Tag: M.W=150-200

An article Formation of furo[3,2-c]quinolone-2-carbonitriles and 4-oxo-4,5-dihydrofuro[3,2-c]quinolone-2-carboxamides from reaction of quinoline-2,4-diones with 2-[bis(methylthio)methylene]malononitrile WOS:000513256900009 published article about DERIVATIVES; INHIBITORS; FUROQUINOLINE; ALKALOIDS; MODEL in [Aly, Ashraf A.; Mohamed, Asmaa H.] Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt; [Ishak, Esam] Al Azhar Univ, Fac Sci, Dept Chem, Assiut, Egypt; [Ishak, Esam] Jouf Univ, Coll Sci & Arts, Dept Chem, Alquurrayate, Saudi Arabia; [Shwaky, Ahmed M.] Umm Al Qura Univ, STU, Mecca, Saudi Arabia in 2020, Cited 31. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3. Computed Properties of C9H7NO2

Quinoline-2,4-diones reacted with 2-[bis(methylthio)methylene]malononitrile in DMF/Et3N to produce 3-(methylthio)-4-oxo-4,5-dihydrofuro[3,2-c]quinolone-2-carbonitriles and 3-(methylthio)-4-oxo-4,5-dihydrofuro[3,2-c]quinolone-2-carboxamides in state of 2-imino-substituted 4-(methylthio)-5,6-dihydro-2H-pyrano[3,2-c]quinolone-3-carbonitriles. The structures of all new products were proved using NMR, IR, and mass spectral data. The possible mechanism for the reaction is also discussed. Graphic abstract

About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Aly, AA; Ishak, E; Shwaky, AM; Mohamed, AH or concate me.. Computed Properties of C9H7NO2

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

In 2020 J PHARM HEALTH CARE published article about SEASONAL INFLUENZA; DURATION; OSELTAMIVIR; RISK in [Umemura, Takumi; Kawamura, Takato; Saito, Masayuki; Mizuno, Takahito; Ota, Aiko; Kozaki, Koji; Yamada, Tetsuya] Tosei Gen Hosp, Dept Pharm, 160 Nishi Oiwakecho, Seto, Aichi 4898642, Japan; [Umemura, Takumi; Mutoh, Yoshikazu; Ichihara, Toshihiko] Tosei Gen Hosp, Dept Infect & Prevent, 160 Nishi Oiwakecho, Seto, Aichi 4898642, Japan; [Ikeda, Yoshiaki] Kinjo Gakuin Univ, Coll Pharm, Moriyama Ku, 2-1723 Omori, Nagoya, Aichi 4638521, Japan in 2020, Cited 20. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Formula: C7H5F3O

Background Baloxavir marboxil (baloxavir) is a new anti-influenza virus agent that is comparable to oseltamivir phosphate (oseltamivir). Since the efficacy of baloxavir in preventing household transmission of influenza is not well established, we compared the secondary household influenza virus transmission rates between patients on baloxavir vs oseltamivir. Methods Between October 2018 and March 2019, we enrolled index patients (diagnosed with influenza and treated with baloxavir or oseltamivir) and household members. The secondary attack rate of household members was compared between index patients treated with baloxavir vs oseltamivir. Risk factors of household transmission were determined using multivariate logistic analyses. Results In total, 169 index patients with influenza type A were enrolled. The median age was 27.0 (interquartile range; 11-57) years. The number of index patients treated with baloxavir and oseltamivir was 49 and 120, respectively. The secondary attack rate was 9.0% (95% confidence interval [CI]: 4.6-15.6) in the baloxavir group and 13.5% (95% CI: 9.8-17.9) in the oseltamivir group. In the multivariate analysis, independent risk factors were 0-6 years of age (odds ratio [OR] 2.78, 95% CI: 1.33-5.82,p < 0.01) and not being on baloxavir treatment. (OR: 0.63, 95% CI: 0.30-1.32,p = 0.22). Conclusion The household secondary attack rate of influenza was comparable in patients treated with baloxavir vs oseltamivir. Therefore, baloxavir can be used as an alternative therapy to oseltamivir in reducing household transmission of influenza. Formula: C7H5F3O. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Umemura, T; Mutoh, Y; Kawamura, T; Saito, M; Mizuno, T; Ota, A; Kozaki, K; Yamada, T; Ikeda, Y; Ichihara, T or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Janetka, JW; Hopper, AT; Yang, ZP; Barks, J; Dhason, MS; Wang, QL; Sibley, LD in [Janetka, James W.] Washington Univ, Sch Med, Dept Biochem & Mol Biophys, St Louis, MO 63110 USA; [Barks, Jennifer; Dhason, Mary Savari; Wang, Qiuling; Sibley, L. David] Washington Univ, Sch Med, Dept Mol Microbiol, St Louis, MO 63110 USA; [Hopper, Allen T.; Yang, Ziping] Vyera Pharmaceut, New York, NY 10016 USA published Optimizing Pyrazolopyrimidine Inhibitors of Calcium Dependent Protein Kinase 1 for Treatment of Acute and Chronic Toxoplasmosis in 2020, Cited 56. Name: 3-(Trifluoromethyl)phenol. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9.

Calcium dependent protein kinase 1 (CDPK1) is an essential Ser/Thr kinase that controls invasion and egress by the protozoan parasite Toxoplasma gondii. The Gly gatekeeper of CDPK1 makes it exquisitely sensitive to inhibition by small molecule 1H-pyrazolo[3,4-d]pyrimidine-4-amine (PP) compounds that are bulky ATP mimetics. Here we rationally designed, synthesized, and tested a series of novel PP analogs that were evaluated for inhibition of CDPK1 enzyme activity in vitro and parasite growth in cell culture. Optimal substitution on the PP scaffold included 2-pyridyl ethers directed into the hydrophobic pocket and small carbocyclic rings accessing the ribose-binding pocket. Further optimization of the series led to identification of the lead compound 3a that displayed excellent potency, selectivity, safety profile, and efficacy in vivo. The results of these studies provide a foundation for further work to optimize CDPK1 inhibitors for the treatment of acute and chronic toxoplasmosis.

Name: 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Janetka, JW; Hopper, AT; Yang, ZP; Barks, J; Dhason, MS; Wang, QL; Sibley, LD or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Safety of 4-Hydroxyquinolin-2(1H)-one. Authors Aly, AA; Hassan, AA; Mohamed, NK; Abd El-Haleem, LE; Brase, S in SAGE PUBLICATIONS LTD published article about in [Aly, Ashraf A.; Hassan, Alaa A.; Mohamed, Nasr K.; Abd El-Haleem, Lamiaa E.] Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt; [Brase, Stefan] Karlsruhe Inst Technol, Inst Biol & Chem Syst Funct Mol Syst IBCS FMS, Eggenstein Leopoldshafen, Germany in 2020, Cited 13. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3

A novel series of 7,8-dichlorobenzofuro[3,2-c]quinoline-6,9,10(5H)-triones was obtained regioselectively in good yields. The products were formed by the reactions of the 4-hydroxy-2(1H)-quinolinones with 3,4,5,6-tetrachloro-1,2-benzoquinone in tetrahydrofuran as the solvent. Infrared, nuclear magnetic resonance (two-dimensional nuclear magnetic resonance), mass spectra and elemental analysis were used to elucidate the structures of new compounds.

Safety of 4-Hydroxyquinolin-2(1H)-one. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Aly, AA; Hassan, AA; Mohamed, NK; Abd El-Haleem, LE; Brase, S or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Quality Control of 3-(Trifluoromethyl)phenol. Authors Ning, L; Wang, SM; Du, L; Guo, BY; Zhang, JJ; Lu, HZ; Dong, YH in ROYAL SOC CHEMISTRY published article about in [Ning, Lei; Wang, Simin; Guo, Bingyi; Zhang, Jianjun; Lu, Huizhe; Dong, Yanhong] China Agr Univ, Dept Chem, Beijing 100193, Peoples R China; [Ning, Lei; Wang, Simin; Guo, Bingyi; Zhang, Jianjun; Lu, Huizhe; Dong, Yanhong] China Agr Univ, Innovat Ctr Pesticide Res, Beijing 100193, Peoples R China; [Du, Lin] China Agr Univ, Coll Agron & Biotechnol, Beijing 100193, Peoples R China in 2021, Cited 41. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9

A series of azamacrolides containing the carbamate or urea moiety were synthesized and evaluated for their fungicidal activities against several agriculturally important pathogens. In addition, they were investigated for their ability to inhibit quorum sensing in Agrobacterium tumefaciens. The results showed that most of the derivatives had moderate to high fungicidal activities against the tested fungi, especially towards Sclerotinia sclerotiorum. Additionally, D16-19 could be used as a potential broad-spectrum fungicide while D16-4 exhibited a fungicidal activity (EC50 = 1.87 mg L-1) similar to that of carbendazim (EC50 = 1.34 mg L-1) against S. sclerotiorum. The three-dimensional Quantitative Structure-Activity Relationship (3D-QSAR) models were also established based on the experimental results and they would provide valuable information for further optimization. Moreover, D16-17 not only showed a better fungicidal activity against S. sclerotiorum but also had the highest ability to inhibit quorum sensing. These findings suggested that some azamacrolide compounds hold potential for the development of novel fungicides or inhibitors of quorum sensing.

Quality Control of 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Ning, L; Wang, SM; Du, L; Guo, BY; Zhang, JJ; Lu, HZ; Dong, YH or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Coleman, MA; Burchill, L; Sumby, CJ; George, JH in [Coleman, Matthew A.; Burchill, Laura; Sumby, Christopher J.; George, Jonathan H.] Univ Adelaide, Dept Chem, Adelaide, SA 5005, Australia published Biomimetic Synthesis Enables the Structure Revision of Furoerioaustralasine in 2019, Cited 12. Name: 4-Hydroxyquinolin-2(1H)-one. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

The structure of furoerioaustralasine, a unique Australian alkaloid, has been revised based on a concise, biomimetic synthesis. The key step is a stereospecific, intramolecular ring opening of an epoxide to form a central dihydrofuran fused to a quinoline ring system.

Name: 4-Hydroxyquinolin-2(1H)-one. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Coleman, MA; Burchill, L; Sumby, CJ; George, JH or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Computed Properties of C7H5F3O. Recently I am researching about RESISTANCE PROTEIN BCRP/ABCG2; MULTIDRUG-RESISTANCE; SELECTIVE INHIBITORS; DRUG-RESISTANCE; HIGHLY POTENT; CANCER; TRANSPORTER; BCRP; EXPRESSION; CELLS, Saw an article supported by the . Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Krapf, MK; Gallus, J; Spindler, A; Wiese, M. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol

Multidrug resistance (MDR) is a major obstacle for effective chemotherapeutic treatment of cancer frequently leading to failure of the therapy. MDR is often associated with the overexpression of ABC transport proteins like ABCB1 or ABCG2 which efflux harmful substances out of cells at the cost of ATP hydrolysis. One way to overcome MDR is to apply potent inhibitors of ABC transporters to restore the sensitivity of the cells toward cytostatic agents. This study focusses on the synthesis and evaluation of novel 2,4-disubstituted quinazoline derivatives regarding the structure-activity-relationship (SAR), their ability to reverse MDR and their mode of interaction with ABCG2. Hence, the inhibitory potency and selectivity toward ABCG2 was determined. Moreover, the intrinsic cytotoxicity and the reversal of MDR were investigated. Interaction type studies with the substrate Hoechst 33342 and conformational analyses of ABCG2 with 5D3 monoclonal antibody were performed for a better understanding of the underlying mechanisms. In our study we could further enhance the inhibitory effect against ABCG2 (compound 31, IC50: 55 nM) and identify the structural features that are crucial for inhibitory potency, the impact on transport activity and binding to the protein. (C) 2018 Elsevier Masson SAS. All rights reserved,

Computed Properties of C7H5F3O. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Krapf, MK; Gallus, J; Spindler, A; Wiese, M or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Recently I am researching about RESISTANT STAPHYLOCOCCUS-AUREUS; DIVISION PROTEIN FTSZ; IN-VITRO; INHIBITORS; CYTOKINESIS; BACTERIA; INSIGHTS, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81973179, 81673284]; Key Project of Major Project of New and Old Kinetic Energy Conversion of Shandong Province. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Song, D; Zhang, N; Zhang, PP; Zhang, N; Chen, WJ; Zhang, L; Guo, T; Gu, XT; Ma, ST. The CAS is 120-14-9. Through research, I have a further understanding and discovery of 3,4-Dimethoxybenzaldehyde. Safety of 3,4-Dimethoxybenzaldehyde

With the increasing incidence of antibiotic resistance, new antibacterial agents having novel mechanisms of action hence are in an urgent need to combat infectious diseases caused by multidrug-resistant (MDR) pathogens. Four novel series of substituted 9-arylalkyl-10-methylacridinium derivatives as FtsZ inhibitors were designed, synthesized and evaluated for their antibacterial activities against various Gram-positive and Gram-negative bacteria. The results demonstrated that they exhibited broad-spectrum activities with substantial efficacy against MRSA and VRE, which were superior or comparable to the berberine, sanguinarine, linezolid, ciprofloxacin and vancomycin. In particular, the most promising compound 15f showed rapid bactericidal properties, which avoid the emergence of drug resistance. However, 15f showed no inhibitory effect on Gram-negative bacteria but biofilm formation study gave possible answers. Further target identification and mechanistic studies revealed that 15f functioned as an effective FtsZ inhibitor to alter the dynamics of FtsZ self-polymerization, which resulted in termination of the cell division and caused cell death. Further cytotoxicity and animal studies demonstrated that 15f not only displayed efficacy in a murine model of bacteremia in vivo, but also no significant hemolysis to mammalian cells. Overall, this compound with novel skeleton could serve as an antibacterial lead of FtsZ inhibitor for further evaluation of drug-likeness. (C) 2021 Elsevier Masson SAS. All rights reserved.

Safety of 3,4-Dimethoxybenzaldehyde. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Song, D; Zhang, N; Zhang, PP; Zhang, N; Chen, WJ; Zhang, L; Guo, T; Gu, XT; Ma, ST or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Formula: C9H7NO2. I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Design, synthesis and biological evaluation of fused naphthofuro[3,2-c]quinoline-6,7,12-triones and pyrano[3,2-c]quinoline-6,7,8,13-tetraones derivatives as ERK inhibitors with efficacy in BRAF-mutant melanoma published in 2019, Reprint Addresses Aly, AA (corresponding author), Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt.; Kaoud, TS (corresponding author), Univ Texas Austin, Div Chem Biol & Med Chem, Austin, TX 78712 USA.. The CAS is 86-95-3. Through research, I have a further understanding and discovery of 4-Hydroxyquinolin-2(1H)-one.

Approximately 60% of human cancers exhibit enhanced activity of ERK1 and ERK2, reflecting their multiple roles in tumor initiation and progression. Acquired drug resistance, especially mechanisms associated with the reactivation of the MAPK (RAF/MEK/ERK) pathway represent a major challenge to current treatments of melanoma and several other cancers. Recently, targeting ERK has evolved as a potentially attractive strategy to overcome this resistance. Herein, we report the design and synthesis of novel series of fused naphthofuro[3,2-c] quinoline-6,7,12-triones 3a-f and pyrano[3,2-c]quinoline-6,7,8,13-tetraones 5a,b and 6, as potential ERK inhibitors. New inhibitors were synthesized and identified by different spectroscopic techniques and X-ray crystallography. They were evaluated for their ability to inhibit ERK1/2 in an in vitro radioactive kinase assay. 3b and 6 inhibited ERK1 with IC50s of 0.5 and 0.19 mu M, and inhibited ERK2 with IC50s of 0.6 and 0.16 mu M respectively. Kinetic mechanism studies revealed that the inhibitors are ATP-competitive inhibitors where 6 inhibited ERK2 with a K-i of 0.09 mu M. Six of the new inhibitors were tested for their in vitro anticancer activity against the NCI-60 panel of tumor cell lines. Compound 3b and 6 were the most potent against most of the human tumor cell lines tested. Moreover, 3b and 6 inhibited the proliferation of the BRAF mutant A375 melanoma cells with IC50s of 3.7 and 0.13 mu M, respectively. In addition, they suppressed anchorage-dependent colony formation. Treatment of the A375 cell line with 3b and 6 inhibited the phosphorylation of ERK substrates p-90RSK and ELK-1 and induced apoptosis in a dose dependent manner. Finally, a molecular docking study showed the potential binding mode of 3b and 6 within the ATP catalytic binding site of ERK2.

About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Aly, AA; El-Sheref, EM; Bakheet, MEM; Mourad, MAE; Brase, S; Ibrahim, MAA; Nieger, M; Garvalov, BK; Dalby, KN; Kaoud, TS or concate me.. Formula: C9H7NO2

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles

Recommanded Product: 3,4-Dimethoxybenzaldehyde. Authors Liu, Y; Zhang, Y; Huang, QW; Gou, CA; Li, QZ; Dai, QS; Leng, HJ; Li, JL in WILEY-V C H VERLAG GMBH published article about in [Liu, Yue; Zhang, Ying; Huang, Qian-Wei; Gou, Chuan; Li, Qing-Zhu; Dai, Qing-Song; Leng, Hai-Jun; Li, Jun-Long] Chengdu Univ, Sichuan Ind Inst Antibiot, Sch Pharm, Antibiot Res & Reevaluat Key Lab Sichuan Prov, Chengdu 610106, Peoples R China in 2021.0, Cited 77.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

Asymmetric construction of pharmacologically interesting tetrahydrofuranyl spirooxindole frameworks has been achieved through organocatalytic [3+2] annulations of the readily available 3-hydroxyoxindoles and pyrrolidone-derived cyclic ketolactams. A variety of chiral spiro tetrahydrofuranyl products, which contain four contiguous stereocenters including two tetrasubstituted carbon centers, have been rapidly synthesized with remarkable results (up to 99% yield, >95:5 dr, and 99:1 er). Synthetic derivatization of the hemiketal moiety enables the installation of various halogen atoms into the structurally complex molecules in a stereospecific manner. Preliminary screening of anticancer bioactivity was performed, and 4 w showed obvious inhibitory capacity to the proliferation on a panel of cancer cell lines.

Recommanded Product: 3,4-Dimethoxybenzaldehyde. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Liu, Y; Zhang, Y; Huang, QW; Gou, CA; Li, QZ; Dai, QS; Leng, HJ; Li, JL or concate me.

Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles