Day: December 6, 2021

Poladian, Q; Sahin, O; Karakurt, T; Ilhan-Ceylan, B; Kurt, Y in [Poladian, Qumars; Ilhan-Ceylan, Berat; Kurt, Yasemin] Istanbul Univ Cerrahpasa, Engn Fac, Dept Chem, TR-34320 Istanbul, Turkey; [Sahin, Onur] Sinop Univ, Fac Hlth Sci, Dept Occupat Hlth & Safety, TR-57000 Sinop, Turkey; [Karakurt, Tuncay] Kirsehir Ahi Evran Univ, Fac Engn Architecture, Dept Chem & Proc Engn, TR-40100 Kirsehir, Turkey published A new zinc(II) complex with N2O2-tetradentate schiff-base derived from pyridoxal-S-methylthiosemicarbazone: Synthesis, characterization, crystal structure, DFT, molecular docking and antioxidant activity studies in 2021.0, Cited 69.0. Recommanded Product: 65-22-5. The Name is 3-Hydroxy-5-(hydroxymethyl)-2-methylisonicotinaldehyde hydrochloride. Through research, I have a further understanding and discovery of 65-22-5.

A new unsymmetrical N2O2-tetradentate Schiff-base complex of zinc(II) was synthesized by the template reaction of pyridoxal-S-methylthiosemicarbazone and 2-hydroxy-4-methoxy-benzaldehyde as starting compounds. S-methylthiosemicarbazone (1) and zinc(II) complex [Zn(L)CH3OH] ( 2) were characterized by elemental analysis, FT-IR, UV-visible, H-1, and C-13 NMR spectra. The molecular structure of the complex (2) was determined by single crystal X-ray diffraction technique. The structure consists of a distorted square-pyramidal geometry around the central metal, Zn(II). Quantum chemical calculations were carried out using density functional theory DFT/B3LYP, 6-31G (d), and LanL2DZ basis sets for theoretical characterization of the compounds. The experimental and theoretical data were compared comprehensively. The potential energy distribution (PED) analysis was performed for the assignment of vibration frequencies. In order to support in vitro studies, molecular docking studies have been carried out so that the title compound can be an inhibitor of Epidermal Growth Factor Receptor (1 m17), and the relationship between calculated HOMO energies and docking studies has been examined. In addition, the total antioxidant capacity (as TEAC value) and free radical scavenging activity of the compounds were determined by Cupric Reducing Antioxidant Capacity (CUPRAC) and 1,1-diphenyl-2-picryl hydrazyl (DPPH) methods, respectively. (C) 2021 Elsevier Ltd. All rights reserved.

Recommanded Product: 65-22-5. Welcome to talk about 65-22-5, If you have any questions, you can contact Poladian, Q; Sahin, O; Karakurt, T; Ilhan-Ceylan, B; Kurt, Y or send Email.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

Category: pyridine-derivatives. In 2020.0 DALTON T published article about NI-II COMPLEXES; MOLECULAR-STRUCTURE; HYDROLYSIS; MECHANISM; LIGANDS; ESTERS; DRUGS; COBALT(III); DERIVATIVES; KINETICS in [Dasgupta, Sanchari; Karim, Suhana; Das, Debasis] Univ Calcutta, Dept Chem, 92 APC Rd, Kolkata 700009, India; [Banerjee, Saswati; Saha, Moumita; Saha, Krishna Das] CSIR Indian Inst Chem Biol, Canc Biol & Inflammatory Disorder Div, 4 Raja SC Mullick Rd, Kolkata 700032, India in 2020.0, Cited 48.0. The Name is Phenyl(pyridin-2-yl)methanone. Through research, I have a further understanding and discovery of 91-02-1.

Three asymmetric tridentate acyl hydrazone Schiff base ligands namely L1, L2 and L3 were prepared via condensation of 4-methoxybenzohydrazide with picolinaldehyde, 1-(pyridin-2-yl)ethanone and phenyl(pyridin-2-yl)methanone respectively. Three bio-relevant mononuclear zinc(ii) complexes [Zn(L1)Cl-2]2H(2)O (1), [Zn(L2)Cl-2] (2) and [Zn(L3)Cl-2] (3) were synthesized by treatment of zinc(ii) chloride with the corresponding Schiff base ligands and characterised by the usual physicochemical techniques. The solid state structures of complexes 1 and 3 were evaluated by single crystal X-ray analysis. All complexes were able to hydrolyse the P-O bond of the phosphate monoester in 90% (v/v) DMSO-water medium using 4-nitrophenylphosphate (4-NPP) as the model substrate and the trend in their activity is 1 approximate to 2 > 3. On considering the highly efficient hydrolysis properties, complexes 1-3 were tested as potential therapeutic agents for cancer using HCT116 (human colorectal carcinoma), HepG2 (human hepatocellular carcinoma) and A549 (human non-small lung carcinoma) cells. Complex 2 showed the highest IC50 values for anti-cancer activity towards all three cell lines among the three complexes and complex 3 showed the least activity as observed in the phosphatase activity study. The internucleosomal degradation of DNA during apoptosis can be detected by cell death detection ELISA. DNA fragmentation that leads to cell death was examined and when induced by complex 2 in HepG2 cells a significant level of DNA fragmentation was observed at regular intervals of time.

Category: pyridine-derivatives. Bye, fridends, I hope you can learn more about C12H9NO, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

COA of Formula: C12H9NO. Yuan, Q; Chen, LL; Zhu, XH; Yuan, ZH; Duan, YT; Yang, YS; Wang, BZ; Wang, XM; Zhu, HL in [Yuan, Qing; Chen, Li-Li; Zhu, Xiao-Hua; Yuan, Zeng-Hui; Yang, Yu-Shun; Wang, Bao-Zhong; Wang, Xiao-Ming; Zhu, Hai-Liang] Nanjing Univ, Sch Life Sci, State Key Lab Pharmaceut Biotechnol, Nanjing 210023, Peoples R China; [Duan, Yong-Tao] Zhengzhou Univ, Childrens Hosp, Henan Prov Key Lab Childrens Genet & Metab Dis, Zhengzhou 450018, Peoples R China published An imidazo[1,5-alpha]pyridine-derivated fluorescence sensor for rapid and selective detection of sulfite in 2020.0, Cited 55.0. The Name is Phenyl(pyridin-2-yl)methanone. Through research, I have a further understanding and discovery of 91-02-1.

Sulfur-containing species are essential in the composition and the metabolism of the organisms, thus developing a full set of implements to cover all of them is still a favorable choice. Herein, we chose imidazo [1,5-alpha] pyridine moiety as the basic fluorophore for the detection of sulfite, and preliminarily completed the toolset since biothiols (GSH, Cys, Hcy), H2S, and PhSH could be detected by sensors based on the same backbone. The designed sensor, IPD-SFT, with structural novelty and large Stokes shift (130 nm), indicated the most attractive advantages of remarkably rapid response period (within 1 min) and high selectivity for sulfite from all the sulfurcontaining species. Other practical properties included high sensitivity (LOD = 50 nM) and wide pH adaptability (5.0-11.0). Furthermore, IPD-SFT could monitor both exogenous and endogenous sulfite. It not only raised a potential tool for sulfite detection, but also preliminarily completed the toolset for all the sulfur-containing species. The development of such toolsets might reveal the sulfur-containing metabolism and corresponding physiology and pathological procedures.

COA of Formula: C12H9NO. Bye, fridends, I hope you can learn more about C12H9NO, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

Recommanded Product: Phenyl(pyridin-2-yl)methanone. Recently I am researching about NUCLEOPHILIC FLUOROMETHYLATION; STRAIGHTFORWARD ACCESS; EFFICIENT SYNTHESIS; FLUORINE; HOMOLOGATION; CARBENOIDS; STABILITY; MONOFLUOROMETHYLATION; FLUOROALKYLATION; EPOXIDATION, Saw an article supported by the University of Vienna; project Laboratorio Sistema – MIURMinistry of Education, Universities and Research (MIUR) [PONa300369]; MISEMinistry of Economic Development, Italy; Horizon 2020 – PON 2014/2020 FARMIDIAB [338]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Monticelli, S; Colella, M; Pillari, V; Tota, A; Langer, T; Holzer, W; Degennaro, L; Luisi, R; Pace, V. The CAS is 91-02-1. Through research, I have a further understanding and discovery of Phenyl(pyridin-2-yl)methanone

An expeditious, high-yielding synthesis of rare alpha-fluoroepoxides and alpha-fluoroaziridines through the addition of the unkown fluoroiodomethyllithium (LiCHIF)-formed via deprotonation the commercially available fluoroiodomethane with a lithium amide base-to carbonyl-like compounds is documented. The ring-closure reactions, leading to alpha-fluorinated three-membered heterocycles, rely on the diversely reactive C-I and C-F bonds. Excellent chemoselectivity was observed in the presence of highly sensitive functionalities-aldehyde, ketone, nitrile, alkene-which remained untouched during the homologation sequence.

Recommanded Product: Phenyl(pyridin-2-yl)methanone. Bye, fridends, I hope you can learn more about C12H9NO, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

An article 4-Het(aryl)-2-pyrrolidone-3(5)-carboxylic acid alkyl(hetaryl)idenecarbohydrazides: synthesis and structure WOS:000524864600006 published article about HYDRAZONES in [Gorodnicheva, N. V.; Vasil’eva, O. S.; Ostroglyadov, E. S.; Baichurin, R. I.; Makarenko, S. V.] Herzen State Pedag Univ Russia, 48 Nab R Moiki, St Petersburg 191186, Russia; [Karamov, F. A.] Kazan Natl Res Tech Univ, 10 Ul K Marksa, Kazan 420111, Russia; [Lodochnikova, O. A.; Litvinov, I. A.] Russian Acad Sci, Kazan Sci Ctr, Fed Res Ctr, AE Arbuzov Inst Organ & Phys Chem, 8 Ul Akad Arbuzova, Kazan 420088, Russia in 2020.0, Cited 25.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. SDS of cas: 500-22-1

4-Het(aryl)-2-pyrrolidone-3(5)-carboxylic acid hydrazides react with aromatic aldehydes, acetone, and acetophenone to give new representatives of N ‘-alkyl(hetaryl)idenecarbohydrazides of (3R*,4S*)-4-het(aryl)-2-pyrrolidone-3- and (4R*,5R*)-4-het(aryl)-2-pyrrolidone-5-carboxylic acids.

Welcome to talk about 500-22-1, If you have any questions, you can contact Gorodnicheva, NV; Vasil’eva, OS; Ostroglyadov, ES; Baichurin, RI; Makarenko, SV; Karamov, FA; Lodochnikova, OA; Litvinov, IA or send Email.. SDS of cas: 500-22-1

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

An article Synthesis, molecular docking analysis and carbonic anhydrase I-II inhibitory evaluation of new sulfonamide derivatives WOS:000487812000049 published article about BIOLOGICAL EVALUATION; ISOZYMES I; ISOFORMS I; DRUG DESIGN; HYDRAZONE; POTENT; COMPLEXES; XII; SOLUBILITY; ANALOGS in [Saglik, Begum Nurpelin; Cevik, Ulviye Acar; Osmaniye, Derya; Levent, Serkan; Cavusoglu, Betul Kaya; Ozkay, Yusuf; Kaplancikli, Zafer Asim] Anadolu Univ, Fac Pharm, Dept Pharmaceut Chem, TR-26470 Eskisehir, Turkey; [Saglik, Begum Nurpelin; Cevik, Ulviye Acar; Osmaniye, Derya; Levent, Serkan; Ozkay, Yusuf] Anadolu Univ, Fac Pharm, Doping & Narcot Cpds Anal Lab, TR-26470 Eskisehir, Turkey; [Demir, Yeliz] Ardahan Univ, Nihat Delibalta Gole Vocat High Sch, Dept Pharm Serv, TR-75700 Ardahan, Turkey; [Ilgin, Sinem] Anadolu Univ, Fac Pharm, Dept Toxicol, TR-26470 Eskisehir, Turkey; [Koparal, Ali Savas] Anadolu Univ, Open Educ Fac, TR-26470 Eskisehir, Turkey; [Beydemir, Sukru] Anadolu Univ, Fac Pharm, Dept Biochem, TR-26470 Eskisehir, Turkey in 2019.0, Cited 60.0. Application In Synthesis of 3-Pyridinecarboxaldehyde. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

New sulfonamide-hydrazone derivatives (3a-3n) were synthesized to evaluate their inhibitory effects on purified human carbonic anhydrase (hCA) I and II. The inhibition profiles of the synthesized compounds on hCA I-II isoenzyme were investigated by comparing their IC50 and K-i values. Acetazolamide (5-acetamido-1,3,4-thia-diazole-2-sulfonamide, AZA) has also been used as a standard inhibitor. The compound 3e demonstrated the best hCA I inhibitory effect with a K-i value of 0.1676 +/- 0.017 mu M. Besides, the compound 3m showed the best hCA II inhibitory effect with a K-i value of 0.2880 +/- 0.080 mu M. Cytotoxicity of the compounds 3e and 3m toward NIH/3T3 mouse embryonic fibroblast cell line was observed and the compounds were found to be non-cytotoxic. Molecular docking studies were performed to investigate the interaction types between active compounds and hCA enzymes. Pharmacokinetic profiles of compounds were assessed by theoretical ADME predictions. As a result of this study a novel and potent class of CA inhibitors were identified with a good activity potential.

Application In Synthesis of 3-Pyridinecarboxaldehyde. Welcome to talk about 500-22-1, If you have any questions, you can contact Saglik, BN; Cevik, UA; Osmaniye, D; Levent, S; Cavusoglu, BK; Demir, Y; Ilgin, S; Ozkay, Y; Koparal, AS; Beydemir, S; Kaplancikli, ZA or send Email.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

Name: Ethyl nicotinate. In 2020 ORG BIOMOL CHEM published article about RECYCLABLE CATALYSTS; ALKYL NITRATES; THERAPY in [An, Jichao; Liu, Peipei; Si, Mengyuan; Li, Wenhao; He, Pan; Yang, Bo; Yang, Guanyu] Zhengzhou Univ, Coll Chem, Zhengzhou 450001, Peoples R China in 2020, Cited 23. The Name is Ethyl nicotinate. Through research, I have a further understanding and discovery of 614-18-6.

To pursue a sustainable and efficient approach for aliphatic nitroester preparation from alcohol, europium-triflate-catalyzed nitration, which directly uses commercial nitric acid, has been successfully developed. Gram scalability with operational ease showed its practicability.

Name: Ethyl nicotinate. Welcome to talk about 614-18-6, If you have any questions, you can contact An, JC; Liu, PP; Si, MY; Li, WH; He, P; Yang, B; Yang, GY or send Email.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

Zhang, Y; Hatami, N; Lange, NS; Ronge, E; Schilling, W; Jooss, C; Das, S in [Zhang, Yu; Das, Shoubhik] Univ Antwerp, Dept Chem, ORSY Div, Gronenborgerlaan 171, B-2020 Antwerp, Belgium; [Zhang, Yu; Hatami, Nareh; Lange, Niklas Simon; Schilling, Waldemar] Georg August Univ Gottingen, Inst Biomol & Organ Chem, Tammannstr 2, D-37077 Gottingen, Germany; [Ronge, Emanuel; Jooss, Christian] Georg August Univ Gottingen, Inst Materialphys, Friedrich Hund Pl 1, D-37077 Gottingen, Germany published A metal-free heterogeneous photocatalyst for the selective oxidative cleavage of C = C bonds in aryl olefins via harvesting direct solar energy in 2020, Cited 68. COA of Formula: C12H9NO. The Name is Phenyl(pyridin-2-yl)methanone. Through research, I have a further understanding and discovery of 91-02-1.

Selective cleavage of C & xe001;C bonds is highly important for the synthesis of carbonyl containing fine chemicals and pharmaceuticals. Novel methodologies such as ozonolysis reactions, Lemieux-Johnson oxidation reactionetc. already exist. Parallel to these, catalytic methods using homogeneous catalysts also have been discovered. Considering the various advantages of heterogeneous catalysts such as recyclability and stability, couple of transition metal-based heterogeneous catalysts have been applied for this reaction. However, the pharmaceutical industries prefer to use metal-free catalysts (especially transition metal-free) to avoid further leaching in the final products. This is for sure a big challenge to an organic chemist and to the pharmaceutical industries! To make this feasible, a mild and efficient protocol has been developed using polymeric carbon nitrides (PCN) as metal-free heterogeneous photocatalysts to convert various olefins into the corresponding carbonyls. Later, this catalyst has been applied in the gram scale synthesis of pharmaceutical drugs using direct solar energy. Detailed mechanistic studies revealed the actual role of oxygen, the catalyst, and the light source.

COA of Formula: C12H9NO. Bye, fridends, I hope you can learn more about C12H9NO, If you have any questions, you can browse other blog as well. See you lster.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

An article Antimicrobial and antitumor activity of S-methyl dithiocarbazate Schiff base zinc(II) complexes WOS:000667427600006 published article about X-RAY-STRUCTURE; METAL-COMPLEXES; BIOLOGICAL EVALUATION; CRYSTAL-STRUCTURE; DNA-BINDING; METHYLDITHIOCARBAZATE SMDTC; ANTIBACTERIAL ACTIVITY; ANTIFUNGAL ACTIVITY; CIRCULAR-DICHROISM; ZN(II) COMPLEXES in [Ramilo-Gomes, Filipa; Addis, Yemataw; Tekamo, Israel; Cavaco, Isabel; Matilde Marques, M.; Pessoa, Joao Costa; Correia, Isabel] Univ Lisbon, Inst Super Tecn, Ctr Quim Estrutural, Av Rovisco Pais, P-1049001 Lisbon, Portugal; [Ramilo-Gomes, Filipa; Addis, Yemataw; Tekamo, Israel; Cavaco, Isabel; Matilde Marques, M.; Pessoa, Joao Costa; Correia, Isabel] Univ Lisbon, Inst Super Tecn, Dept Engn Quim, Av Rovisco Pais, P-1049001 Lisbon, Portugal; [Ramilo-Gomes, Filipa] Univ Lisbon, Inst Invest Medicamento IMed ULisboa, Fac Farm, Av Prof Gama Pinto, P-1649003 Lisbon, Portugal; [Addis, Yemataw; Tekamo, Israel; Cavaco, Isabel] Univ Algarve, Dept Quim & Farm, Campus Gambelas, P-8005139 Faro, Portugal; [Campos, Debora L.; Pavan, Fernando R.] UNESP, Fac Ciencias Farmaceut, CP 582, BR-14801902 Araraquara, SP, Brazil; [Gomes, Clara S. B.] Univ NOVA Lisboa, Dept Quim, LAQV REQUIMTE Lab Associado Quim Verde, Fac Ciencias & Tecnol, P-2829516 Monte De Caparica, Portugal; [Gomes, Clara S. B.] Univ NOVA Lisboa, Appl Mol Biosci Unit UCIBIO, Fac Ciencias & Tecnol, P-2829516 Monte De Caparica, Portugal; [Brito, Vanessa; Santos, Adriana O.; Domingues, Fernanda; Luis, Angelo; Ferreira, Susana; Silvestre, Samuel] Univ Beira Interior, CICS UBI Hlth Sci Res Ctr, Av Infante D Henrique, P-6200506 Covilha, Portugal in 2021.0, Cited 80.0. The Name is 3-Hydroxy-5-(hydroxymethyl)-2-methylisonicotinaldehyde hydrochloride. Through research, I have a further understanding and discovery of 65-22-5. Recommanded Product: 65-22-5

Schiff bases (SB) obtained from S-methyl dithiocarbazate and aromatic aldehydes: salicylaldehyde (H2L1), ovanillin (H2L2), pyridoxal (H2L3) and 2,6-diformyl-4-methylphenol (H3L4), and their corresponding Zn(II)complexes (1-4), are synthesized. All compounds are characterized by elemental analyses, infrared, UV-Vis, nuclear magnetic resonance spectroscopy and mass spectrometry. The structures of H2L2 and [Zn-2(L-1)(2)(H2O) (DMF)] (1a) (DMF = dimethylformamide) are solved by single crystal X-ray diffraction. The SB coordinates the metal center through the Ophenolate, Nimine and Sthiolate atoms. The radical scavenging activity is tested using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, with all ligand precursors showing IC50 values similar to 40 mu M. Cytotoxicity studies with several tumor cell lines (PC-3, MCF-7 and Caco-2) as well as a non-tumoral cell line (NHDF) are reported. Interestingly, 1 has relevant and selective antiproliferative effect against Caco-2 cells (IC50 = 9.1 mu M). Their antimicrobial activity is evaluated in five bacterial strains (Klebsiella pneumoniae, Acinetobacter baumannii, Listeria monocytogenes, Pseudomonas aeruginosa and Staphylococcus aureus) and two yeast strains (Candida albicans and Candida tropicalis) with some compounds showing bacteriostatic and fungicidal activity. The minimal inhibitory concentration (MIC90) of HnL against Mycobacterium tuberculosis is also reported, with H2L2 and H3L4 showing very high activity (MIC90 < 0.6 mu g/mL). The ability of the compounds to bind bovine serum albumin (BSA) and DNA is evaluated for H3L4 and [Zn-2(L-4)(CH3COO)] (4), both showing high binding constants to BSA (ca. 106 M 1) and ability to bind DNA. Overall, the reported compounds show relevant antitumor and antimicrobial properties, our data indicating they may be promising compounds in several fields of medicinal chemistry. Recommanded Product: 65-22-5. About 3-Hydroxy-5-(hydroxymethyl)-2-methylisonicotinaldehyde hydrochloride, If you have any questions, you can contact Ramilo-Gomes, F; Addis, Y; Tekamo, I; Cavaco, I; Campos, DL; Pavan, FR; Gomes, CSB; Brito, V; Santos, AO; Domingues, F; Luis, A; Marques, MM; Pessoa, JC; Ferreira, S; Silvestre, S; Correia, I or concate me.

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

In 2021.0 ACTA PHARMACOL SIN B published article about CELL-DEATH; IN-VITRO; CLASSIFICATION; ORGANIZATION; ANTIFUNGAL in [Zhao, Bing; Zhang, Xinhui; Yu, Tingting; Liu, Ying; Zhang, Xiaoling; Yao, Yongfang; Feng, Xuejian; Liu, Hongmin; Ma, Liying; Qin, Shangshang] Zhengzhou Univ, State Key Lab Esophageal Canc Prevent & Treament, Key Lab Technol Drug Preparat,Inst Pharmaceut Res, Minist Educ China,Key Lab Henan Prov Drug Qual &, Zhengzhou 450001, Henan, Peoples R China; [Zhao, Bing; Zhang, Xinhui; Yu, Tingting; Liu, Ying; Zhang, Xiaoling; Yao, Yongfang; Feng, Xuejian; Liu, Hongmin; Ma, Liying; Qin, Shangshang] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China; [Yu, Dequan] Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China in 2021.0, Cited 44.0. The Name is Phenyl(pyridin-2-yl)methanone. Through research, I have a further understanding and discovery of 91-02-1. Recommanded Product: 91-02-1

New Delhi metallo-beta-lactamase-1 (NDM-1) is capable of hydrolyzing nearly all beta-lactam antibiotics, posing an emerging threat to public health. There are currently less effective treatment options for treating NDM-1 positive superbug, and no promising NDM-1 inhibitors were used in clinical practice. In this study, structure-activity relationship based on thiosemicarbazone derivatives was systematically characterized and their potential activities combined with meropenem (MEM) were evaluated. Compounds 19bg and 19bh exhibited excellent activity against 10 NDM-positive isolate clinical isolates in reversing MEM resistance. Further studies demonstrated compounds 19bg and 19bh were uncompetitive NDM-1 inhibitors with Ki = 0.63 and 0.44 mu mol/L, respectively. Molecular docking speculated that compounds 19bg and 19bh were most likely to bind in the allosteric pocket which would affect the catalytic effect of NDM-1 on the substrate meropenem. Toxicity evaluation experiment showed that no hemolysis activities even at concentrations of 1000 mg/mL against red blood cells. In vivo experimental results showed combination of MEM and compound 19bh was markedly effective in treating infections caused by NDM-1 positive strain and prolonging the survival time of sepsis mice. Our finding showed that compound 19bh might be a promising lead in developing new inhibitor to treat NDM-1 producing superbug. (C) 2021 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.

About Phenyl(pyridin-2-yl)methanone, If you have any questions, you can contact Zhao, B; Zhang, XH; Yu, TT; Liu, Y; Zhang, XL; Yao, YF; Feng, XJ; Liu, HM; Yu, DQ; Ma, LY; Qin, SS or concate me.. Recommanded Product: 91-02-1

Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem