Category: pyridine-derivatives

Parvanak Boroujeni, Kaveh; Shojaei, Pegah published the artcile< Poly(4-vinylpyridine)-supported dual acidic ionic liquid: an environmentally friendly heterogeneous catalyst for the one-pot synthesis of 4,4'-(arylmethylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ols)>, Formula: C9H13NO3S, the main research area is sulfobutylpyridinium sulfate as catalyst Knoevenagel condensation Michael addition.

A poly(4-vinylpyridine)-supported Bronsted ionic liquid was easily prepared from its starting materials and used as a novel, highly efficient, and reusable heterogeneous catalytic system for the synthesis of 4,4′-(arylmethylene)bis(3-methyl-1-phenyl-1H-pyrazol-5-ol derivatives) by a condensation reaction between aromatic aldehydes and 2 equiv of 3-methyl-l-phenyl-5-pyrazolone. The synthesis of the target compound (catalyst) was achieved by a reaction of 1,2-oxathiane 2,2-dioxide (1,4-butanesultone) with 4-Vinylpyridine divinylbenzene copolymer and a subsequent anion exchange. The catalyst thus formed was a polymer-supported 1-(4-sulfobutyl)pyridinium sulfate ionic liquid The reaction products thus formed included 4,4′-(phenylmethylene)bis[3-methyl-1-phenyl-1H-pyrazol-5-ol] derivatives, a furan derivative [4,4′-[(2-furanyl)methylene]bis[3-methyl-1-phenyl-1H-pyrazolo-5-ol]], a thiophene derivative [4,4′-[(2-thienyl)methylene]bis[3-methyl-1-phenyl-1H-pyrazolo-5-ol]].

Turkish Journal of Chemistry published new progress about Addition reaction. 21876-43-7 belongs to class pyridine-derivatives, and the molecular formula is C9H13NO3S, Formula: C9H13NO3S.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hameed P, Shahul; Raichurkar, Anandkumar; Madhavapeddi, Prashanti; Menasinakai, Sreenivasaiah; Sharma, Sreevalli; Kaur, Parvinder; Nandishaiah, Radha; Panduga, Vijender; Reddy, Jitendar; Sambandamurthy, Vasan K.; Sriram, D. published the artcile< Benzimidazoles: Novel Mycobacterial Gyrase Inhibitors from Scaffold Morphing>, Formula: C5H6FN3, the main research area is benzimidazole DNA gyrase inhibitor scaffold morphing Mycobacterium; DNA gyrase; NBTIs; Tuberculosis; aminopiperidines; benzimidazoles; type II topoisomerases.

Type II topoisomerases are well conserved across the bacterial species, and inhibition of DNA gyrase by fluoroquinolones has provided an attractive option for treatment of tuberculosis (TB). However, the emergence of fluoroquinolone-resistant strains of Mycobacterium tuberculosis (Mtb) poses a threat for its sustainability. A scaffold hopping approach using the binding mode of novel bacterial topoisomerase inhibitors (NBTIs) led to the identification of a novel class of benzimidazoles as DNA gyrase inhibitors with potent anti-TB activity. Docking of benzimidazoles to a NBTI bound crystal structure suggested that this class of compound makes key contacts in the enzyme active site similar to the reported NBTIs. This observation was further confirmed through the measurement of DNA gyrase inhibition, and activity against Mtb strains harboring mutations that confer resistance to aminopiperidines based NBTIs and Mtb strains resistant to moxifloxacin. Structure-activity relationship modification at the C-7 position of the left-hand side ring provided further avenue to improve hERG selectivity for this chem. series that has been the major challenges for NBTIs.

ACS Medicinal Chemistry Letters published new progress about DNA gyrases Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (inhibitors). 212268-13-8 belongs to class pyridine-derivatives, and the molecular formula is C5H6FN3, Formula: C5H6FN3.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ran, Wei; Liu, Xiaoyu; Chang, Lu; Cai, Ying; Zheng, Chao; Liu, Jia; Li, Yaping; Zhang, Pengcheng published the artcile< Self-assembling mertansine prodrug improves tolerability and efficacy of chemotherapy against metastatic triple-negative breast cancer>, Quality Control of 2127-03-9, the main research area is self assembling mertansine prodrug nanoparticle drug delivery system; Chemotherapy; Prodrug; Self-assembly; Supramolecular; Triple-negative breast cancer.

Metastatic triple-neg. breast cancer is one of the most devastating cancer types. Systemic chemotherapy is necessary, but its clin. performance is largely limited by severe side effects. Herein, we report a mertansine prodrug, which could self-assemble into spherical nanoparticles in water and readily convert into active mertansine at the presence of glutathione. The self-assembling mertansine prodrugs (SAMPDs) entered cancer cells via a caveolae-mediated pathway and exhibited potent cytotoxicity. The self-delivering SAMPDs did not cause hemolysis, and more importantly increased maximum tolerated dose (MTD) of mertansine by 8 folds via reducing free mertansine exposure in most of the major organs. SAMPDs improved intratumoral drug exposure and showed dose-dependent antitumor activity. When dosed at MTD, SAMPDs inhibited primary tumor growth and pulmonary metastasis by 80% and 95%, while mertansine dosed at MTD only reduced primary tumor growth and metastasis by <50% and 60%, resp. Our results reveal the mechanism of in vivo biotransformation of self-assembling prodrug and highlight the unique advantages of self-assembling prodrug strategy in improving the efficacy and safety of chemotherapy. Journal of Controlled Release published new progress about Antitumor agents. 2127-03-9 belongs to class pyridine-derivatives, and the molecular formula is C10H8N2S2, Quality Control of 2127-03-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Clark, Richard A. F. published the artcile< Oxidative Stress and ""Senescent"" Fibroblasts in Non-Healing Wounds as Potential Therapeutic Targets>, Formula: C7H5BrN2, the main research area is review oxidative stress senescent fibroblast nonhealing wound therapeutic target.

A review. In chronic wounds, fibroblast dysfunctions, such as increased apoptosis, premature senescence, senescence-like phenotype, or poor growth response in the absence of senescence markers, have been reported. Some of these differential dysfunctions may be secondary to differences in patient age or sex, ulcer size or duration, edge vs. base sampling, or culture technique. Nevertheless, the entire spectrum of fibroblast dysfunction may exist and be secondary to, or a response to, different amounts of oxidative stress. Journal of Investigative Dermatol. (2008) 128, 2361-2364. doi:10.1038/jid.2008.257.

Journal of Investigative Dermatology published new progress about Cell aging. 23612-36-4 belongs to class pyridine-derivatives, and the molecular formula is C7H5BrN2, Formula: C7H5BrN2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhao, Li-Xia; Peng, Jian-Feng; Liu, Feng-Yi; Zou, Yue-Li; Gao, Shuang; Fu, Ying; Ye, Fei published the artcile< Design, Synthesis, and Herbicidal Activity of Diphenyl Ether Derivatives Containing a Five-Membered Heterocycle>, Product Details of C6H4F3N, the main research area is herbicide phenoxypyridine heterocycle derivative preparation protoporphyrinogen oxidase inhibitor; PPO; cumulative analysis; diphenyl ether derivatives; field trial; greenhouse herbicidal activity; molecular docking.

Protoporphyrinogen oxidase (PPO, EC 1.3.3.4) is an important target for discovering novel herbicides, and it causes bleaching symptoms by inhibiting the synthesis of chlorophyll and heme. In this study, the active fragments of several com. herbicides were joined by substructure splicing and bioisosterism, and a series of novel di-Ph ether derivatives containing five-membered heterocycles were synthesized. The greenhouse herbicidal activity and the PPO inhibitory activity in vitro were discussed in detail. The results showed that most compounds had good PPO inhibitory activity, and target compounds containing trifluoromethyl groups tended to have higher activity. Among them, compound (I) showed the best inhibitory activity, with a half-maximal inhibitory concentration (IC50) of 0.0468 μmol/L, which was approx. 3 times better than that of oxyfluorfen (IC50 = 0.150 μmol/L). In addition, mol. docking indicated that compound I formed obvious π-π stacking interactions and hydrogen bond interactions with PHE-392 and ARG-98, resp. Remarkably, compound I had good safety for corn, wheat, rice, and soybean, and the cumulative concentration in crops was lower than that of oxyfluorfen. Therefore, compound I can be used to develop potential lead compounds for novel PPO inhibitors.

Journal of Agricultural and Food Chemistry published new progress about Abutilon theophrasti. 3796-23-4 belongs to class pyridine-derivatives, and the molecular formula is C6H4F3N, Product Details of C6H4F3N.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Chun; Santiago, Celine B.; Kou, Lei; Sigman, Matthew S. published the artcile< Alkenyl Carbonyl Derivatives in Enantioselective Redox Relay Heck Reactions: Accessing α,β-Unsaturated Systems>, Quality Control of 1428537-19-2, the main research area is arylboronic acid unsaturated carbonyl enantioselective regioselective arylation Heck; aryl unsaturated carbonyl stereoselective preparation.

A highly enantioselective and site-selective Pd-catalyzed arylation of alkenes linked to carbonyl derivatives to yield α,β-unsaturated systems is reported. The high site selectivity is attributed to both a solvent effect and the polarized nature of the carbonyl group, both of which have been analyzed through multidimensional anal. tools. The reaction can be performed in an iterative fashion allowing for a diastereoselective installation of two aryl groups along an alkyl chain.

Journal of the American Chemical Society published new progress about Arylation, stereoselective (regioselective). 1428537-19-2 belongs to class pyridine-derivatives, and the molecular formula is C13H15F3N2O, Quality Control of 1428537-19-2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Salinas, Yolanda; Brueggemann, Oliver; Monkowius, Uwe; Teasdale, Ian published the artcile< Visible light photocleavable ruthenium-based molecular gates to reversibly control release from mesoporous silica nanoparticles>, Category: pyridine-derivatives, the main research area is ruthenium silicon nanoparticle delivery controlled release visible light irradiation; cargo release on demand; mesoporous silica nanoparticles (MSNs); molecular gates; reversibility; ruthenium complex; visible light photocleavage.

Herein we present hybrid mesoporous silica nanomaterials (MSN) with visible light-sensitive ruthenium complexes acting as gates. Two different [Ru(bpy)2L1L2]2+ complexes were investigated by grafting [Ru(bpy)2(4AMP)2](PF6)2 (RC1) and [Ru(bpy)2(PPh3)Cl]Cl (RC2) via two or one ligands onto the surface of mesoporous silica nanoparticles (MSNs), to give MSN1-RC1 and MSN2-RC2, resp. The pores were previously loaded with a common dye, safranin O, and release studies were conducted. The number and position of the ligands were shown to influence the photocages behavior and thus the release of the cargo. Release studies from MSN1-RC1 in acetonitrile showed that in the dark the amount of dye released was minimal after 300 min, whereas a significant increase was measured upon visible light irradiation (ca. 90%). Release studies from the second nanomaterial MSN2-RC2, where the complex RC2 was bound to the MSN via only one ligand, showed stability under darkness and in aqueous solution up to 180 min and, rapid release of the dye when irradiated with visible light. Furthermore, this system was demonstrated to be reversible, since, upon heating to 80°C, the system could effectively re-close the pores and re-open it again upon visible light irradiation

Nanomaterials published new progress about Ligands Role: THU (Therapeutic Use), BIOL (Biological Study), USES (Uses). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Hao; Gao, Ang; Liu, Xiu-Yan; Ding, Chang-Hua; Xu, Bin; Hou, Xue-Long published the artcile< Kinetic Resolution of 5-Substituted Cyclohexenols by Palladium-Catalyzed Asymmetric Redox-Relay Heck Reaction>, Name: (S)-4-(tert-Butyl)-2-(5-(trifluoromethyl)pyridin-2-yl)-4,5-dihydrooxazole, the main research area is cyclohexenol arylboronic acid palladium catalyst Heck reaction kinetic resolution; aryl cyclohexanone cyclohexenol preparation enantioselective diastereoselective.

The kinetic resolution of 2-substituted-cyclohexenols via palladium-catalyzed asym. redox-relay Heck reaction was realized, providing optically active 2-substituted cyclohexenols and trans-3,5-disubstituted cyclohexan-1-ones in high yield and good enantioselectivities with an S factor up to 22.

Synthesis published new progress about Cyclic ketones Role: BYP (Byproduct), PRP (Properties), PUR (Purification or Recovery), SPN (Synthetic Preparation), PREP (Preparation). 1416819-91-4 belongs to class pyridine-derivatives, and the molecular formula is C13H15F3N2O, Name: (S)-4-(tert-Butyl)-2-(5-(trifluoromethyl)pyridin-2-yl)-4,5-dihydrooxazole.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mei, Tian-Sheng; Patel, Harshkumar H.; Sigman, Matthew S. published the artcile< Enantioselective construction of remote quaternary stereocentres>, Quality Control of 1416819-91-4, 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). 1416819-91-4 belongs to class pyridine-derivatives, and the molecular formula is C13H15F3N2O, Quality Control of 1416819-91-4.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Hou, Lixia; Zhang, Yujin; Li, Cuicui; Wang, Xuede; Wang, Selina C. published the artcile< Determination of main bitter compounds in soaked and germinated sesame pastes>, HPLC of Formula: 93-60-7, the main research area is sesame paste germination soaking bitter compound determination; bitterness; germination; non-volatile; sesame pastes; volatile compounds.

The flavor and taste of the foods play an important or even a decisive role in the acceptance and preference of the consumers. It was found that the sesame paste prepared with the germinated sesame seeds was bitter in our previous experiment In the study, the volatile and non-volatile bitter-taste components of the sesame paste samples were comprehensively analyzed. 2-methylbutanal, hexanal, acetic acid, and butyric acid were the predominant volatile compounds in the soaked and germinated sesame pastes. Oxalate was significantly reduced by the germination (p < 0.05). The contents of sesaminoltriglucoside in sesame pastes ranged from 129.04 to 217.57μg/g. Both total and individual free amino acid contents increased with the prolongation of the germinating time. The bitter-taste amino acid Arg had the highest score of Taste Activity Value for the bitterest sample made from the seeds germinated for 36 h. The bitter-tasting Arg was first reported to impart a bitter taste to the germinated sesame paste. Journal of Oleo Science published new progress about Acids Role: ANT (Analyte), FFD (Food or Feed Use), ANST (Analytical Study), BIOL (Biological Study), USES (Uses). 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, HPLC of Formula: 93-60-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem