Category: indole-building-block

An article Catalytic O-H bond insertion reactions using surface modified sewage sludge as a catalyst WOS:000519903900026 published article about WET AIR OXIDATION; ARYL-ALPHA-DIAZOACETATES; FENTON-LIKE DEGRADATION; SI-H; CARBENE INSERTION; NATURAL-PRODUCTS; DIAZO-COMPOUNDS; N-H; HYDROGEN-ATOM; M-CRESOL in [Zhang, Zhipeng; Huang, Fei; Huang, He] Nanjing Normal Univ, Sch Food Sci & Pharmaceut Engn, Nanjing 210023, Peoples R China; [Zhang, Zhipeng] South China Univ Technol, Sch Biol & Biol Engn, Guangzhou 510006, Peoples R China; [Yu, Yang; He, Yide] Nanjing Tech Univ, Sch Environm Sci & Engn, Nanjing 211816, Peoples R China; [Yi, Xiangyan; Baell, Jonathan B.; Huang, He] Nanjing Tech Univ, Sch Pharmaceut Sci, Nanjing 211816, Peoples R China; [Xu, Yao] Soochow Univ, Affiliated Hosp 1, Suzhou 215006, Peoples R China; Monash Univ, Monash Inst Pharmaceut Sci, Med Chem, Parkville, Vic 3052, Australia in 2020, Cited 108. Application In Synthesis of 3-(Trifluoromethyl)phenol. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9

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.

Application In Synthesis of 3-(Trifluoromethyl)phenol. Welcome to talk about 98-17-9, 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 send Email.

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. In 2019.0 RES CHEM INTERMEDIAT published article about MOLECULAR DOCKING; ORGANIC SELENIDES; TOPOISOMERASE-II; MICROTUBULE; ANTIOXIDANT; CELLS in [Bakherad, Zohreh; Fassihi, Afshin; Sadeghi-Aliabadi, Hojjat; Saghaie, Lotfollah] Isfahan Univ Med Sci, Sch Pharm & Pharmaceut Sci, Dept Med Chem, Esfahan 8174673461, Iran; [Safavi, Maliheh] Iranian Res Org Sci & Technol, Dept Biotechnol, Tehran 33535111, Iran; [Sepehri, Saghi] Ardabil Univ Med Sci, Sch Pharm, Dept Med Chem, Ardebil 5618953141, Iran; [Bakherad, Mohammad] Shahrood Univ Technol, Sch Chem, Shahrood, Iran; [Rastegar, Hossein] MOE & ME, Food & Drug Lab Res Ctr, Food & Drug Control Labs, Tehran, Iran; [Larijani, Bagher; Mahdavi, Mohammad] Univ Tehran Med Sci, Endocrinol & Metab Res Ctr, Endocrinol & Metab Res Inst, Tehran, Iran in 2019.0, Cited 32.0. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.

A series of novel imidazopyridine derivatives of indole has been synthesized. All the synthesized derivatives were evaluated for their antiproliferative activity against A-549, T-47D, Hep-G2 and MCF-7 human cancer cell lines. The results demonstrated that some of these derivatives exhibited moderate to excellent cytotoxic activities. Compounds 7a having a cyclohexyl ring substituted to the second amine of imidazopyridyl moiety and phenyl ring of the C-2 indole ring and 7f with a para-methylphenyl ring at the same position exhibited the highest activity against the A-594 cell line with IC50 of 11.48 mu M and 10.66 mu M, respectively. The results indicate that compounds 7a and 7f are more cytotoxic towards cancer cell lines compared with etoposide in vitro. In addition, compounds, 7d and 7j showed the most potent activity against Hep-G2, equal to etoposide as the standard drug. Also, most of the compounds were inactive against the T-47D and MCF-7 cell lines. The morphological analysis by the acridine orange/ethidium bromide double-staining test and flow cytometry analysis indicated that compounds 7a and 7f induced apoptosis in A-549 cells. Furthermore, in silico and in vitro results of the synthesized compounds showed good correlation with each other. Molecular docking results of the compounds of the 7a-k series with the cyclohexyl ring substituted to the second amine of the imidazopyridyl moiety compared with the 7l-t members with the t-butyl group at the same position confirmed the effect of the higher lipophilicity on hydrophobic interactions with the studied enzymes. Moreover, all the compounds showed higher affinity to tubulin than topoisomerase II alpha enzyme.

Category: indole-building-block. About 4′-Hydroxyacetophenone, If you have any questions, you can contact Bakherad, Z; Safavi, M; Sepehri, S; Fassihi, A; Sadeghi-Aliabadi, H; Bakherad, M; Rastegar, H; Larijani, B; Saghaie, L; Mahdavi, 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

In 2019 ORG LETT published article about ERIOSTEMON; SYNTHASE in [Coleman, Matthew A.; Burchill, Laura; Sumby, Christopher J.; George, Jonathan H.] Univ Adelaide, Dept Chem, Adelaide, SA 5005, Australia in 2019, Cited 12. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3. Safety of 4-Hydroxyquinolin-2(1H)-one

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.

Safety of 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

Recently I am researching about HIGHLY ENANTIOSELECTIVE APPROACH; CYCLOADDITION; 4C+3C, Saw an article supported by the M.D. Anderson Foundation; University of Houston. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Li, J; Gilbertson, SR. The CAS is 123-11-5. Through research, I have a further understanding and discovery of 4-Methoxybenzaldehyde. Category: indole-building-block

A diastereoselective [4 + 2] cycloisomerization of asymmetric allenyl dienes is reported. The asymmetric dienyl allenes are synthesized using the method reported by Ma. These substrates readily undergo diastereoselective intramolecular rhodium catalyzed [4 + 2] cycloisomerization analogous to thermal intramolecular Diels-Alder reactions. Overall, 29 examples are presented with tethers possessing nitrogen, oxygen, and carbon. Diastereoselectivities range from 99:1 to 90:10 in most examples.

Category: indole-building-block. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Li, J; Gilbertson, SR 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 Griseofulvin Derivatives: Synthesis, Molecular Docking and Biological Evaluation WOS:000483383900006 published article about INDOLE ALKALOIDS; ENDOPHYTIC FUNGUS; A-C; PENICILLIUM; BIOCHEMISTRY; PRODUCT; TUBULIN in [Kartsev, Victor] InterBioscreen, Moscow, Russia; [Geronikaki, Athina; Petrou, Anthi] Aristotle Univ Thessaloniki, Dept Pharm, Sch Hlth, Thessaloniki 54124, Greece; [Lichitsky, Boris] Zelinsky Inst Organ Chem, Moscow 119991, Russia; [Kostic, Marina; Smiljkovic, Marija; Sokovic, Marina] Univ Belgrade, Mycol Lab, Dept Plant Physiol, Inst Biol Res Sinisa Stankov, Bulevar Despota Stefana 142, Belgrade 11000, Serbia; [Sirakanyan, Samvel] Natl Acad Sci Republ Armenia, Sci Technol Ctr Organ & Pharmaceut Chem, Inst Fine Organ Chem AL Mnjoyan, Ave Azatutyan 26, Yerevan 0014, Armenia in 2019.0, Cited 48.0. Safety of 3-Hydroxybenzaldehyde. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4

Background: Griseofulvin – a mold metabolite produced by Penisilium griseofulvum is known as an antifungal drug. Objective: Thus, the goal of this paper is the design and synthesis of new griseofulvin derivatives and evaluation of their antifungal activity. Methods: Forty-two new compounds were synthesized using classical methods of organic synthesis and evaluated for their antimicrobial activity by microdilution method. Results: All forty-two new compounds exhibited very good activity against eight tested micromycetes with MIC ranging from 0.0075-0.055 mg/ml and MFC from 0.02-024 mg/ml. All compounds exhibited better activity than reference drugs ketoconazole (7-42 times) and bifonazole (3-16 fold). The most promising was compound 15. The most sensitive fungal was found to be T. viride, while the most resistant, as was expected, was A. fumigatus. It should be mentioned that most of compounds exhibited better activity than griseofulvin. The molecular docking studies revealed that the most active compound have the same hydrophobic and H-bonding interactions with Thr276 residue observed for griseofulvin forming 3 hydrogen bonds while griseofulvin only one. In general, the molecular docking results coincide with experimental. Conclusion: Forty-two giseofulvin derivatives were designed, synthesized and evaluated for antimicrobial activity. These derivatives revealed good antifungal activity, better than reference drugs ketoconazole, bifonazole, and griseofulvin as well.

About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Kartsev, V; Geronikaki, A; Petrou, A; Lichitsky, B; Kostic, M; Smiljkovic, M; Sokovic, M; Sirakanyan, S or concate me.. Safety of 3-Hydroxybenzaldehyde

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 Biomimetic Synthesis Enables the Structure Revision of Furoerioaustralasine WOS:000494553300055 published article about ERIOSTEMON; SYNTHASE in [Coleman, Matthew A.; Burchill, Laura; Sumby, Christopher J.; George, Jonathan H.] Univ Adelaide, Dept Chem, Adelaide, SA 5005, Australia in 2019, Cited 12. Safety 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

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.

Safety of 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

An article A Rapid Ultrasound Synthesis of Xanthenediones Catalyzed by Boric acid in Ethanol-Water Medium: Single Crystal, DFT and Hirshfeld Surface Analysis of Two Representative Compounds WOS:000609159200018 published article about DENSITY-FUNCTIONAL THERMOCHEMISTRY; INTERMOLECULAR INTERACTIONS; PROMOTED SYNTHESIS; SULFURIC-ACID; EFFICIENT; DERIVATIVES; 1,8-DIOXO-OCTAHYDROXANTHENES; ALDEHYDES in [Shashi, R.; Begum, Noor Shahina] Bangalore Univ, Dept Studies Chem, Bangalore 560056, Karnataka, India; [Panday, Anoop Kumar] Indian Inst Technol, Dept Chem, Bihta 801103, Bihar, India in 2021, Cited 45. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9. SDS of cas: 120-14-9

A highly versatile and efficient ultrasound promoted synthesis of xanthenedione derivatives is achieved through condensation of dimedone with various aromatic aldehydes using boric acid as catalyst in ethanol-water medium. The advantages of this method being, mild reaction conditions, short reaction time, easy work-up, purification of products by non-chromatographic methods and additionally this method provides excellent yields. Two of the Xanthendiones derivatives 3a and 3b gave good crystals on recrystallization and their molecular structures were confirmed by crystallographic studies. The molecules in the crystal lattice are held together by weak intermolecular C-H center dot center dot center dot O and C-H center dot center dot center dot N interactions. Further insights into these interactions using Hirshfeld surface analysis and DFT/B3LYP studies show that in compound 3a H center dot center dot center dot H (54.7%), O center dot center dot center dot H (18.3%) and in 3b H center dot center dot center dot H (53.7%), O center dot center dot center dot H (17.6%) are the major contributors to the intermolecular interactions which stabilize the crystal structures. In order to determine molecular electrical transport properties, we studied the energy difference between Highest Occupied, HOMO, and Lowest Unoccupied, LUMO orbitals and the HOMO and LUMO energy gap for compounds 3a and 3b was found to be 3.9261 eV and 4.6436 eV respectively. The 2D fingerprint plot provided percentage contribution of each individual atom-to-atom interactions. The Mulliken atomic charges and molecular electrostatic potential on molecular van der Waals surface were calculated to know the electrophilic and nucleophilic regions of the molecular surface. (C) 2020 Elsevier B.V. All rights reserved.

SDS of cas: 120-14-9. About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Shashi, R; Begum, NS; Panday, AK 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. Li, LX; Dong, L; Li, DD; Guo, Y; Liu, XH; Wang, YQ in [Li, Lingxiao; Dong, Lin; Li, Didi; Guo, Yong; Liu, Xiaohui; Wang, Yanqin] East China Univ Sci & Technol, Sch Chem & Mol Engn, Res Inst Ind Catalysis, Shanghai Key Lab Funct Mat Chem, Shanghai 200237, Peoples R China published Hydrogen-Free Production of 4-Alkylphenols from Lignin via Self-Reforming-Driven Depolymerization and Hydrogenolysis in 2020.0, Cited 59.0. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.

Lignin is constructed from methoxylated phenylpropanoid with plenty of hydroxys and methoxys. Its conversion to valuable products is extremely attractive but especially challenging without additional hydrogen sources. Herein we report a hydrogen-free production of 4-alkylphenols directly from native lignin via self-reforming-driven depolymerization and hydrogenolysis over Pt/NiAl2O4. This is the first example of acquiring 4-alkylphenols from native lignin. Using this strategy, high yields of 4-alkylphenols, 17.3 wt %, were obtained from birch lignin. Reaction pathway and mechanism studies revealed that this strategy initiates from the reforming of aliphatic hydroxys, followed by the cleavage of C-O linkages, and ends via demethoxylation over Pt/NiAl2O4. Moreover, the subsequent aqueous phase reforming of the as-formed methanol accelerates the whole process. This strategy realizes the one-pot production of 4-alkylphenols from lignin by fully utilizing the structural hydrogen in lignin and H2O, providing a low-cost and safe method of lignin valorization.

About 4′-Hydroxyacetophenone, If you have any questions, you can contact Li, LX; Dong, L; Li, DD; Guo, Y; Liu, XH; Wang, YQ or concate me.. Category: indole-building-block

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 Mentese, E; Sokmen, BB in WILEY published article about MOLECULAR DOCKING; BIOLOGICAL-ACTIVITIES; BEARING TRIAZOLE; DERIVATIVES; ANTIOXIDANT; OXADIAZOLE in [Mentese, Emre] Recep Tayyip Erdogan Univ, Art & Sci Fac, Dept Chem, Rize, Turkey; [Sokmen, Bahar Bilgin] Giresun Univ, Fac Arts & Sci, Dept Chem, TR-28049 Giresun, Turkey in 2019.0, Cited 27.0. Quality Control of 4′-Hydroxyacetophenone. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4

A novel series of N ‘-(substituted benzylidene)-2-(5,6-dichloro-2-methyl-1H-benzimidazol-1-yl)acetohydrazides and N ‘-(1-(substituted phenyl)ethylidene)-2-(5,6-dichloro-2-methyl-1H-benzimidazol-1-yl)acetohydrazides were synthesized and then studied for their urease inhibitory activities using thiourea as a standard drug. All newly synthesized compounds were found to exhibit potent inhibitory properties against urease enzyme in the range of IC50 = 0.0155 +/- 0.0039-0.0602 +/- 0.0071 mu M, when compared with the thiourea as standard (IC50 = 0.5115 +/- 0.0233 mu M). All target molecules were characterized by H-1-NMR, C-13-NMR, IR, and electrospray ionization mass spectrometry.

Quality Control of 4′-Hydroxyacetophenone. About 4′-Hydroxyacetophenone, If you have any questions, you can contact Mentese, E; Sokmen, BB 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

Field, T; Peterson, J; Ma, CC; Jagadesan, P; Da Silva, JP; Rubina, M; Ramamurthy, V; Givens, RS in [Field, Thomas; Peterson, Julie; Ma, Chicheng; Rubina, Marina; Givens, Richard S.] Univ Kansas, Dept Chem, Lawrence, KS 66045 USA; [Jagadesan, Pradeepkumar; Ramamurthy, V.] Univ Miami, Dept Chem, Coral Gables, FL 33124 USA; [Da Silva, Jose P.] Univ Algarve, CCMAR Ctr Marine Sci, Campus Gambelas, P-8005139 Faro, Portugal published Competing pathways for photoremovable protecting groups: the effects of solvent, oxygen and encapsulation in 2020.0, Cited 58.0. Name: 4′-Hydroxyacetophenone. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4.

Extending the applications of Photoremovable Protecting Groups (PPGs) to cage phenols has generally met with unusually complex PPG byproducts. In this study, we demonstrate that thep-hydroxyphenacyl (pHP) cage for both simple and complex phenolics, including tyrosine, dispenses free phenols. With the simpler unsubstituted phenols, the reaction is governed by their Bronsted Leaving Group ability. On the other hand, the byproducts of the cage vary with these phenols. For the more acidic phenols the cage byproduct follows the Favorskii rearrangement to formp-hydroxyphenylacetic acid whereas for the weaker phenols other reactions such as reduction and hydrolysis begin to emerge. When the photolysis is conducted in octa acid (OA) containers, non-Favorskii, unrearranged fragments of the cage and other byproducts arise.

Name: 4′-Hydroxyacetophenone. About 4′-Hydroxyacetophenone, If you have any questions, you can contact Field, T; Peterson, J; Ma, CC; Jagadesan, P; Da Silva, JP; Rubina, M; Ramamurthy, V; Givens, RS 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