Tag: M.W=100-150

Arshad, Zarina; Saied, Sumayya; Ali, Basharat; Salar, Uzma; Tauseef, Saima; Arshia; Ajaz, Munazza; Khan, Uroosa; Haider, Syed Moazzam; Taha, Muhammad; Khan, Khalid Mohammed published the artcile< Synthesis of N'-nicotinoyl sulfonohydrazides and their antimicrobial activity>, Formula: C7H7NO2, the main research area is nicotinoyl sulfonohydrazide preparation antibacterial antifungal.

N’-Nicotinoyl sulfonohydrazide derivatives I [R = Me, Ph, 2-O2NC6H4, etc.] were synthesized from nicotinyl hydrazide and evaluated for their antimicrobial potential against Gram pos. bacterial strains (Bacillus cereus, Bacillus subtilis, Corynebacterium diphtheriae, Staphylococcus fecalis, Staphylococcus aureus and MRSA (Methicillin-resistant Staphylococcus aureus)) and Gram neg. bacterial strains (Escherichia.coli, Pseudomonas aeruginosa, Salmonella ParatyphiB, Salmonella tyhpi). Compound I [R = 2-OH-3,5-diClC6H2] showed outstanding antibacterial activity against Staphylococcus fecalis and compounds I [R = 2-O2NC6H4, 2-OH-3,5-diClC6H2] were found to be moderately activite against Salmonella Paratyphi B, shown by their zone of inhibition values. In addition to that compond I [R = Me] also showed moderate activity against Escherichia coli. All derivatives I were also subjected for the evaluation of their antifungal activity against Saccharomyces cerevisiae, Microsporum canin, Rhizopus, Aspergillus niger, Candida albicans and Candida tropicalis. Compound I [R = 2-OH-3,5-diClC6H2] showed promising antifungal activity against Rhizopus sp. and compounds I [R = Me, 2,4-di-MeOC6H3] showed moderate antifungal potential against Microsporum canis, Aspergillus niger and Candida tropicalis.

Journal of the Chemical Society of Pakistan published new progress about Antibacterial agents. 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Formula: C7H7NO2.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Pesti, Jaan A.; Huhn, George F.; Yin, Jianguo; Xing, Yide; Fortunak, Joseph M.; Earl, Richard A. published the artcile< Efficient Pyridinylmethyl Functionalization: Synthesis of 10,10-Bis[(2-fluoro-4-pyridinyl)methyl]-9(10H)-anthracenone (DMP 543), an Acetylcholine Release Enhancing Agent>, COA of Formula: C6H6FNO, the main research area is methylpyridine chlorination; pyridylmethyl methanesulfonate preparation alkylation reagent; fluoropyridinylmethylanthrone preparation; anthrone bisfluoropyridinylmethyl preparation.

2-Fluoro-4-methylpyridine is efficiently functionalized by chlorination, hydrolysis and methanesulfonylation into the novel alkylating agent 2-Fluoro-4-methanesulfonylmethylpyridine. This mesylate is used for the bisalkylation of anthrone under carefully defined conditions to prepare the title compound, a cognition enhancer drug candidate. This process proceeds in up to 37% overall yield and is adaptable for large scale synthesis. The chlorination of other methylpyridines was also investigated.

Journal of Organic Chemistry published new progress about Chlorination. 131747-55-2 belongs to class pyridine-derivatives, and the molecular formula is C6H6FNO, COA of Formula: C6H6FNO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Chaojie; Wei, Zhangwen; Pan, Mei; Deng, Haiying; Jiang, Jijun; Su, Chengyong published the artcile< Structural tuning of coordination polymers by 4-connecting metal node and secondary building process>, Synthetic Route of 3731-53-1, the main research area is transition metal pyridylmethylnaphthalenediimide coordination polymer preparation crystal structure.

Five transition metal coordination polymers, {[Cu(4-pmntd)2(NO3)2]•2CHCl3}n (1), {[Cu(4-pmntd)2(NO3)2]·3C7H8}n (2), {[Cu(4-pmntd)2(CF3SO3)(H2O)]·CF3SO3·H2O·MeOH}n (3), [Cd(4-pmntd)2]n·nSiF6·x(MeOH)·y(CHCl3) (4), and [Zn(4-pmntd)2(CF3SO3)2]n·x(solvent) (5), were obtained from a ditopic ligand, N,N’-bis(4-pyridylmethyl)naphthalene diimide (4-pmntd). Either sql- or dia- structures are generated from four connecting coordination nodes of the metal centers. While delicate interpenetration and structural tuning in these complexes is achieved by the different conformations and spatially extending geometries adopted by the ligand and secondary building process induced by pillar-like anions.

Chinese Chemical Letters published new progress about Coordination polymers Role: PRP (Properties), SPN (Synthetic Preparation), PREP (Preparation). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Synthetic Route of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Chen, Hong; Li, Ridong; Ning, Xianling; Zhao, Xuyang; Jin, Yan; Yin, Yuxin published the artcile< Synthesis and anti-tumor efficacy of novel 2, 4-diarylaminopyrimidine derivatives bearing N-(3-pyridinylmethyl) urea moiety as anaplastic lymphoma kinase inhibitors>, Safety of Pyridin-4-ylmethanamine, the main research area is chloro amino pyrimidinylamino methoxyphenyl pyridinylmethyl urea preparation; antitumor activity anaplastic lymphoma kinase inhibition SAR docking cytotoxicity; ALK inhibitor; Anti-proliferation activity; NSCLC; Structure modification.

A series of novel 2,4-diarylaminopyrimidine derivatives I [R = 3,5-dimethoxyphenyl, 6-quinolyl, 3-methoxy-4-morpholino-Ph, etc.] possessing a unique N-(3-pyridinylmethyl)urea moiety as ALK inhibitors were synthesized. The most promising analog compound I [R = 3-methoxy-4-morpholino-phenyl] significantly inhibited proliferation of ALK pos. H3122 and Karpas-299 cells with IC50 values about 10 nM, which were comparable with pos. control LDK378. Compound I [R = 3-methoxy-4-morpholino-phenyl] suppressed phosphorylation of ALK and its downstream proteins and showed low cytotoxicity on normal human primary fibroblast cells (BJ cells). The binding mode of compound I [R = 3-methoxy-4-morpholino-phenyl] was proposed by docking simulation, which explains the important role of N-(3-pyridinylmethyl)urea moiety. Furthermore, compound I [R = 3-methoxy-4-morpholino-phenyl] exhibited favorable liver microsomal stability and significant efficacy in H3122 xenograft mice model. Interestingly, compound I [R = 3-methoxy-4-morpholino-phenyl] also showed broader anti-proliferative activity on other human tumor cell lines, which was different from other ALK inhibitors.

European Journal of Medicinal Chemistry published new progress about Amines Role: ADV (Adverse Effect, Including Toxicity), PAC (Pharmacological Activity), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Safety of Pyridin-4-ylmethanamine.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Dong; Jiang, Yuanyang; Dong, Linru; Li, Gaoyu; Sun, Baoying; Desaubry, Laurent; Yu, Peng published the artcile< One-Pot Selective Saturation and Functionalization of Heteroaromatics Leading to Dihydropyridines and Dihydroquinolines>, Related Products of 93-60-7, the main research area is pyridine one pot regioselective dearomatization bond formation; dihydropyridine preparation; quinoline one pot regioselective dearomatization bond formation; dihydroquinoline preparation.

A one-pot regioselective two C-C-bond-forming dearomatization of pyridines and quinolines is disclosed. Two 3,4-betaines are identified for the first time as very useful organic synthons in heterocyclic chem. Furthermore, the chem. reactivity of the prepared trifluoromethyl ketones, a new type of push-pull enones, has been explored to develop straightforward methods for their functionalization. This protocol represents a breakthrough in the dearomatization of heteroaromatics as both the selective saturation and functionalization of heteroaromatics are achieved in high efficiency by the attachment of two substituents, including the valuable trifluoromethyl ketone group.

Journal of Organic Chemistry published new progress about C-C bond formation. 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, Related Products of 93-60-7.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Wang, Chao; Rui, Xiyan; Si, Dongjuan; Dai, Rupeng; Zhu, Yueyue; Wen, Hongmei; Li, Wei; Liu, Jian published the artcile< Copper-Catalyzed Three-Component Cascade Reaction of Benzaldehyde with Benzylamine and Hydroxylamine or Aniline: Synthesis of 1,2,4-Oxadiazoles and Quinazolines>, Quality Control of 3731-53-1, the main research area is aryl aldehyde aromatic amine copper catalyst tandem cyclization; biaryl oxadiazole preparation green chem; benzaldehyde benzylamine copper catalyst tandem cyclization green chem; diphenyl quinazoline preparation.

The analogous three-component synthesis strategy for substituted 1,2,4-oxadiazoles and quinazolines derivatives from readily available benzaldehydes, benzylamines and hydroxylamine or anilines was developed. Both the cascade reaction sequences involved nucleophilic addition of C-N bond, introduction a halogen donor, nucleophilic substitution and Cu(II)-catalyzed aerobic oxidation This synthesis methodol. demonstrated good yields, broad substrate scope and oxygen as a green oxidant. Thus, this synthesis protocol provided strategies for the construction of substituted 1,2,4-oxadiazole and quinazolines from readily and simple starting materials.

Advanced Synthesis & Catalysis published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Quality Control of 3731-53-1.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Mohammad Arshad published the artcile< Design, Drug-Likeness, Synthesis, Characterization, Antimicrobial Activity, Molecular Docking, and MTT Assessment of 1,3-Thiazolidin-4-one Bearing Piperonal and Pyrimidine Moieties>, Category: pyridine-derivatives, the main research area is thiazolidinone piperonal pyrimidine moiety antimicrobial activity mol docking.

The recent study reported the designing of substituted 3-[4-(1,3-benzodioxol-5-yl)-6-(pyridin-2-yl)pyrimidin-2-yl]-2-(pyridin-2-yl)-1,3-thiazolidin-4-one derivatives and assessed computationally to calculate the bioactivity and physicochem. properties. The substituted 3-[4-(1,3-benzodioxol-5-yl)-6-(pyridin-2-yl)pyrimidin-2-yl]-2-(pyridin-2-yl)-1,3-thiazolidin-4-one derivatives represented the bioactivity score in the zone for an active drug mol. and were in compliance with the Lipinski Rule of five. Then the synthesis, characterization, and biol. screening as antimicrobial potential and percent viability of cells were carried out for the substituted 3-[4-(1,3-benzodioxol-5-yl)-6-(pyridin-2-yl)pyrimidin-2-yl]-2-(pyridin-2-yl)-1,3-thiazolidin-4-one derivatives The zone of inhibition and min. inhibitory concentration (MIC) findings portrayed that the compounds-(IV) and compound-(V) possessed better antimicrobial activity than the reference drug ciprofloxacin, while the significant antimicrobial potential was observed by other members of the series. The mol. docking studies were performed to assist the in vitro antimicrobial results and the findings exhibited that significant H-bonding in between the substituted 3-[4-(1,3-benzodioxol-5-yl)-6-(pyridin-2-yl)pyrimidin-2-yl]-2-(pyridin-2-yl)-1,3-thiazolidin-4-one derivatives and the residues of GlcN-6-P-synthase, like ASP 474 (I-IX), SER 316 (I-VI), ASN 522 (I-IX), TRP 313 (V) with good binding affinity ranging -7.7 to -6.8 kcal/mol. The compounds represented the less toxic effects to the HepG2 cells and the percent viability of the cells ranging from 93-98%, 73-78% and 70-76% up to 3.125, 50, 100 mmol/L resp.

Russian Journal of Bioorganic Chemistry published new progress about Antimicrobial agents. 350-03-8 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Liu, Jinguo; Yin, Feng; Hu, Jun; Ju, Yong published the artcile< Cu2+-triggered shrinkage of a natural betulin-derived supramolecular gel to fabricate moldable self-supporting gel>, Category: pyridine-derivatives, the main research area is copper ion shrinkage betulin supramol gel moldable self supporting.

Most supramol. gels have a poor ability to be molded into well-defined shapes, preventing them from having the same potential as clay-based and polymeric gels in applications. In this research, a natural betulin-derived bola-type amphiphile Py-BL was synthesized and found to assemble into a supramol. gel with left-handed helixes driven by hydrogen bonding and hydrophobic interactions. Due to the pyridine groups, which were able to coordinate metal ions and were sensitive to acidity, the resulting Py-BL gel exhibited responses to certain metal ions, and Cu2+-selective gel shrinkage was observed, with a contraction of the gel phase in three dimensions. The coordination between Cu2+ and pyridine groups in the ratio of 1 : 4 led to a cross-linked network of nanofibers and decreased the hydrophilic performance of the Py-BL gel, consequently causing the gelling solvent to extrude from the gel network with a macroscopic gel shrinkage. This Cu2+-triggered shrunken gel exhibited an improved rheol. strength and could self-demold spontaneously through the shrinkage process with a precise amount of Cu2+. Using this strategy, we fabricated moldable self-supporting supramol. gels with designed shapes and elec. conductivity It is believed that the Cu2+-triggered shrinkage provides a novel approach to the fabrication of moldable self-supporting supramol. gels at ultralow gel loadings.

Materials Chemistry Frontiers published new progress about Fluorescence. 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Garrett, Mark D.; Scott, Robin; Sheldrake, Gary N.; Dalton, Howard; Goode, Paul published the artcile< Biotransformation of substituted pyridines with dioxygenase-containing microorganisms>, Product Details of C5H4ClNO, the main research area is toluene dioxygenase substituted pyridine oxidation.

A series of 2-, 3- and 4-substituted pyridines was metabolized using the mutant soil bacterium Pseudomonas putida UV4 which contains a toluene dioxygenase (TDO) enzyme. The regioselectivity of the biotransformation in each case was determined by the position of the substituent. 4-Alkylpyridines were hydroxylated exclusively on the ring to give the corresponding 4-substituted 3-hydroxypyridines, while 3-alkylpyridines were hydroxylated stereoselectively on C-1 of the alkyl group with no evidence of ring hydroxylation. 2-Alkylpyridines gave both ring and side-chain hydroxylation products. Chloro- and bromo-substituted pyridines, and pyridine itself, while being poor substrates for P. putida UV4, were converted to some extent to the corresponding 3-hydroxypyridines. These unoptimized biotransformations are rare examples of the direct enzyme-catalyzed oxidation of pyridine rings and provide a novel synthetic method for the preparation of substituted pyridinols. Evidence for the involvement of the same TDO enzyme in both ring and side-chain hydroxylation pathways was obtained using a recombinant strain of Escherichia coli (pKST11) containing a cloned gene for TDO. The observed stereoselectivity of the side-chain hydroxylation process in P. putida UV4 was complicated by the action of an alc. dehydrogenase enzyme in the organism which slowly leads to epimerization of the initial (R)-alc. bioproducts by dehydrogenation to the corresponding ketones followed by stereoselective reduction to the (S)-alcs.

Organic & Biomolecular Chemistry published new progress about Oxidation, regioselective. 96630-88-5 belongs to class pyridine-derivatives, and the molecular formula is C5H4ClNO, Product Details of C5H4ClNO.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Campos, Debora L.; Machado, Ignacio; Ribeiro, Camila M.; Gambino, Dinorah; Pavan, Fernando R. published the artcile< Bactericidal effect of pyridine-2-thiol 1-oxide sodium salt and its complex with iron against resistant clinical isolates of Mycobacterium tuberculosis>, Category: pyridine-derivatives, the main research area is Mycobacterium antibacterial pyridine thiol oxide sodium salt.

We determined the activity of pyridine-2-thiol 1-oxide sodium salt (Na mpo) and its complex with iron [Fe(mpo)3] against Mycobacterium tuberculosis. The compounds were tested against a standard strain of M. tuberculosis H37Rv (ATCC 27294), with minimal inhibitory concentrations (MIC90) of 7.20 and 1.07 μM to Na mpo and [Fe(mpo)3], resp., and against 3 clin. isolates with different genotypic profiles, with MIC values ranging 0.74-6.52 and 0.30-2.25 μM to Na mpo and [Fe(mpo)3], resp. [Fe(mpo)3] was more effective against susceptible strains but both compounds were effective in inhibiting MDR and XDR-TB clin. strains. The profile activity was determined through the methodol. of a time-kill curve against standard and clin. strains of M. tuberculosis. Time-kill studies indicated that Na mpo had an early bactericidal activity against H37Rv and clin. isolates, with sterilizing effects observed in 5 and 7 days, resp., at its MIC90. The anti MDR and XDR-M. tuberculosis activity and bactericidal effect of Na mpo and [Fe(mpo)3] demonstrate their potential as new compounds for the treatment of tuberculosis.

Journal of Antibiotics published new progress about Mycobacterium tuberculosis. 3811-73-2 belongs to class pyridine-derivatives, and the molecular formula is C5H4NNaOS, Category: pyridine-derivatives.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem