Tag: M.W=150-200

An article Metal-free multicomponent synthesis and in vitro antioxidant activity of indolylpyrazolopyrimidines WOS:000647318700001 published article about ANTIINFLAMMATORY ACTIVITY; FUNCTIONALIZATION; INDOLE; NANOCOMPOSITES; CYTOTOXICITY; INHIBITORS; EXTRACT; PDE1 in [Nadiveedhi, Maheshwara Reddy; Shaik, Mahammad Sadik; Krishnammagari, Suresh Kumar; Cirandur, Suresh Reddy] Sri Venkateswara Univ, Dept Chem, Tirupati 51750, Andhra Pradesh, India in 2021.0, Cited 50.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9. Application In Synthesis of 3,4-Dimethoxybenzaldehyde

Multisubstituted indolylpyrazolopyrimidines were synthesized in good yields with base promoted one-pot multicomponent system from aldehyde, ketone, and indolylpyrazolamine. Milder and cost-effective conditions are the highlights of the present protocol. Among the synthesized compounds (4a-j) 4b, 4c, 4e, and 4f have shown significant better in vitro antioxidant activity compared to standard ascorbic acid.

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Nadiveedhi, MR; Shaik, MS; Krishnammagari, SK; Cirandur, SR or concate me.. Application In Synthesis of 3,4-Dimethoxybenzaldehyde

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

An article Identification of 3-(trifluoromethyl)phenol as the malodorous compound in a pollution incident in the water supply in Catalonia (NE Spain) WOS:000468977800027 published article about ODOR THRESHOLD CONCENTRATIONS; TASTE; EVENTS; PERCEPTION; PANEL in [Quintana, Jordi; Hernandez, Alejandra; Devesa, Ricard; Rosa Boleda, Maria] Aigues Barcelona, Empresa Metropolitana Gestio Cicle Integral Aigua, Gen Batet 1-7, Barcelona 08028, Spain; [Ventura, Francesc] Spanish Council Sci Res IDAEA CSIC, Dept Environm Chem, Inst Environm Assessment & Water Res, Jordi Girona 18, Barcelona 08034, Spain in 2019, Cited 37. Category: indole-building-block. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9

A study of organic compounds that caused a serious taste and odor episode of water supply in two residential areas in Catalonia (N.E. Spain) was carried out. Sweet and paint/solvent odor were the main descriptors used by consumers. Some cases of sickness and nausea were also associated with drinking water consumption by the consumers. Closed-loop stripping analysis (CLSA) combined with sensory gas chromatography and gas chromatography mass spectrometry detection were used to study the problem. As a result, 3-(trifluoromethyl)phenol (CAS number 98-17-9) was for the first time identified as a responsible of an odor incident in drinking water. Concentration levels of this compound were up to 17,000ng/L in groundwater and up to 600ng/L in distributed water. Odor threshold in water for 3-(trifluoromethyl)phenol was determined as 13ng/L (45 degrees C).

Category: indole-building-block. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Quintana, J; Hernandez, A; Ventura, F; Devesa, R; Boleda, MR 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. COA of Formula: C9H10O3

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.

COA of Formula: C9H10O3. 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

COA of Formula: C9H7NO2. In 2019 J HETEROCYCLIC CHEM published article about TETRAPROPYLAMMONIUM BROMIDE; BIOLOGICAL EVALUATION; DERIVATIVES; CATALYST; WATER in [Marjani, Ahmad Poursattar; Khalafy, Jabbar; Farajollahi, Ayda] Urmia Univ, Dept Organ Chem, Fac Chem, Orumiyeh, Iran in 2019, Cited 41. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

In this research, in order to synthesize a series of ethyl 2-amino-4-benzoyl-5-oxo-5,6-dihydro-4H-pyrano[3,2-c]quinoline-3-carboxylates, a green and an efficient method is proposed through one-pot three-component reaction of substituted arylglyoxals, ethyl cyanoacetate, and 4-hydroxyquinolin-2(1H)-one in the presence of terapropylammonium bromide as a catalyst in good yields. All synthesized new substances were characterized by FTIR, H-1-NMR, and C-13-NMR spectral data and elemental analysis.

COA of Formula: C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Marjani, AP; Khalafy, J; Farajollahi, A 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

Application In Synthesis of 3-(Trifluoromethyl)phenol. Recently I am researching about NICKEL-CATALYZED AMINATION; ARYL 2-PYRIDYL ETHERS; ARENES; ACTIVATION; BORYLATION; OLEFINATION; ARYLATION; LIGAND; ALKYLATION; CLEAVAGE, Saw an article supported by the NSF of ChinaNational Natural Science Foundation of China (NSFC) [20502012, 21172111, 21672116]; NIH ((National Institute of General Medical Sciences))United States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute of General Medical Sciences (NIGMS) [5R01GM102265]; NATIONAL INSTITUTE OF GENERAL MEDICAL SCIENCESUnited States Department of Health & Human ServicesNational Institutes of Health (NIH) – USANIH National Institute of General Medical Sciences (NIGMS) [R01GM102265] Funding Source: NIH RePORTER. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Xu, JC; Chen, JJ; Gao, F; Xie, SG; Xu, XH; Jin, Z; Yu, JQ. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol

The use of a template as a linchpin motif in directed remote C-H functionalization is a versatile yet relatively underexplored strategy. We have developed a template-directed approach to realizing one-pot sequential palladium-catalyzed meta-selective C-H olefination of phenols, and nickel-catalyzed ipso-C-O activation and arylation. Thus, this bifunctional template converts phenols to synthetically useful 1,3-disubstituted arenes.

Application In Synthesis of 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Xu, JC; Chen, JJ; Gao, F; Xie, SG; Xu, XH; Jin, Z; Yu, JQ 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

Authors Nevesely, T; Daniliuc, CG; Gilmour, R in AMER CHEMICAL SOC published article about Z ISOMERIZATION; ATOM ECONOMY; IONIC LIQUID; COUMARINS; BIOSYNTHESIS; DERIVATIVES; ALKYNOATES in [Nevesely, Tomas; Daniliuc, Constantin G.; Gilmour, Ryan] Westfalische Wilhelms Univ Munster, Inst Organ Chem, Corrensstr 40, D-48149 Munster, Germany in 2019, Cited 38. HPLC of Formula: C7H5F3O. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9

An operationally simple one-pot protocol has been developed to enable the conversion of diversely substituted cinnamic acid derivatives into angularly-fused dihydrocoumarins (up to 94%). Inspired by coumarin biosynthesis, this reaction cascade harnesses photochemical E -> Z alkene isomerization enabled by energy transfer catalysis using inexpensive thioxanthen-9-one (TX) under irradiation at 402 nm. Subsequent lactonization generates the heterocyclic core prior to a second photosensitization event to induce a [2 + 2] cycloaddition, again mediated by TX. The tetracyclic products are generated efficiently, and proof of the structure was established by X-ray crystallography. Mechanistic investigations, including structural probes and NMR reaction monitoring, support the postulated order of events. The study underscores the synthetic value of inexpensive small-molecule organic photocatalysts in the generation of structural complexity via sequential pi-bond activation.

HPLC of Formula: C7H5F3O. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Nevesely, T; Daniliuc, CG; Gilmour, R 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

Verma, PK; Prasad, KS; Varghese, D; Geetharani, K in [Verma, Piyush Kumar; Prasad, K. Sujit; Varghese, Dominic; Geetharani, K.] Indian Inst Sci, Dept Inorgan & Phys Chem, Bangalore 560012, Karnataka, India published Cobalt(I)-Catalyzed Borylation of Unactivated Alkyl Bromides and Chlorides in 2020, Cited 61. Product Details of 98-17-9. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9.

A cobalt-complex-catalyzed borylation of a wide range of alkyl halides with a diboron reagent (B(2)pin(2) or B(2 )neop(2)) has been developed under mild reaction conditions, demonstrating the first cobalt-mediated cross-coupling with alkyl electrophiles. This protocol allows alkyl boronic esters to be accessed from alkyl halides, including alkyl chlorides, which were used rarely as coupling partners. Mechanistic studies reveal the possible involvement of an alkyl radical intermediate in this cobalt-mediated catalytic cycle.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Verma, PK; Prasad, KS; Varghese, D; Geetharani, K or concate me.. Product Details of 98-17-9

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

I found the field of Pharmacology & Pharmacy very interesting. Saw the article Hydroxyazole scaffold-based Plasmodium falciparum dihydroorotate dehydrogenase inhibitors: Synthesis, biological evaluation and X-ray structural studies published in 2019. Computed Properties of C7H5F3O, Reprint Addresses Lolli, ML (corresponding author), Univ Turin, Dept Sci & Drug Technol, Via Pietro Giuria 9, I-10125 Turin, Italy.. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol

Plasmodium falciparum dihydroorotate dehydrogenase (PJDHODH) has been clinically validated as a target for antimalarial drug discovery, as a triazolopyrimidine class inhibitor (DSM265) is currently undergoing clinical development. Here, we have identified new hydroxyazole scaffold-based PJDHODH inhibitors belonging to two different chemical series. The first series was designed by a scaffold hopping strategy that exploits the use of hydroxylated azoles. Within this series, the hydroxythiadiazole 3 was identified as the best selective PJDHODH inhibitor (IC50 12.0 mu M). The second series was designed by modulating four different positions of the hydroxypyrazole scaffold. In particular, hydroxypyrazoles 7e and 7f were shown to be active in the low mu M range (IC50 2.8 and 5.3 mu M, respectively). All three compounds, 3, 7e and 7f showed clear selectivity over human DHODH (IC50> 200 mu M), low cytotoxicity, and retained micromolar activity in P. falciparum-infected erythrocytes. The crystallographic structures of PJDHODH in complex with compounds 3 and 7e proved their binding mode, supplying essential data for future optimization of these scaffolds. (C) 2018 Elsevier Masson SAS. All rights reserved.

Computed Properties of C7H5F3O. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Pippione, AC; Sainas, S; Goyal, P; Fritzson, I; Cassiano, GC; Giraudo, A; Giorgis, M; Tavella, TA; Bagnati, R; Rolando, B; Caing-Carlsson, R; Costa, FTM; Andrade, CH; Al-Karadaghi, S; Boschi, D; Friemann, R; Lolli, ML 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 4-Hydroxyquinolin-2(1H)-one. Aly, AA; El-Sheref, EM; Bakheet, MEM; Mourad, MAE; Brase, S; Ibrahim, MAA; Nieger, M; Garvalov, BK; Dalby, KN; Kaoud, TS in [Aly, Ashraf A.; El-Sheref, Essmat M.; Bakheet, Momtaz E. M.; Ibrahim, Mahmoud A. A.] Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt; [Mourad, Mai A. E.] Port Said Univ, Med Chem Dept, Fac Pharm, Port Said 42526, Egypt; [Kaoud, Tamer S.] Menia Univ, Fac Pharm, Dept Med Chem, El Minia 61519, Egypt; [Brase, Stefan] Karlsruhe Inst Technol, Inst Toxikol & Genet, Hermann von Helmholts Pl 1,Campus Nord, D-76344 Eggenstein Leopoldsha, Germany; [Brase, Stefan] Inst Toxikol & Genet, Hermann von Helmholts Pl 1,Campus Nord, D-76344 Eggenstein Leopoldsha, Germany; [Nieger, Martin] Univ Helsinki, Dept Chem, POB 55, Helsinki 00014, Finland; [Garvalov, Boyan K.] Mannhe Univ Heidelberg, Ctr Biomed & Med Technol Mannheim, Med Fac, D-68167 Mannheim, Germany; [Dalby, Kevin N.; Kaoud, Tamer S.] Univ Texas Austin, Div Chem Biol & Med Chem, Austin, TX 78712 USA published 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 in 2019, Cited 57. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3.

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.

Quality Control of 4-Hydroxyquinolin-2(1H)-one. 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.

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

Category: indole-building-block. I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Synthesis of New Fused Heterocyclic 2-Quinolones and 3-Alkanonyl-4-Hydroxy-2-Quinolones published in 2019, Reprint Addresses Aly, AA (corresponding author), Menia Univ, Fac Sci, Chem Dept, El Minia 61519, Egypt.; Brase, S (corresponding author), Karlsruhe Inst Technol, Inst Organ Chem, D-76131 Karlsruhe, Germany.; Brase, S (corresponding author), Karlsruhe Inst Technol, Inst Toxicol & Genet, D-76344 Eggenstein Leopoldshafen, Germany.. The CAS is 86-95-3. Through research, I have a further understanding and discovery of 4-Hydroxyquinolin-2(1H)-one.

Herein, we report the synthesis of 5,12-dihydropyrazino[2,3-c:5,6-c ‘]difuro[2,3-c:4,5-c ‘]-diquinoline-6,14(5H,12H)diones, 2-(4-hydroxy-2-oxo-1,2-dihydroquinolin-3-yl)-1,4-diphenyl- butane-1,4-diones and 4-(benzo-[d]oxazol-2-yl)-3-hydroxy-1H-[4,5]oxazolo[3,2-a]pyridine-1-one. The new candidates were synthesized and identified by different spectroscopic techniques, and X-ray crystallography.

Category: indole-building-block. 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; Polamo, M; Nieger, M; Brown, AB 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