Category: 500-22-1

Application In Synthesis of 3-Pyridinecarboxaldehyde. Authors Gein, VL; Rubtsova, DD; Bobyleva, AA; Yankin, AN in MAIK NAUKA/INTERPERIODICA/SPRINGER published article about in [Gein, V. L.; Rubtsova, D. D.; Bobyleva, A. A.] Perm State Pharmaceut Acad, Perm 614990, Russia; [Yankin, A. N.] Natl Res Univ ITMO, St Petersburg 197101, Russia in 2020.0, Cited 5.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

5-Aryl(heteryl)-1-hydroxyethyl-4-(furyl-2-carbonyl)-3-hydroxy-3-pyrroline-2-ones were synthesized via reactions of methyl ester of furyl-2-carbonylpyruvic acid with a mixture of aromatic or heterocyclic aldehyde and ethanolamine in dioxane. Antibacterial and antifungal activities of the synthesized compounds was studied.

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

An article Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators WOS:000573916100021 published article about CELL-DEATH; ENDOPLASMIC-RETICULUM; DUAL ROLES; APOPTOSIS; EXPRESSION; STRESS; UBIQUITINATION; METABOLISM; ACTIVATION; INDUCTION in [Li, Baicun; Yao, Jie; Guo, Kaiqiang; He, Fengming; Chen, Kun; Lin, Zongxin; Liu, Shunzhi; Huang, Jiangang; Wu, Qiaoqiong; Fang, Meijuan; Zeng, Jinzhang; Wu, Zhen] Xiamen Univ, Sch Pharmaceut Sci, Fujian Prov Key Lab Innovat Drug Target Res, Xiamen 361102, Peoples R China; [Li, Baicun; Yao, Jie; Guo, Kaiqiang; He, Fengming; Chen, Kun; Lin, Zongxin; Liu, Shunzhi; Huang, Jiangang; Wu, Qiaoqiong; Fang, Meijuan; Zeng, Jinzhang; Wu, Zhen] Xiamen Univ, Sch Pharmaceut Sci, State Key Lab Cellular Stress Biol, Xiamen 361102, Peoples R China; [Li, Baicun] Chinese Acad Med Sci, Inst Basic Med Sci, Dept Physiol, State Key Lab Med Mol Biol, Beijing 100005, Peoples R China; [Li, Baicun] Peking Union Med Coll, Sch Basic Med, Beijing 100005, Peoples R China in 2020.0, Cited 74.0. Recommanded Product: 500-22-1. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

Nur77 is a potential target for the treatment of cancer such as HCC. Herein, we detailed the discovery of a novel series of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as potential Nur77 modulators. The studies of antiproliferative activity and Nur77-binding affinity of target compounds resulted in the discovery of a lead candidate (10g), which was a good Nur77 binder (K-D = 3.58 +/- 0.16 mu M) with a broad-spectrum antiproliferative activity against all tested hepatoma cells (IC50 < 2.0 mu M) and was low toxic to normal LO2 cells. 10g could up-regulate Nur77 expression and mediate sub-cellular localization of Nur77 to induce apoptosis in hepatocellular carcinoma cell lines, which relied on 10g inducing Nur77-dependent autophagy and endoplasmic reticulum stress as the upstream of apoptosis. Moreover, the in vivo assays verified that 10g significantly inhibited xenograft tumor growth. These results indicate that 10g has the potential to be developed as a novel Nur77-targeting anti-hepatoma drug. (C) 2020 Elsevier Masson SAS. All rights reserved. Recommanded Product: 500-22-1. About 3-Pyridinecarboxaldehyde, If you have any questions, you can contact Li, BC; Yao, J; Guo, KQ; He, FM; Chen, K; Lin, ZX; Liu, SZ; Huang, JG; Wu, QQ; Fang, MJ; Zeng, JZ; Wu, Z or concate me.

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

An article Structure-based design and synthesis of novel furan-diketopiperazine-type derivatives as potent microtubule inhibitors for treating cancer WOS:000526982300002 published article about IN-VITRO; AGENT; MECHANISM; INSIGHTS in [Ding, Zhongpeng; Li, Feifei; Zhong, Changjiang; Liu, Yuqian; Zhao, Jianchun; Li, Wenbao] Ocean Univ China, Sch Med & Pharm, Qingdao 266003, Peoples R China; [Li, Wenbao] Qingdao Natl Lab Marine Sci & Technol, Innovat Ctr Marine Drug Screening & Evaluat, Qingdao 266071, Peoples R China; [Li, Feng] Weifang Univ Sci & Technol, Shandong Peninsula Engn Res Ctr Comprehens Brine, Weifang 262700, Shandong, Peoples R China; [Wang, Shixiao; Zhao, Jianchun; Li, Wenbao] Marine Biomed Res Inst Qingdao, Qingdao 266071, Peoples R China in 2020.0, Cited 24.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Recommanded Product: 3-Pyridinecarboxaldehyde

Plinabulin, a synthetic analog of the marine natural product diketopiperazine phenylahistin, displayed depolymerization effects on microtubules and targeted the colchicine site, which has been moved into phase III clinical trials for the treatment of non-small cell lung cancer (NSCLC) and the prevention of chemotherapy-induced neutropenia (CIN). To develop more potent anti-microtubule and cytotoxic derivatives, the co-crystal complexes of plinabulin derivatives were summarized and analyzed. We performed further modifications of the tert-butyl moiety or C-ring of imidazole-type derivatives to build a library of molecules through the introduction of different groups for novel skeletons. Our structure-activity relationship study indicated that compounds 17o (IC50 = 14.0 nM, NCI-H460) and 17p (IC50 = 2.9 nM, NCI-H460) with furan groups exhibited potent cytotoxic activities at the nanomolar level against various human cancer cell lines. In particular, the 5-methyl or methoxymethyl substituent of furan group could replace the alkyl group of imidazole at the 5-position to maintain cytotoxic activity, contradicting previous reports that the tert-butyl moiety at the 5-position of imidazole was essential for the activity of such compounds. Immunofluorescence assay indicated that compounds 17o and 17p could efficiently inhibit microtubule polymerization. Overall, the novel furan-diketopiperazine-type derivatives could be considered as a potential scaffold for the development of anti-cancer drugs.

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

In 2019.0 CHEM-EUR J published article about SITU CLICK-CHEMISTRY; BENZOTRIAZOLE-ASSISTED SYNTHESIS; PLASMINOGEN-ACTIVATOR SYSTEM; IN-SITU; MULTICOMPONENT REACTIONS; COMBINATORIAL CHEMISTRY; GUIDED SYNTHESIS; PROTEASE; ACETYLCHOLINESTERASE; AMINOALKYLATION in [Gladysz, Rafaela; Vrijdag, Johannes; Van Rompaey, Dries; Augustyns, Koen; De Winter, Hans; Van der Veken, Pieter] Univ Antwerp, Dept Pharmaceut Sci, Lab Med Chem UAMC, Univ Pl 1, B-2610 Antwerp, Belgium; [Vrijdag, Johannes; Lambeir, Anne-Marie] Univ Antwerp, Dept Pharmaceut Sci, Lab Med Biochem, Univ Pl 1, B-2610 Antwerp, Belgium in 2019.0, Cited 72.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Computed Properties of C6H5NO

Target-guided synthesis (TGS) has emerged as a promising strategy in drug discovery. Although reported examples of TGS generally involve two-component reactions, there is a strong case for developing target-guided versions of three-component reactions (3CRs) because of their potential to deliver highly diversified druglike molecules. To this end, the Groebke-Blackburn-Bienayme reaction was selected as a model 3CR. We recently reported a series of druglike urokinase inhibitors, and these serve as reference compounds in the present study. Due to the limited number of literature reports on target-guided 3CRs, multiple experimental parameters were optimized here. Most challenging was the formation of imine intermediates under near-physiological conditions. This aspect was addressed by exploring chemical imine stabilization strategies. Notably, imines are also crucial intermediates of other 3CRs. Such systematic studies are strongly required for further development of the TGS domain but are largely absent in the literature. Hence, this work is intended as a reference for future multicomponent-based TGS studies.

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

In 2019.0 ANTI-CANCER AGENT ME published article about ACRIDINE-DERIVATIVES; ANTIOXIDANT; POTENT; AGENTS in [Kalirajan, R.; Gaurav, K.; Pandiselvi, A.; Gowramma, B.; Sankar, S.] Deemed Univ, Constituent Coll JSS Acad Higher Educ & Res, Dept Pharmaceut Chem, JSS Coll Pharm, Udhagamandalam 643001, Tamil Nadu, India in 2019.0, Cited 26.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Name: 3-Pyridinecarboxaldehyde

Background: 9-anilinoacridines are acting as DNA-intercalating agents which plays an important role as antitumor drugs, due to their anti-proliferative properties. Some anticancer agents contain 9-anilinoacridines such as amsacrine (m-AMSA), and nitracrine (Ledakrine) have been already developed. Methods: In this study, novel 9-anilinoacridines substituted with thiazines 4a-r were designed, synthesized, characterized by physical and spectral data and their cytotoxic activities against DLA cell lines were evaluated. Results: Among those compounds, 4b, c, e, g, i, j, k, m, o, p, q, r exhibited significant short term in vitro cytotoxic activity against Daltons lymphoma ascites (DLA) cells with CTC50 value of 0.18 to 0.31 mu M. The compounds 4b, c, e, g, y j, k, m, o, p, q, r are also exhibited significant long term in vitro anti-tumour activity against human tumor cell lines, HEp-2 (laryngeal epithelial carcinoma) by Sulforhodamine B assay with CTC50 value of 0.20 to 0.39 mu M. The compounds 4b, i, j exhibited significant in vivo antitumor activity with % Increase in Life Span (ILS) 48-82%. Conclusion: Results obtained in this study clearly demonstrated that many of the thiazine substituted 9-anilinoacridines exert interesting anti-tumour activity. The compounds 4b, i, j have significant anti-tumour activity and useful drugs after further refinement. The above derivatives will encourage to design future antitumor agents with high therapeutic potentials.

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Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem

In 2020.0 ORG BIOMOL CHEM published article about DONOR-ACCEPTOR CYCLOPROPANES; ENANTIOSELECTIVE SYNTHESIS; ALLYLIC ALCOHOLS; CHEMISTRY; FLUORINE; ACID; DERIVATIVES; OLEFINS; ROUTE; ZINC in [Kazia, Armands; Melngaile, Renate; Mishnev, Anatoly; Veliks, Janis] Latvian Inst Organ Synth, Aizkraukles 21, LV-1006 Riga, Latvia in 2020.0, Cited 44.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Formula: C6H5NO

Johnson-Corey-Chaykovsky fluorocyclopropanation of double activated alkenes utilizing S-monofluoromethyl-S-phenyl-2,3,4,5-tetramethylphenylsulfonium tetrafluoroborate is an efficient approach to obtain a range of monofluorocyclopropane derivatives. So far, fluoromethylsulfonium salts have displayed the broadest scope for direct fluoromethylene transfer. In contrast to more commonly used fluorohalomethanes or freon derivatives, diarylfluoromethylsulfonium salts are bench stable, easy-to use reagents useful for the direct transfer of a fluoromethylene group to alkenes giving access to the challenging products – fluorocyclopropane derivatives. Interplay between the reactivity of the starting materials and stability of the fluorocyclopropanes formed determines the outcome of the process.

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

An article Structure-Activity Relationships of Cinnamate Ester Analogues as Potent Antiprotozoal Agents WOS:000495757700001 published article about CAFFEIC ACID-ESTERS; ANTILEISHMANIAL ACTIVITIES; TRYPANOSOMA-BRUCEI; PHENOLIC-COMPOUNDS; IN-VITRO; ASSAY; ESTERIFICATION; RHODESIENSE; SENSITIVITY; CATALYSTS in [Bernal, Freddy A.; Schmidt, Thomas J.] Westfalische Wilhelms Univ Munster, IPBP, Corrensstr 48, D-48149 Munster, Germany; [Kaiser, Marcel] Swiss Trop & Publ Hlth Inst Swiss TPH, Socinstr 57, CH-4051 Basel, Switzerland; [Kaiser, Marcel] Univ Basel, Peterspl 1, CH-4003 Basel, Switzerland; [Wuensch, Bernhard] Westfalische Wilhelms Univ Munster, Inst Pharmazeut & Med Chem, Corrensstr 48, D-8149 Munster, Germany in 2020.0, Cited 51.0. Recommanded Product: 3-Pyridinecarboxaldehyde. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1

Protozoal infections are still a global health problem, threatening the lives of millions of people around the world, mainly in impoverished tropical and sub-tropical regions. Thus, in view of the lack of efficient therapies and increasing resistances against existing drugs, this study describes the antiprotozoal potential of synthetic cinnamate ester analogues and their structure-activity relationships. In general, Leishmania donovani and Trypanosoma brucei were quite susceptible to the compounds in a structure-dependent manner. Detailed analysis revealed a key role of the substitution pattern on the aromatic ring and a marked effect of the side chain on the activity against these two parasites. The high antileishmanial potency and remarkable selectivity of the nitro-aromatic derivatives suggested them as promising candidates for further studies. On the other hand, the high in vitro potency of catechol-type compounds against T. brucei could not be extrapolated to an in vivo mouse model.

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

Category: pyridine-derivatives. I found the field of Pharmacology & Pharmacy; Chemistry very interesting. Saw the article Synthesis of novel 4,5-dihydropyrrolo[1,2-a]quinoxalines, pyrrolo[1,2-a]quinoxalin]-2-ones and their antituberculosis and anticancer activity published in 2020.0, Reprint Addresses Rode, HB (corresponding author), CSIR Indian Inst Chem Technol, Dept Organ Synth & Proc Chem, Hyderabad 500007, Telangana, India.. The CAS is 500-22-1. Through research, I have a further understanding and discovery of 3-Pyridinecarboxaldehyde.

A facile strategy was developed for the synthesis of biologically important 4,5-dihydropyrrolo[1,2-a]quinoxalines and pyrrolo[1,2-a]quinoxalin]-2-ones by treating 2-(1H-pyrrol-1-yl)anilines with imidazo[1,2-a]pyridine-3-carbaldehyde or isatin, using amidosulfonic acid (NH3SO3) as a solid catalyst in water at room temperature. The protocol has been extended to electrophile ninhydrin. The catalyst could be recycled for six times without the loss of activity. The compounds were evaluated for their antituberculosis, antibacterial, and anticancer activities. It is worth noting that compounds3dand3edemonstrated a minimum inhibitory concentration value of 6.25 mu M againstMycobacterium tuberculosisH37Rv, whereas compounds3d,3g,5d,5e, and5ishowed a remarkable inhibition of A549, DU145, HeLa, HepG2, MCF-7, and B16-F10 cell lines, respectively.Staphylococcus aureuswas inhibited by compounds5b,5e,5d,5g, and5lat 32 mu g/ml.

Category: pyridine-derivatives. Bye, fridends, I hope you can learn more about C6H5NO, If you have any questions, you can browse other blog as well. See you lster.

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

An article Exploiting the Nucleophilicity of the Nitrogen Atom of Imidazoles: One-Pot Three-Component Synthesis of Imidazo-Pyrazines WOS:000470996600117 published article about MULTICOMPONENT REACTIONS; CHEMISTRY; ISOCYANIDES; DISCOVERY; MECHANISM; REVEALS; BIOLOGY; IMINES in [Galli, Ubaldina; Hysenlika, Rejdia; Del Grosso, Erika; Tron, Gian Cesare] Univ Piemonte Orientale, Dipartimento Sci Farmaco, I-28100 Novara, Italy; [Meneghetti, Fiorella] Univ Milan, Dipartimento Sci Farmaceut, I-20133 Milan, Italy; [Pelliccia, Sveva; Novellino, Ettore; Giustiniano, Mariateresa] Univ Napoli Federico II, Dipartimento Farm, I-80131 Naples, Italy in 2019.0, Cited 38.0. The Name is 3-Pyridinecarboxaldehyde. Through research, I have a further understanding and discovery of 500-22-1. Recommanded Product: 500-22-1

A novel one-pot multicomponent reaction to synthesize substituted imidazopyrazines is described. In brief, 1H-(imidazol-5-yl)-N-substituted methanamines react with aldehydes and isocyanides in methanol at room temperature to give imidazopyrazine derivatives in excellent yields. The imidazole nitrogen atom was able to intercept the nascent nitrilium ion, channeling the reaction toward to the sole formation of imidazopyrazines, suppressing the competitive formation of other possible side products deriving from the reaction with the high-energy nitrilium ion. The number of examples and the variability of the nature of isocyanides, aldehydes, and amine components herein employed, witness the robustness of this novel methodology.

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

Application In Synthesis of 3-Pyridinecarboxaldehyde. I found the field of Biochemistry & Molecular Biology very interesting. Saw the article N-Benzyl Derivatives of Long-Chained 4-Amino-7-chloro-quionolines as Inhibitors of Pyocyanin Production in Pseudomonas aeruginosa published in 2019.0, Reprint Addresses Opsenica, DM; Senerovic, L (corresponding author), Univ Belgrade, Inst Mol Genet & Genet Engn, Vojvode Stepe 444a, Belgrade 11010, Serbia.; Opsenica, DM (corresponding author), Univ Belgrade, ICTM, Ctr Excellence Environm Chem & Engn, Belgrade 11000, Serbia.. The CAS is 500-22-1. Through research, I have a further understanding and discovery of 3-Pyridinecarboxaldehyde.

Pseudomonas aeruginosa is a leading cause of nosocomial infections that are becoming increasingly difficult to treat due to the occurrence of antibiotic resistant strains. Since P. aeruginosa virulence is controlled through quorum sensing, small molecule treatments inhibiting quorum sensing signaling pathways provide a promising therapeutic option. Consequently, we synthesized a series of N-octaneamino-4-aminoquinoline derivatives to optimize this chemotype’s antivirulence activity against P. aeruginosa via inhibition of pyocyanin production. The most potent derivative, which possesses a benzofuran substituent, provided effective inhibition of pyocyanin production (IC50 = 12 mu M), biofilm formation (BFIC50 = 50 mu M), and motility. Experimentally, the compound’s activity is achieved through competitive inhibition of PqsR, and structure-activity data were rationalized using molecular docking studies.

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