Month: October 2021

An article Polyfluoroaromatic stavudine (d4T) ProTides exhibit enhanced anti-HIV activity WOS:000497964000013 published article about DERIVATIVES; NUCLEOSIDE; PHOSPHATE in [Kandil, Sahar; Chapman, Fiona M.; Westwell, Andrew D.; McGuigan, Christopher] Cardiff Univ, Sch Pharm & Pharmaceut Sci, King Edward VII Ave, Cardiff CF10 3NB, S Glam, Wales; [Pannecouque, Christophe] Katholieke Univ Leuven, Rega Inst Med Res, Lab Virol & Chemotherapy, Minderbroedersstr 10, B-3000 Leuven, Belgium in 2019, Cited 17. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. HPLC of Formula: C7H5F3O

Human Immunodeficiency Virus (HIV) damages the immune system and leads to the life-threatening acquired immunodeficiency syndrome (AIDS). Despite the advances in the field of antiretroviral treatment, HIV remains a major public health challenge. Nucleosides represent a prominent chemotherapeutic class for treating viruses, however their cellular uptake, kinase-mediated activation and catabolism are limiting factors. Herein, we report the synthesis and in vitro evaluation of stavudine (d4T) ProTides containing polyfluorinated aryl groups against two strains; HIV-1 (IIIB) and HIV-2 (ROD). ProTide 5d containing a meta-substituted pentafluorosulfanyl (3-SF5) aryl group showed superior antiviral activity over the parent d4T and the nonfluorinated analogue 5a. ProTide 5d has low nano-molar antiviral activity; (IC50=30 nM, HIV-1) and (IC50=36 nM, HIV-2) which is over tenfold more potent than d4T. Interestingly, ProTide 5d showed a significantly high selectivity indices with SI=1753 (HIV-1) and 1461 (HIV-2) which is more than twice that of the d4T. All ProTides were screened in wild type as well as thymidine kinase deficient (TK-) cells. Enzymatic activation of ProTide 5d using carboxypeptidase Y enzyme and monitored using both P-31 and F-19 NMR is presented.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Kandil, S; Pannecouque, C; Chapman, FM; Westwell, AD; McGuigan, C or concate me.. HPLC of Formula: C7H5F3O

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: C7H8O. Wu, JQ; Hua, WM; Yue, YH; Gao, Z in [Wu, Jiequn; Hua, Weiming; Yue, Yinghong; Gao, Zi] Fudan Univ, Shanghai Key Lab Mol Catalysis & Innovat Mat, Dept Chem, Shanghai 200438, Peoples R China published A Highly Efficient Bifunctional Catalyst CoOx/tri-g-C(3)N(4)for One-Pot Aerobic Oxidation-Knoevenagel Condensation Reaction in 2020.0, Cited 43.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6.

A highly efficient bifunctional catalyst of an s-triazine-based carbon-nitride-supported cobalt oxide is developed for the aerobic oxidation-Knoevenagel condensation tandem reaction of benzyl alcohol and malononitrile, whereby 96.4% benzyl alcohol conversion with nearly 100% selectivity towards benzylmalononitrile can be obtained in 6 h at 80 degrees C. The excellent catalytic performance derives from the high basicity of carbon nitride and strong redox ability of Co species induced by carbon nitride. The catalyst is also quite stable and can be reused without any regeneration treatment, whose product yield is only an 11.5% reduction after four runs.

COA of Formula: C7H8O. About Benzyl Alcohol, If you have any questions, you can contact Wu, JQ; Hua, WM; Yue, YH; Gao, Z 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

Sousa, SCA; Realista, S; Royo, B in [Sousa, Sara C. A.; Realista, Sara; Royo, Beatriz] Univ Nova Lisboa, Inst Tecnol Quim & Biol Antonio Xavier, ITQB NOVA, Oeiras, Portugal published Bench-Stable Manganese NHC Complexes for the Selective Reduction of Esters to Alcohols with Silanes in 2020.0, Cited 58.0. Name: Benzyl Alcohol. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6.

Selective reduction of esters to alcohols was accomplished through Mn(I)-mediated hydrosilylation reaction. The manganese tricarbonyl complex [Mn(bis-NHC)(CO)(3)Br] resulted an active pre-catalyst for the reduction of a variety of esters using phenylsilane and the cheap and readily available polymethylhydrosiloxane. Anin situexamination of the catalytic reaction using(55)Mn NMR spectroscopy allowed us to detect the formation of Mn(I) intermediate active species.

Name: Benzyl Alcohol. About Benzyl Alcohol, If you have any questions, you can contact Sousa, SCA; Realista, S; Royo, B 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: C9H10O3. In 2021.0 CHEM PAP published article about CRYSTAL-STRUCTURE; ORGANIC-CRYSTAL; Z-SCAN; GROWTH; ABSORPTION; STABILIZATION; MOLECULES in [Raghavendra, S.] Adichunchanagiri Inst Technol, Dept Engn Phys, Chikmagaluru 577102, India; [Kumar, C. S. Chidan] Visvesvaraya Technol Univ, Vidya Vikas Inst Engn & Technol, Dept Chem, Mysuru 570028, Karnataka, India; [Kumar, D. J. Madhu] Ramaiah Univ Appl Sci, Fac Pharm, Bengaluru 560054, India; [Al-Ghorbani, Mohammed] Thamar Univ, Dept Chem, Coll Educ, Thamar, Yemen; [Alsalme, Ali] King Saud Univ, Dept Chem, Coll Sci, POB 2455, Riyadh 11451, Saudi Arabia; [Quah, C. K.] Univ Sains Malaysia, Xray Crystallog Unit, Sch Phys, Gelugor 11800, Penang, Malaysia; [Raghavendra, P. V.] SDM Coll Engn & Technol, Dept Phys, Dharwad 580002, Karnataka, India; [Serrao, Felcy Jyothi] Sahyadri Coll Engn & Management, Dept Engn Phys, Mangaluru 575007, India; [Dharmaprakash, S. M.] Mangalore Univ, Dept Studies Phys, Mangalagangothri 574199, India in 2021.0, Cited 52.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9.

Herein, we report the third-order nonlinear absorption and optical limiting property of fluorinated polymorphic nonlinear optical (NLO) material 1-(3,4-dimethoxyphenyl)-3-(4-fluorophenyl) prop-2-en-1-one (abbreviated as PDPFO) based on reverse saturable absorption. The FTIR studies of optically transparent PDPFO single crystals confirm the presence of various functional groups. PDPFO is optically transparent in the visible wavelength region. The open aperture Z-scan technique showed the intensity-dependent nonlinear absorption. A decrease in normalized transmittance with input intensity indicated the optical limiting behavior at the wavelength 532 nm. The excited-state absorption cross-section value (sigma(ex)= 1.72 x 10(-16) cm(2)) is much greater than ground-state absorption cross-section value (sigma(g)= 2.49 x 10(-22) cm(2)), suggesting that optical limiting phenomena are due to RSA.

Formula: C9H10O3. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Raghavendra, S; Kumar, CSC; Kumar, DJM; Al-Ghorbani, M; Alsalme, A; Quah, CK; Raghavendra, PV; Serrao, FJ; Dharmaprakash, SM 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 m-Methoxyphenol. Tang, ZQ; Li, DD; Yue, YD; Peng, D; Liu, L in [Tang, Zhiqiong; Li, Dongdong; Yue, Yidi; Peng, Dan; Liu, Lu] East China Normal Univ, Sch Chem & Mol Engn, 500 Dongchuan Rd, Shanghai 200241, Peoples R China; [Liu, Lu] East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, Shanghai 200062, Peoples R China published Bronsted acid catalysed chemo- and ortho-selective aminomethylation of phenol in 2021.0, Cited 69.0. The Name is m-Methoxyphenol. Through research, I have a further understanding and discovery of 150-19-6.

We have developed a Bronsted acid catalysed highly ortho-selective functionalization of free phenols with readily available N,O-acetals under mild conditions, furnishing various corresponding aminomethylated phenol products in moderate to excellent yields. The salient features of this transformation include mild conditions, good substrate scope, excellent ortho-selectivity, high efficiency, and ease of further transformation.

About m-Methoxyphenol, If you have any questions, you can contact Tang, ZQ; Li, DD; Yue, YD; Peng, D; Liu, L or concate me.. Application In Synthesis of m-Methoxyphenol

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 ESCHERICHIA-COLI; ANTIBIOTIC-RESISTANCE; CRYSTAL-STRUCTURE; MOLECULAR-BASIS; FOLIC-ACID; BINDING; METHOTREXATE; INTEGRONS; CLASS-1; WATER, Saw an article supported by the Natural Sciences and Engineering Research Council of CanadaNatural Sciences and Engineering Research Council of Canada (NSERC)CGIAR [227853, 2018-04686]; Canada Foundation for Innovation grantCanada Foundation for Innovation [11510]; CIHR operating grantCanadian Institutes of Health Research (CIHR) [MOP-13107]; Fondation Marcel et Rolande Gosselin; les Fonds Quebecois pour la Recherche sur la Nature et les Technologies (FQRNT)FQRNT; Hydro-Quebec; Faculte des etudes superieures et post-doctorales de l’Universite de Montreal (FESP); PROTEO, the Quebec Network for Research on Protein, Function, Engineering and Applications; Natural Sciences and Engineering Research Council of CanadaNatural Sciences and Engineering Research Council of Canada (NSERC)CGIAR; McGill University; CIHR Strategic Initiative in Chemical BiologyCanadian Institutes of Health Research (CIHR); NSERC CREATE Program in Bionanomachines; PROTEO. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Toulouse, JL; Yachnin, BJ; Ruediger, EH; Deon, D; Gagnon, M; Saint-Jacques, K; Ebert, MCCJC; Forge, D; Bastien, D; Colin, DY; Eynde, JJV; Marinier, A; Berghuis, AM; Pelletier, JN. The CAS is 100-83-4. Through research, I have a further understanding and discovery of 3-Hydroxybenzaldehyde. Recommanded Product: 100-83-4

The worldwide use of the broad-spectrum antimicrobial trimethoprim (TMP) has induced the rise of TMP-resistant microorganisms. In addition to resistance-causing mutations of the microbial chromosomal dihydrofolate reductase (Dfr), the evolutionarily and structurally unrelated type II Dfrs (DfrBs) have been identified in TMP-resistant microorganisms. DfrBs are intrinsically TMP-resistant and allow bacterial proliferation when the microbial chromosomal Dfr is TMP-inhibited, making these enzymes important targets for inhibitor development. Furthermore, DfrBs occur in multiresistance plasmids, potentially accelerating their dissemination. We previously reported symmetrical bisbenzimidazoles that are the first selective inhibitors of the only well-characterized DfrB, DfrB1. Here, their diversification provides a new series of inhibitors (K-i = 1.7-12.0 mu M). Our results reveal two prominent features: terminal carboxylates and inhibitor length allow the establishment of essential interactions with DfrB1. Two crystal structures demonstrate the simultaneous binding of two inhibitor molecules in the symmetrical active site. Observations of those dimeric inhibitors inspired the design of monomeric analogues, binding in a single copy yet offering similar inhibition potency (K-i = 1.1 and 7.4 mu M). Inhibition of a second member of the DfrB family, DfrB4, suggests the generality of these inhibitors. These results provide key insights into inhibition of the highly TMP-resistant DfrBs, opening avenues to downstream development of antibiotics for combatting this emergent source of resistance.

Recommanded Product: 100-83-4. About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Toulouse, JL; Yachnin, BJ; Ruediger, EH; Deon, D; Gagnon, M; Saint-Jacques, K; Ebert, MCCJC; Forge, D; Bastien, D; Colin, DY; Eynde, JJV; Marinier, A; Berghuis, AM; Pelletier, JN 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

Recommanded Product: 86-95-3. I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Novel Pyrazoloquinolin-2-ones: Design, synthesis, docking studies, and biological evaluation as antiproliferative EGFR-TK inhibitors published in 2019, Reprint Addresses Aly, AA (corresponding author), Menia Univ, Fac Sci, Dept Chem, Al Minya 61519, Egypt.; Abuo-Rahma, GEDA (corresponding author), Menia Univ, Fac Pharm, Dept Med Chem, Al Minya 61519, Egypt.. The CAS is 86-95-3. Through research, I have a further understanding and discovery of 4-Hydroxyquinolin-2(1H)-one.

Two new series of diethyl 2-[2-(substituted-2-oxo-1,2-dihydroquinolin-4-yl)hydrazono]-succinates 6a-g and 1-(2-oxo-1,2-dihydroquinolin-4-yl)-1H-pyrazoles 7a-f have been designed and synthesized. The structures of the synthesized compounds were proved by IR, mass, NMR (2D) spectra and elemental analyses. The target compounds were evaluated for their in vitro cytotoxic activity against 60 cancer cell lines according to NCI protocol. Consequently, seven compounds were further examined against the most sensitive cell lines, leukemia CCRFCEM, and MOLT-4. 5-Amino-1-(6-bromo-2-oxo-1,2-dihydroquinolin-4-yl)-1H-pyrazole-3,4-dicarbonitrile (7f) was the most active product, with IC50= 1.35 uM and 2.42 uM against MOLT-4 and CCRF-CEM, respectively. Also, it showed a remarkable inhibitory activity compared to erlotinib on the EGFR TK with IC50 = 247.14 nM and 208.42 nM, respectively. Cell cycle analysis of MOLT-4 cells treated with 7f showed cell cycle arrest at G2/M phase (supported by Caspases, BAX and Bcl-2 studies) with a significant pro-apoptotic activity as indicated by annexin V-FITC staining. Moreover, the docking study indicated that both the pyrazole moiety and the quinolin-2-one ring showed good fitting into EGFR (PDB code: 1M17). In order to interpret SAR of the designed compounds, and provide a basis for further optimization, molecular docking of the synthesized compounds to known EGFR inhibitors was performed. The study illustrated the effect of several factors on the compounds’ activity.

Recommanded Product: 86-95-3. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Elbastawesy, MAI; Aly, AA; Ramadan, M; Elshaier, YAMM; Youssif, BGM; Brown, AB; Abuo-Rahma, GEDA 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

An article Fe3O4/GO@melamine-ZnO nanocomposite: A promising versatile tool for organic catalysis and electrical capacitance WOS:000505567400031 published article about DIHYDROPYRANO 2,3-C PYRAZOLE; REDUCED GRAPHENE OXIDE; MULTICOMPONENT SYNTHESIS; ONE-POT; ACID; DERIVATIVES; EFFICIENT; GREEN; WATER in [Eivazzadeh-Keihan, Reza; Taheri-Ledari, Reza; Khosropour, Nastaran; Maleki, Ali] Iran Univ Sci & Technol, Dept Chem, Catalysts & Organ Synth Res Lab, Tehran 1684613114, Iran; [Dalvand, Samad; Mousavi-Khoshdel, S. Morteza] Iran Univ Sci & Technol, Fac Chem, Ind Electrochem Res Lab, Tehran 1684613114, Iran; [Sohrabi, Hessamaddin] Univ Tabriz, Fac Chem, Dept Analyt Chem, Tabriz, Iran in 2020.0, Cited 47.0. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4. Quality Control of 3-Hydroxybenzaldehyde

Herein, an efficient versatile nanocomposite constructed of melamine-functionalized graphene oxide nano-sheets (GO@melamine), iron oxide nanoparticles (Fe3O4 NPs), and zinc oxide (ZnO NPs) is presented. Moreover, two different applications have been studied for the prepared Fe3O4/GO@melamine-ZnO nanocomposite: First, as a heterogeneous catalyst for synthesis of pyrano[2,3-c]pyrazole derivatives in short reaction time (10 min) with high yields (96 %), second, as a substantial electrical supercapacitor with typical capacitive behavior, high resistance, and excellent electrode stability. From the catalytic aspect, high effectiveness, convenient isolation, and significant reusability could be referred as the distinguished properties for the produced nanocomposite. Turn-over number (TON) and turn-over frequency (TOF) values for the presented catalytic system have been estimated 17.2 x 10(6) and 1.71 x 10(6) min(-1), respectively, which revealed high catalytic performance of this catalytic system. From electrochemical aspect, economic benefits for fabrication of the introduced nanocomposite containing low-cost materials, make it as a suitable electrical supercapacitor for industrial applications.

Quality Control of 3-Hydroxybenzaldehyde. About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Eivazzadeh-Keihan, R; Taheri-Ledari, R; Khosropour, N; Dalvand, S; Maleki, A; Mousavi-Khoshdel, SM; Sohrabi, H 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

Recommanded Product: 120-14-9. Authors Awasthi, A; Yadav, P; Tiwari, DK in ROYAL SOC CHEMISTRY published article about in [Awasthi, Annapurna; Yadav, Pushpendra; Tiwari, Dharmendra Kumar] Ctr Biomed Res CBMR, Mol Synth & Drug Discovery Unit, SGPGIMS Campus,Raibareli Rd, Lucknow 226014, Uttar Pradesh, India; [Awasthi, Annapurna; Yadav, Pushpendra] Banaras Hindu Univ, Inst Sci, Dept Chem, Varanasi 221005, Uttar Pradesh, India in 2021.0, Cited 63.0. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

An efficient, general, and practical route for highly diastereoselective synthesis of aza-spirocyclic pyrazolones from easily available alpha-amino acids, aldehydes, and alkylidene pyrazolones by means of a decarboxylative annulation process is reported. This high-yielding reaction proceeds through a [3+2]-cycloaddition reaction between alkylidene pyrazolones and a nonstabilized azomethine ylide generated in situ. This method provides easy and smooth access to a variety of highly functionalized aza-spirocyclic pyrazolones in excellent yields (up to 96%). The obtained spiro-pyrazolones comprise four contiguous stereogenic centers including a quaternary carbon center.

Recommanded Product: 120-14-9. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Awasthi, A; Yadav, P; Tiwari, DK 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 WET AIR OXIDATION; ARYL-ALPHA-DIAZOACETATES; FENTON-LIKE DEGRADATION; SI-H; CARBENE INSERTION; NATURAL-PRODUCTS; DIAZO-COMPOUNDS; N-H; HYDROGEN-ATOM; M-CRESOL, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [21901124]; Natural Science Foundation of the Jiangsu Higher Education Institutions of ChinaNational Natural Science Foundation of China (NSFC) [19KJB150032, 19KJB610013]; China Postdoctoral Science FoundationChina Postdoctoral Science Foundation [2019M651809]; Jiangsu Planned Projects for Postdoctoral Research Funds [2019K110]; Natural Science Foundation of Jiangsu ProvinceNatural Science Foundation of Jiangsu Province [BK20160989]. Published in ROYAL SOC CHEMISTRY in CAMBRIDGE ,Authors: Zhang, ZP; Yu, Y; Huang, F; Yi, XY; Xu, Y; He, YD; Baell, JB; Huang, H. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol. Quality Control of 3-(Trifluoromethyl)phenol

Developing a greener, sustainable catalyst is a very important but challenging task in organic synthesis. Herein, for the first time, we choose more economical and greener surface modified sewage sludge-derived carbonaceous materials (SW) treated by perchloric acid as a new catalyst for carbene insertion of alpha-aryl alpha-diazoacetates into O-H bonds of phenols with good yields and high functional group tolerance. Significantly, we explored the scope of natural phenols with compelling biological activity, and successfully afforded the O-H insertion and meta C-H functionalization products. Their structures have been confirmed by single-crystal X-ray crystallography. Furthermore, the bioactivities (anti-tumor and anti-inflammatory) of the majority of O-H insertion products are better than those of the natural phenols themselves. The IC50 values indicated that the remarkable compounds 7a (IC50 = 16.80 mu M) and 7c (IC50 = 16.48 mu M) had better inhibition for tumor cell A-549 than positive control DDP (IC50 = 20.62 mu M). It should be noted that these transformations may provide a new strategy to derive natural products and discover new drugs.

Quality Control of 3-(Trifluoromethyl)phenol. About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Zhang, ZP; Yu, Y; Huang, F; Yi, XY; Xu, Y; He, YD; Baell, JB; Huang, H 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