-loaded counterparts had almost the same toxicity as free DOX to cancer cells. Therefore, the developed multifunctional materials can be used as promising drug controlled delivery platforms for cancer therapy.

Journal of Industrial and Engineering Chemistry (Amsterdam, Netherlands) published new progress about Binding energy. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Application In Synthesis of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem