Day: October 19, 2021

An article Synthesis and antiviral effect of novel fluoxetine analogues as enterovirus 2C inhibitors WOS:000540343900005 published article about POLIOVIRUS; REPLICATION; PROTEIN; ATPASE; CLASSICS; MOTIF in [Manganaro, Roberto; Zonsics, Birgit; Lopez, Moira Lorenzo; Saporito, Fabiana; Ferla, Salvatore; Brancale, Andrea] Cardiff Univ, Sch Pharm & Pharmaceut Sci, King Edward VII Ave, Cardiff CF10 3NB, Wales; [Bauer, Lisa; Donselaar, Tim; Zwaagstra, Marleen; Strating, Jeroen R. P. M.; Hurdiss, Daniel L.; van Kuppeveld, Frank J. M.] Univ Utrecht, Fac Vet Med, Dept Infect Dis & Immunol, Virol Div, NL-3584 CL Utrecht, Netherlands; [Coutard, Bruno] UVE Aix Marseille Univ, Inserm 1207, IHU Mediterranee Infect, Unite Virus Emergents,IRD 190, Marseille, France; [Coutard, Bruno] Aix Marseille Univ, CNRS, AFMB UMR 7257, Marseille, France in 2020, Cited 24. Formula: C7H5F3O. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9

Enteroviruses (EV) are a group of positive-strand RNA ( + RNA) viruses that include many important human pathogens (e.g. poliovirus, coxsackievirus, echovirus, numbered enteroviruses and rhinoviruses). Fluoxetine was identified in drug repurposing screens as potent inhibitor of enterovirus B and enterovirus D replication. In this paper we are reporting the synthesis and the antiviral effect of a series of fluoxetine analogues. The results obtained offer a preliminary insight into the structure-activity relationship of its chemical scaffold and confirm the importance of the chiral configuration. We identified a racemic fluoxetine analogue, 2b, which showed a similar antiviral activity compared to (S)-fluoxetine. Investigating the stereochemistry of 2b revealed that the Senantiomer exerts potent antiviral activity and increased the antiviral spectrum compared to the racemic mixture of 2b. In line with the observed antiviral effect, the Senantiomer displayed a dose-dependent shift in the melting temperature in thermal shift assays, indicative for direct binding to the recombinant 2C protein.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Manganaro, R; Zonsics, B; Bauer, L; Lopez, ML; Donselaar, T; Zwaagstra, M; Saporito, F; Ferla, S; Strating, JRPM; Coutard, B; Hurdiss, DL; van Kuppeveld, FJM; Brancale, A or concate me.. 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

I found the field of Biochemistry & Molecular Biology; Chemistry very interesting. Saw the article Regioselective Monobromination of Phenols with KBr and ZnAl-BrO3–Layered Double Hydroxides published in 2020. Recommanded Product: 98-17-9, Reprint Addresses Wang, LG; Hu, J (corresponding author), Zhejiang Univ Technol, Coll Chem Engn, Hangzhou 310004, Peoples R China.. The CAS is 98-17-9. Through research, I have a further understanding and discovery of 3-(Trifluoromethyl)phenol

The regioselective mono-bromination of phenols has been successfully developed with KBr and ZnAl-BrO3–layered double hydroxides (abbreviated as ZnAl-BrO3–LDHs) as brominating reagents. The para site is much favorable and the ortho site takes the priority if para site is occupied. This reaction featured with excellent regioselectivity, cheap brominating reagents, mild reaction condition, high atom economy, broad substrate scope, and provided an efficient method to synthesize bromophenols.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Wang, LG; Feng, C; Zhang, Y; Hu, J or concate me.. Recommanded Product: 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

COA of Formula: C7H8O. Kong, CL; Li, AH; Su, J; Wang, XC; Chen, CQ; Tao, YS in [Kong, Cai-Lin; Wang, Xing-Chen; Chen, Chao-Qi; Tao, Yong-Sheng] Northwest A&F Univ, Coll Enol, Xinong Rd 22, Yangling 712100, Shaanxi, Peoples R China; [Li, Ai-Hua] Northwest A&F Univ, Coll Food Sci & Engn, Yangling 712100, Shaanxi, Peoples R China; [Su, Jun] Res Ctr Spine Grapes, Hongjiang 418200, Hunan, Peoples R China; [Tao, Yong-Sheng] Shaanxi Engn Res Ctr Viti Viniculture, Yangling 712100, Shaanxi, Peoples R China published Flavor modification of dry red wine from Chinese spine grape by mixed fermentation with Pichia fermentans and S. cerevisiae in 2019.0, Cited 38.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6.

Mixed fermentation of Pichia fermentans and Saccharomyces cerevisiae was designed to circumvent the problem of weak aroma in Chinese spine grape wines. Spine grape, Xiang Pearl, was used for wine production by red wine making processes. Physicochemical indices were measured using titratable and spectroscopic methodologies. Volatiles were quantified by SPME-GC-MS, and aroma attributes were analyzed by trained panelists. Results showed mixed fermentation benefited color properties by improving total anthocyanin, polymeric anthocyanin, and total tannin contents. The content of varietal compounds, except those of thiols, were reduced, whereas fermentative compounds contents, especially those of higher alcohols, esters, and phenylethyls, were increased by mixed fermentation. Sensory analysis showed mixed fermentation enhanced fruity and floral traits in wine; this was confirmed by mathematical regression showing elevated levels of fermentative volatiles dominated the contribution to pleasant aroma, whereas reduced content of varietal compounds, with the exception of thiols, correlated negatively with favorable characteristics.

About Benzyl Alcohol, If you have any questions, you can contact Kong, CL; Li, AH; Su, J; Wang, XC; Chen, CQ; Tao, YS or concate me.. COA of Formula: C7H8O

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: C8H8O2. Authors Mondal, B; Adhikari, U; Hajra, PP; Roy, UK in ROYAL SOC CHEMISTRY published article about in [Mondal, Bibhas; Hajra, Partha Pratim; Roy, Ujjal Kanti] Kazi Nazrul Univ, Dept Chem, Asansol 713340, W Bengal, India; [Mondal, Bibhas; Adhikari, Utpal] Natl Inst Technol Durgapur, Dept Chem, Durgapur 713209, India in 2021.0, Cited 41.0. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5

A simple one pot allylation and propargylation of aldehydes mediated by zinc(0), which is in situ generated from the redox couple of Al and ZnCl2 in 2N HCl, is demonstrated to afford the corresponding homoallyl and homopropargyl alcohols with excellent yields.

Formula: C8H8O2. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Mondal, B; Adhikari, U; Hajra, PP; Roy, UK 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 Ghorbani, F; Pourmousavi, SA; Kiyani, H in BENTHAM SCIENCE PUBL LTD published article about ORDERED MESOPOROUS CARBON; SOLVENT-FREE SYNTHESIS; RECYCLABLE CATALYST; SULFONIC-ACID; REUSABLE CATALYST; 1,1-DIACETATES; DEPROTECTION; CHLORIDE; CONVERSION; MILD in [Ghorbani, Fatemeh; Pourmousavi, Seied Ali; Kiyani, Hamzeh] Damghan Univ, Sch Chem, Damghan 3671641167, Iran; [Pourmousavi, Seied Ali] Damghan Univ, Inst Biol Sci, Damghan 3671641167, Iran in 2020.0, Cited 54.0. COA of Formula: C7H6O2. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4

Background: Much attention has been focused on heterogeneous catalysts. Reactions with these recoverable and reusable catalysts are clean, selective with high efficiency. Among the heterogeneous solid acid catalyst in organic synthesis, Carbon-Based Solid Acids (CBSAs), which are important solid acid with many practical and research applications have been extensively studied. In this work, green Pistachio peel, a biomass waste, was converted into a novel carbon-based solid acid catalyst (Pis-SO3H). Objective: The aim of this work is to synthesize highly sulfonated carbon as an efficient, recyclable, nontoxic solid acid catalyst by simultaneous sulfonation, dehydration and carbonization of green Pistachio peel as biomass and investigate the catalytic activity of Pis-SO3H in acetalization, thioacetalization, acylation of aldehydes and synthesis of 3,3′-Arylmethylene-bis(4-hydroxycoumarin) derivatives. Methods: Pis-SO3H was synthesized by an integrated fast one- step hydrothermal carbonization and sulfonation process in the presence of sulfuric acid. The characterization of the physicochemical properties of Pis-SO3H was achieved by XRD, FT-IR, FE-SEM, and elemental analysis. Results: The result of acid-base titration showed that the total acidity of the catalyst was 7.75 mmol H(+)g(-1). This new heterogeneous catalyst has been efficiently used for the chemoselective thioacetalization, acetalization and acylation of aldehyde and the synthesis of biscoumarins under solvent-free conditions. All the reactions work easily in high yields. The antimicrobial activity of some of the biscoumarins was evaluated in screening by disk diffusion assay for the zone of inhibition. Conclusion: The catalytic activity of the Pis-SO3H was investigated during acetalization, thioacetalization, acylation and synthesis of biscoumarins. The results of protection of carbonyl groups and synthesis of biscoumarins in the present work offer effective alternatives for environmentally friendly utilization of abundant biomass waste.

About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Ghorbani, F; Pourmousavi, SA; Kiyani, H or concate me.. COA of Formula: C7H6O2

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. Zhang, Y; Wang, YY; Zhao, YX; Gu, W; Zhu, YQ; Wang, SF in [Zhang, Yan; Wang, Yunyun; Zhao, Yuxun; Gu, Wen; Wang, Shifa] Nanjing Forestry Univ, Coll Chem Engn, Nanjing 210037, Jiangsu, Peoples R China; [Zhu, Yongqiang] Jiangsu Chia Tai Fenghai Pharmaceut Co Ltd, Nanjing 210046, Jiangsu, Peoples R China; [Gu, Wen; Wang, Shifa] Nanjing Forestry Univ, Coinnovat Ctr Efficient Proc & Utilizat Forest Re, Nanjing 210037, Jiangsu, Peoples R China published Novel camphor-based pyrimidine derivatives induced cancer cell death through a ROS-mediated mitochondrial apoptosis pathway in 2019.0, Cited 41.0. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4.

A series of novel camphor-based pyrimidine derivatives (3a-3x) have been synthesized; their structures were determined by using conventional methods and compound 3f was further confirmed through single crystal XRD analysis. The cytotoxic activity of the target compounds against a panel of human normal (GES-1) and cancer cell lines (MDA-MB-231, RPMI-8226, A549) was evaluated by MTS assay. Here we found that compound 3f exhibited the strongest anti-tumor activity, comparable to that of etoposide, and had much lower cytotoxicity to normal GES-1 cells (IC50 > 50 mu M) than the reference drug (IC50 = 8.89 mu M). Subsequent mechanism studies in MDA-MB-231 cells revealed that compound 3f caused G0/G1 phase arrest and apoptosis in a dose dependent manner. Moreover, the loss of mitochondrial membrane potential and enhancement of cellular ROS levels were also observed upon 3f treatment, which indicated that 3f exerted cytotoxic activity by a ROS-mediated mitochondrial apoptosis pathway. This result was confirmed by a significant increase in the expression of pro-apoptotic proteins Bax, cytochrome C and caspase-3, and downregulation of anti-apoptosis protein Bcl-2. Overall, 3f can be adopted for further investigation in the development of antitumor agents based on natural products.

Category: indole-building-block. About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Zhang, Y; Wang, YY; Zhao, YX; Gu, W; Zhu, YQ; Wang, SF 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 Visible-Light-Induced Carbonylation of Indoles with Phenols under Metal-Free Conditions: Synthesis of Indole-3-carboxylates WOS:000664333200051 published article about CATALYZED DIRECT CARBONYLATION; OXIDATIVE CARBONYLATION; PHOTOREDOX CATALYSIS; CARBOXYLIC-ACIDS; H CARBONYLATION; IODINE; FUNCTIONALIZATION; (HETERO)ARENES; STRATEGIES; ALKALOIDS in [Qi, Zhuang; Li, Lin; Liang, Ying-Kang; Ma, Ai-Jun; Zhang, Xiang-Zhi; Peng, Jin-Bao] Wuyi Univ, Sch Biotechnol & Hlth Sci, Jiangmen 529020, Guangdong, Peoples R China in 2021.0, Cited 43.0. The Name is Mequinol. Through research, I have a further understanding and discovery of 150-76-5. Quality Control of Mequinol

A visible-light-induced carbonylation of indoles with phenols for the synthesis of indole-3-carboxylates has been developed. The reaction proceeded via a radical carbonylation process in which elementary I-2 was used as an effective photosensitive initiator and, thus, avoided the use of transition metal catalysts. A series of different aryl indole-3-carboxylates were prepared in moderate to good yields. The broad applicability of this methodology was further highlighted by the late-stage functionalization of several phenol-containing natural products and pharmaceuticals.

Quality Control of Mequinol. About Mequinol, If you have any questions, you can contact Qi, Z; Li, L; Liang, YK; Ma, AJ; Zhang, XZ; Peng, JB 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 Mitsui, A; Nagao, K; Ohmiya, H in WILEY-V C H VERLAG GMBH published article about in [Mitsui, Atsuhisa; Nagao, Kazunori; Ohmiya, Hirohisa] Kanazawa Univ, Grad Sch Med Sci, Div Pharmaceut Sci, Kakuma Machi, Kanazawa, Ishikawa 9201192, Japan; [Ohmiya, Hirohisa] PRESTO, JST, 4-1-8 Honcho, Kawaguchi, Saitama 3320012, Japan in 2021.0, Cited 59.0. Application In Synthesis of 4-Methoxybenzaldehyde. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5

A reductive cross-coupling reaction between aromatic aldehydes and arylnitriles using a copper catalyst and a silylboronate as a reductant is reported. This protocol represents an unprecedented approach to the chemoselective synthesis of alpha-hydroxy ketones by electrophile-electrophile cross-coupling.

Application In Synthesis of 4-Methoxybenzaldehyde. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Mitsui, A; Nagao, K; Ohmiya, 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

In 2020 CHEMISTRYSELECT published article about COPPER-CATALYZED HYDROXYLATION; ARYLBORONIC ACIDS; IPSO-HYDROXYLATION; BORONIC ACIDS; HETEROGENEOUS CATALYST; ORGANOCATALYTIC OXIDATION; ARYL HALIDES; NANOPARTICLES; MILD; ALDEHYDES in [Gujjarappa, Raghuram; Vodnala, Nagaraju; Malakar, Chandi C.] Natl Inst Technol Manipur, Dept Chem, Imphal 795004, Manipur, India; [Garg, Aakriti; Gupta, Sreya] NIPER, Dept Med Chem, 168 Maniktala Main Rd, Kolkata 700054, India; [Hazra, Chinmoy K.] Indian Inst Technol Delhi, Dept Chem, Hauz Khas, New Delhi 110016, India in 2020, Cited 80. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4. Recommanded Product: 4′-Hydroxyacetophenone

An efficient amino-acid-mediated ipso-hydroxylation of arylboronic acids, aryl boronate esters and aryl trifluoroborates to aryl alcohols has been described. The current protocol was realized by using sub-stoichiometric amount of l-histidine in presence of triethylamine under aerobic conditions in DMF as solvent. This amino-acid-mediated process provides an alternative route for the hydroxylation of organoborons through in situ generation of hydrogen peroxide. The present protocol explores the synthetic utility of amino acids as organocatalysts for the preparation of aryl alcohols. It was observed that l-histidine plays an important role for the conversion of aerial oxygen in to hydrogen peroxide via thermal excitation process followed by thermal degradation of Et3N. The developed approach holds good for a wide range of compounds with excellent yields and competent functional group tolerance.

Recommanded Product: 4′-Hydroxyacetophenone. About 4′-Hydroxyacetophenone, If you have any questions, you can contact Gujjarappa, R; Vodnala, N; Garg, A; Hazra, CK; Gupta, S; Malakar, CC 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

Choo, HJ; Ahn, JH in [Choo, Hye Jeong; Ahn, Joong-Hoon] Konkuk Univ, Bio Mol Informat Ctr, Dept Biosci & Biotechnol, Seoul 05029, South Korea published Synthesis of Three Bioactive Aromatic Compounds by Introducing Polyketide Synthase Genes into Engineered Escherichia coli in 2019, Cited 31. Application In Synthesis of 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.

Intermediates in aromatic amino acid biosynthesis can serve as substrates for the synthesis of bioactive compounds. In this study we used two intermediates in the shikimate pathway of Escherichia coli, chorismate and anthranilate, to synthesize three bioactive compounds: 4-hydroxycoumarin (4-HC), 2,4-dihydroxyquinoline (DHQ), and 4-hydroxy-1-methyl-2(1H)-quinolone (NMQ). We introduced genes for the synthesis of salicylic acid from chorismate to supply the substrate for 4-HC and the gene encoding N-methyltransferase for the synthesis of N-methylanthranilate from anthranilate. Polyketide synthases and coenzyme (Co)A ligases were tested to determine the optimal combination of genes for the synthesis of each compound. We also tested several constructs and identified the best one for increasing levels of endogenous substrates for chorismate, anthranilate, and malonyl-CoA. With the use of these strategies, 255.4 mg/L 4-HC, 753.7 mg/L DHQ, and 17.5 mg/L NMQwere synthesized. This work provides a basis for the synthesis of diverse coumarin and quinoline derivatives with potential medical applications.

About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Choo, HJ; Ahn, JH or concate me.. Application In Synthesis of 4-Hydroxyquinolin-2(1H)-one

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