Day: October 11, 2021

In 2020 MOL DIVERS published article about CORRESPONDING CARBONYL-COMPOUNDS; SECONDARY ALCOHOLS; BROMOSUCCINIMIDE in [Kulkarni, Mahesh R.; Lad, Nitin P.; Gaikwad, Nitin D.] KRT Arts BH Commerce & AM Sci Coll, Organ Chem Res Ctr, Dept Chem, Gangapur Rd, Nasik 422002, MS, India in 2020, Cited 20. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6. Quality Control of Benzyl Alcohol

The oxidation of benzylic alcohol to corresponding aldehyde and ketone using N-chlorosuccinimide (NCS)-N,N-dimethylformamide (DMF) has been described. This method gives easy access to the corresponding carbonyl compounds under metal-free conditions, without the use of corrosive reagent at ambient temperature in good yield.

About Benzyl Alcohol, If you have any questions, you can contact Kulkarni, MR; Lad, NP; Gaikwad, ND or concate me.. Quality Control of Benzyl Alcohol

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 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. Computed Properties of C9H7NO2

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.

Computed Properties of 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

An article Discovery of Carboline Derivatives as Potent Antifungal Agents for the Treatment of Cryptococcal Meningitis WOS:000461537000012 published article about FLUCONAZOLE; COMBINATION in [Tu, Jie; Li, Zhuang; Jiang, Yanjuan; Ji, Changjin; Han, Guiyan; Wang, Yan; Liu, Na; Sheng, Chunquan] Second Mil Med Univ, Sch Pharm, Dept Med Chem, 325 Guohe Rd, Shanghai 200433, Peoples R China in 2019.0, Cited 40.0. The Name is m-Methoxyphenol. Through research, I have a further understanding and discovery of 150-19-6. Formula: C7H8O2

Clinical treatment of cryptococcal meningitis (CM) remains a significant challenge because of the lack of effective and safe drug therapies. Developing novel CM therapeutic agents with novel chemical scaffolds and new modes of action is of great importance. Herein, new beta-hexahydrocarboline derivatives are shown to possess potent anticryptococcal activities. In particular, compound A4 showed potent in vitro and in vivo anticryptococcal activity with good metabolic stability and blood-brain barrier permeability. Compound A4 was orally active and could significantly reduce brain fungal burdens in a murine model of CM. Moreover, compound A4 could inhibit several virulence factors of Cryptococcus neoformans and might act by a new mode of action. Preliminary mechanistic studies revealed that compound A4 induced DNA double-stranded breaks and cell cycle arrest at the G2 phase by acting on the Cdc25c/CDK1/cyclin B pathway. Taken together, beta-hexahydrocarboline A4 represents a promising lead compound for the development of next-generation CM therapeutic agents.

About m-Methoxyphenol, If you have any questions, you can contact Tu, J; Li, Z; Jiang, YJ; Ji, CJ; Han, GY; Wang, Y; Liu, N; Sheng, CQ or concate me.. Formula: C7H8O2

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

Yang, S; Xiong, MF; Tian, WQ; Zhang, H; Xiao, XY; Liu, HY; Chang, CK in [Yang, Shuang; Xiong, Ming-Feng; Tian, Wan-Qun; Zhang, Hao; Xiao, Xin-Yan; Liu, Hai-Yang] South China Univ Technol, Dept Chem, Key Lab Funct Mol Engn Guangdong Prov, Guangzhou 510641, Peoples R China; [Chang, Chi-Kwong] Michigan State Univ, Dept Chem, E Lansing, MI 48824 USA published Construction of C-O bond via cross-dehydrogenative coupling of sp [3] C-H bond with phenols catalyzed by copper porphyrin in 2020, Cited 42. Name: 3-(Trifluoromethyl)phenol. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9.

Copper porphyrin-catalyzed construction of ether bond by cross-dehydrogenative coupling of sp [3] C-H bond with phenols bearing electron-withdrawing groups (EWG) was described for the first time. A broad range of substrates afforded different acetals in moderate to excellent yields with good functional group tolerance. The developed method is not only suitable for phenol substrates with ortho-directing groups, but also suitable for those phenol without ortho-directing groups. Significantly, a high turnover number (TON) up to 7300 was achieved in gram-level test. (C) 2020 Elsevier Ltd. All rights reserved.

About 3-(Trifluoromethyl)phenol, If you have any questions, you can contact Yang, S; Xiong, MF; Tian, WQ; Zhang, H; Xiao, XY; Liu, HY; Chang, CK or concate me.. Name: 3-(Trifluoromethyl)phenol

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 Beatty, JW; Lindsey, EA; Thomas-Tran, R; Debien, L; Mandal, D; Jeffrey, JL; Tran, AT; Fournier, J; Jacob, SD; Yan, XL; Drew, SL; Ginn, E; Chen, A; Pham, AT; Zhao, SR; Jin, LX; Young, SW; Walker, NP; Leleti, MR; Moschutz, S; Strater, N; Powers, JP; Lawson, KV in AMER CHEMICAL SOC published article about ECTO-5′-NUCLEOTIDASE; INSIGHTS; 5-NUCLEOTIDASE; EXPRESSION; ANTI-CD73; ADENOSINE; THERAPY; CD39 in [Beatty, Joel W.; Lindsey, Erick A.; Thomas-Tran, Rhiannon; Debien, Laurent; Mandal, Debashis; Jeffrey, Jenna L.; Tran, Anh T.; Fournier, Jeremy; Jacob, Steven D.; Yan, Xuelei; Drew, Samuel L.; Ginn, Elaine; Chen, Ada; Pham, Amber T.; Zhao, Sharon; Jin, Lixia; Young, Stephen W.; Walker, Nigel P.; Leleti, Manmohan Reddy; Powers, Jay P.; Lawson, Kenneth, V] Arcus Biosci Inc, Hayward, CA 94545 USA; [Moschuetz, Susanne; Straeter, Norbert] Univ Leipzig, Ctr Biotechnol & Biomed, Inst Bioanalyt Chem, D-04103 Leipzig, Germany in 2020.0, Cited 32.0. Product Details of 100-83-4. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4

CD73 is an extracellular mediator of purinergic signaling. When upregulated in the tumor microenvironment, CD73 has been implicated in the inhibition of immune function through overproduction of adenosine. Traditional efforts to inhibit CD73 have involved antibody therapy or the development of small molecules, the most potent of which mimic the acidic and ionizable structure of the enzyme’s natural substrate, adenosine 5′-monophosphate (AMP). Here, we report the systematic discovery of a novel class of non-nucleotide CD73 inhibitors that are more potent than all other nonphosphonate inhibitor classes reported to date. These efforts have culminated in the discovery of 4(-{5-[4-fluoro-1-(2H-indazol-6-yl)-1H-1,2,3-benzotriazol-6-yl]-1H-pyrazol-1-yl}methyl)benzonitrile (73, IC50 = 12 nM) and 4-({5[4-4-chloro-1-(2H-indazol-6-yl)-1H-1,2,3-benzotriazol-6-yl]-1H-pyrazol-1-yl}methyl)benzonitrile (74, IC50 = 19 nM). Cocrystallization of 74 with human CD73 demonstrates a competitive binding mode. These compounds show promise for the improvement of drug-like character via the attenuation of the acidity and low membrane permeability inherent to known nucleoside inhibitors of CD73.

Product Details of 100-83-4. About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Beatty, JW; Lindsey, EA; Thomas-Tran, R; Debien, L; Mandal, D; Jeffrey, JL; Tran, AT; Fournier, J; Jacob, SD; Yan, XL; Drew, SL; Ginn, E; Chen, A; Pham, AT; Zhao, SR; Jin, LX; Young, SW; Walker, NP; Leleti, MR; Moschutz, S; Strater, N; Powers, JP; Lawson, KV 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 ClO2 pre-oxidation changes the yields and formation pathways of chloroform and chloral hydrate from phenolic precursors during chlorination WOS:000452931600025 published article about DISINFECTION BY-PRODUCTS; DISSOLVED ORGANIC-MATTER; AQUATIC HUMIC MATERIAL; DRINKING-WATER; TRIHALOMETHANE FORMATION; AQUEOUS CHLORINATION; MODEL COMPOUNDS; DIOXIDE; OXIDATION; KINETICS in [Gan, Wenhui; Ge, Yuexian; Zhu, Haihui; Huang, Huang; Yang, Xin] Sun Yat Sen Univ, Sch Environm Sci & Engn, Guangdong Prov Key Lab Environm Pollut Control &, Guangzhou 510275, Guangdong, Peoples R China in 2019.0, Cited 51.0. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4. SDS of cas: 99-93-4

Phenolic moieties in natural organic matter (NOM) are important precursors of disinfection by-products (DBPs). In this study, the formation of chloral hydrate from chlorination of seventeen phenolic compounds, including mono-, di- and tri-hydroxybenzenes, were evaluated and the role of chlorine dioxide (ClO2) pre-oxidation on its formation pathways was explored. Chloroform, was also evaluated for comparison. Chlorination of resorcinol exhibited the highest chloral hydrate yield (2.83 +/- 0.13%) followed by chlorination of 2,4,6-trichlorophenol (0.61 +/- 0.03%). The median of chloral hydrate yields from the tested phenolic compounds was 0.22%. ClO2 pre-oxidation reduced the yields of chloroform from phenol derivatives by 37-97%, except 4-methoxyphenol, catechol and 2,3-dihydroxyphenol. On the contrary, ClO2 pre-oxidation of di- and tri-hydroxybenzenes tended to increase chloral hydrate yields in post-chlorination. Mixed results (both increases and decreases) were observed in chloral hydrate formation from chlorination of mono-hydroxybenzenes after ClO2 pre-oxidation. The changes of their formation were dependent on ClO2 pre-oxidation time and dosages. Identification of transformation products suggested that phenolic compounds were mainly converted to unsaturated carbonyl structures by ClO2. Chlorine substituted benzoquinones and cyclopent-4-ene-1,3-diones were important transformation products after a series of ring open, decarboxylation, hydrolysis and chlorine substitution reactions. The changes in the formation yields of chloral hydrate and chloroform were governed by the difference in initial phenolic precursors and the transformation products after ClO2 pre-oxidation. ClO2 pre-oxidation in water treatment can effectively reduce chloroform formation but may have a risk of increasing chloral hydrate formation. (C) 2018 Elsevier Ltd. All rights reserved.

SDS of cas: 99-93-4. About 4′-Hydroxyacetophenone, If you have any questions, you can contact Gan, WH; Ge, YX; Zhu, HH; Huang, H; Yang, X 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 synergetic role of Aegle marmelos fruit ash in the synthesis of biscoumarins and 2-amino-4H-chromenes WOS:000605133500012 published article about POT 3-COMPONENT SYNTHESIS; HETEROGENEOUS CATALYST; BIOLOGICAL EVALUATION; SUBSTITUTED 2-AMINO-4H-CHROMENES; COUMARIN DERIVATIVES; ORGANIC-SYNTHESIS; HIGHLY EFFICIENT; GREEN; WATER; CYTOTOXICITY in [Patil, Rupesh C.; Shinde, Sachinkumar K.; Patil, Uttam P.; Birajdar, Appasaheb T.; Patil, Suresh S.] Shivaji Univ, PDVP Coll, PG Dept Chem, Synthet Res Lab, Sangli 416312, MS, India in 2021, Cited 72. Quality Control of 4-Methoxybenzaldehyde. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5

A dry rind of Aegle marmelos (bael) fruit ash as a synergetic alternative material to an expensive, toxic and corrosive catalysts for the synthesis of biscoumarins and 2-amino-4H-chromenes at ambient temperature in water is reported. The spectroscopic evidence from EDX, FTIR, XRD and SEM analysis of bael fruit ash supports the presence of metal oxides, carbonates and hydroxides which are intensely responsible for the acceleration of the reactions. The striking features of this protocol are utilization of bio-waste, cost-effective, recyclable and biodegradable catalytic system, which provide good to excellent yields in a short reaction time. [GRAPHICS] .

Quality Control of 4-Methoxybenzaldehyde. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Patil, RC; Shinde, SK; Patil, UP; Birajdar, AT; Patil, SS 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 Synthesis of 17 beta-hydroxysteroid dehydrogenase type 10 steroidal inhibitors: Selectivity, metabolic stability and enhanced potency WOS:000600418500049 published article about ALZHEIMERS-DISEASE; A-BETA; CHEMICAL-SYNTHESIS; DESIGN; ABAD/17-BETA-HSD10; IDENTIFICATION; OPTIMIZATION; DERIVATIVES; CHEMISTRY; PEPTIDE in [Boutin, Sophie; Maltais, Rene; Roy, Jenny; Poirier, Donald] CHU Quebec, Res Ctr, Lab Med Chem, Endocrinol & Nephrol Unit, Quebec City, PQ, Canada; [Boutin, Sophie; Poirier, Donald] Univ Laval, Fac Med, Dept Mol Med, Quebec City, PQ, Canada in 2021, Cited 47. SDS of cas: 120-14-9. The Name is 3,4-Dimethoxybenzaldehyde. Through research, I have a further understanding and discovery of 120-14-9

17beta-Hydroxysteroid dehydrogenase type 10 (17 beta-HSD10) is the only mitochondrial member of 17 beta-HSD family. This enzyme can oxidize estradiol (E2) into estrone (E1), thus reducing concentration of this neuroprotective steroid. Since 17 beta-HSD10 possesses properties that suggest a possible role in Alzheimer’s disease, its inhibition appears to be a therapeutic strategy. After we identified the androsterone (ADT) derivative 1 as a first steroidal inhibitor of 17 beta-HSD10, new analogs were synthesized to increase the metabolic stability, to improve the selectivity of inhibition over 17 beta-HSD3 and to optimize the inhibitory potency. From six D-ring derivatives of 1 (17-C = O), two compounds (17 beta-H/17 alpha-OH and 17 beta-OH/17aC CH) were more metabolically stable and did not inhibit the 17 beta-HSD3. Moreover, solid phase synthesis was used to extend the molecular diversity on the 3b-piperazinylmethyl group of the steroid base core. Eight over 120 new derivatives were more potent inhibitors than 1 for the transformation of E2 to E1, with the 4-(4-trifluoromethyl-3-methoxybenzyl)piperazin-1-ylmethyl-ADT (D-3,7) being 16 times more potent (IC50 = 0.14 mM). Finally, D-ring modification of D-3,7 provided 17 beta-OH/17 alpha-C CH derivative 25 and 17 beta-H/17 alpha-OH derivative 26, which were more potent inhibitor than 1 (1.8 and 2.4 times, respectively). (C) 2020 Elsevier Masson SAS. All rights reserved.

About 3,4-Dimethoxybenzaldehyde, If you have any questions, you can contact Boutin, S; Maltais, R; Roy, J; Poirier, D or concate me.. SDS of cas: 120-14-9

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

An article Functionalization of the Chalcone Scaffold for the Discovery of Novel Lead Compounds Targeting Fungal Infections WOS:000457137200158 published article about IN-VITRO; ANTIFUNGAL AGENTS; AMPHOTERICIN-B; SAPROCHAETE; MECHANISMS; PRODUCTS; EFFICACY in [Bonvicini, Francesca; Gentilomi, Giovanna A.] Alma Mater Studiorum Univ Bologna, Dept Pharm & Biotechnol, Via Massarenti 9, I-40138 Bologna, Italy; [Gentilomi, Giovanna A.] Alma Mater Studiorum Univ Bologna, S Orsola Malpighi Hosp, Unit Microbiol, Via Massarenti 9, I-40138 Bologna, Italy; [Bressan, Francesca; Gobbi, Silvia; Rampa, Angela; Bisi, Alessandra; Belluti, Federica] Alma Mater Studiorum Univ Bologna, Dept Pharm & Biotechnol, Via Belmeloro 6, I-40126 Bologna, Italy in 2019.0, Cited 30.0. Category: indole-building-block. The Name is 4′-Hydroxyacetophenone. Through research, I have a further understanding and discovery of 99-93-4

The occurrence of invasive fungal infections represents a substantial threat to human health that is particularly serious in immunocompromised patients. The limited number of antifungal agents, devoid of unwanted toxic effects, has resulted in an increased demand for new drugs. Herein, the chalcone framework was functionalized to develop new antifungal agents able to interfere with cell growth and with the infection process. Thus, a small library of chalcone-based analogues was evaluated in vitro against C. albicans ATCC 10231 and a number of compounds strongly inhibited yeast growth at non-cytotoxic concentrations. Among these, 5 and 7 interfered with the expression of two key virulence factors in C. albicans pathogenesis, namely, hyphae and biofilm formation, while 28 emerged as a potent and broad spectrum antifungal agent, enabling the inhibition of the tested Candida spp. and non-Candida species. Indeed, these compounds combine two modes of action by selectively interfering with growth and, as an added value, weakening microbial virulence. Overall, these compounds could be regarded as promising antifungal candidates worthy of deeper investigation. They also provide a chemical platform through which to perform an optimization process, addressed at improving potency and correcting liabilities.

Category: indole-building-block. About 4′-Hydroxyacetophenone, If you have any questions, you can contact Bonvicini, F; Gentilomi, GA; Bressan, F; Gobbi, S; Rampa, A; Bisi, A; Belluti, F 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 MOLECULES published article about STEP ECONOMY PASE; ONE-POT; CORROSION-INHIBITORS; MULTICOMPONENT REACTIONS; ORGANIC-SYNTHESIS; MILD-STEEL; PARTITION-COEFFICIENTS; ATOM ECONOMY; EFFICIENT; DERIVATIVES in [Ryzhkov, Fedor, V; Ryzhkova, Yuliya E.; Elinson, Michail N.; Fakhrutdinov, Artem N.; Vereshchagin, Anatoly N.; Egorov, Mikhail P.] Russian Acad Sci, ND Zelinsky Inst Organ Chem, Leninsky Pr 47, Moscow 119991, Russia; [Vorobyev, Stepan V.] Gubkin Russian State Univ Oil & Gas, Dept Organ Chem & Petr Chem, 65 Leninsky Prospect, Moscow 119991, Russia in 2020, Cited 63. The Name is 4-Hydroxyquinolin-2(1H)-one. Through research, I have a further understanding and discovery of 86-95-3. HPLC of Formula: C9H7NO2

The Pot, Atom, and Step Economy (PASE) approach is based on the Pot economy principle and unites it with the Atom and Step Economy strategies; it ensures high efficiency, simplicity and low waste formation. The PASE approach is widely used in multicomponent chemistry. This approach was adopted for the synthesis of previously unknown hydroxyquinolinone substituted chromeno[2,3-b]pyridines via reaction of salicylaldehydes, malononitrile dimer and hydroxyquinolinone. It was shown that an ethanol-pyridine combination is more beneficial than other inorganic or organic catalysts. Quantum chemical studies showed that chromeno[2,3-b]pyridines has potential for corrosion inhibition. Real time H-1 NMR monitoring was used for the investigation of reaction mechanism and 2-((2H-chromen-3-yl)methylene)malononitrile was defined as a key intermediate in the reaction.

HPLC of Formula: C9H7NO2. About 4-Hydroxyquinolin-2(1H)-one, If you have any questions, you can contact Ryzhkov, FV; Ryzhkova, YE; Elinson, MN; Vorobyev, SV; Fakhrutdinov, AN; Vereshchagin, AN; Egorov, MP 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