Tag: M.W=100-150

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

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 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

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 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

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

Formula: C8H8O2. Recently I am researching about COPPER-OXIDE NANOPARTICLES; ONE-POT SYNTHESIS; REUSABLE CATALYST; LEAF EXTRACT; ANTIBACTERIAL; EFFICIENT; BIOSYNTHESIS; REDUCTION; OXIDATION, Saw an article supported by the . Published in SPRINGER in DORDRECHT ,Authors: Shinde, B; Kamble, S; Jadhav, H; Mane, P; Khude, K; Kim, H; Karale, B; Burungale, A. The CAS is 123-11-5. Through research, I have a further understanding and discovery of 4-Methoxybenzaldehyde

The biogenic synthesis of copper oxide nanoparticles (CuO NPs) from the leaf extract of Alpinia zerumbet was investigated in this protocol. The basic nature of A. zerumbet leaf extract helps in CuO NPs synthesis. The catalytic activity of A. zerumbet-fabricated CuO NPs is explored in water at room temperature only in the presence of NaPTS hydrotrope. The green catalytic protocol is investigated via synthesis of 1,8-dioxooctahydroxanthene. The biogenic leaf extract fabricated CuO NPs are efficiently reactive, stable and recyclable in aqueous solution of sodium p-toluenesulfonate (NaPTS) hydrotrope. CuO/NaPTS proved to be the best catalytic system as synergistic nanotrope in terms of yield and time of reaction in water at room temperature. The green synthetic approach of CuO NPs, greener medium, easy workup and proficient recyclability are advantages in the said protocol. This is first time report of catalytic activity of biogenic CuO NPs in water at room temperature in the presence of NaPTS.

About 4-Methoxybenzaldehyde, If you have any questions, you can contact Shinde, B; Kamble, S; Jadhav, H; Mane, P; Khude, K; Kim, H; Karale, B; Burungale, A or concate me.. Formula: C8H8O2

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 CATIONIC-POLYMERIZATION; EFFICIENT SYNTHESIS; CHEMISTRY; SILYLKETENES; POLYMERS, Saw an article supported by the National Science FoundationNational Science Foundation (NSF) [NSF 1807510]; NSFNational Science Foundation (NSF) [MRI-1334048]. Published in AMER CHEMICAL SOC in WASHINGTON ,Authors: Mitchell, SM; Xiang, Y; Matthews, R; Arnburgey, AM; Pentzer, EB. The CAS is 150-19-6. Through research, I have a further understanding and discovery of m-Methoxyphenol. Product Details of 150-19-6

Silyl-substituted ketenes are attractive molecular building blocks due to their stability and ease of storage, as opposed to unstable alkyl and aryl ketenes. To better understand the reactivity of silyl ketenes and, in turn, their use in the preparation of highly functionalized small molecules, the reaction of silyl ketenes with different nucleophiles was studied. The addition of alcohol, amine, or thiol nucleophiles to the central carbon of silyl ketene, followed by proton transfer afforded alpha-silyl ester, amide, or thio-ester, respectively. Catalytic amounts of Lewis acid greatly increase the rate of the reaction, and the impact of nucleophile, Lewis acid, and silyl substituent are evaluated. The small molecules produced from these reactions give insight into the use of silyl ketenes as building blocks for complex molecular structures.

About m-Methoxyphenol, If you have any questions, you can contact Mitchell, SM; Xiang, Y; Matthews, R; Arnburgey, AM; Pentzer, EB or concate me.. Product Details of 150-19-6

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 Strain-Induced Nucleophilic Ring Opening of Donor-Acceptor Cyclopropenes for Synthesis of Monosubstituted Succinic Acid Derivatives WOS:000592483300001 published article about CATALYZED CYCLOISOMERIZATION; STEREOSELECTIVE-SYNTHESIS; NORDITERPENOID ALKALOIDS; OXIDATION-STATE; CYCLIZATION; ESTERS in [Marichev, Kostiantyn O.; Wang, Kan; Greco, Nicole; Dong, Kuiyong; Doyle, Michael P.] Univ Texas San Antonio, Dept Chem, One UTSA Circle, San Antonio, TX 78249 USA; [Chen, Jinzhou; Lei, Jinping] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Peoples R China in 2021.0, Cited 54.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6. Application In Synthesis of Benzyl Alcohol

1,2,3-Trisubstituted donor-acceptor cyclopropenes (DACPs) generated in situ from enoldiazo compounds react with nucleophiles to form alpha-substituted succinic acid derivatives in high yields. Initial dirhodium(II) carboxylate catalysis rapidly converts enoldiazo-acetates or -acetamides to DACPs that undergo catalyst-free Favorskii ring opening with amines, and also with anilines, alcohols, and thiols, when facilitated by catalytic amounts of 4-dimethylaminopyridine (DMAP). This methodology provides easy access to mixed esters and amides of monosubstituted succinic acids, including derivatives of naturally occurring compounds. It also affords dihydrazide, dihydroxamic acid, and diamide derivatives, as well as alpha-substituted tetrahydropyridazine-3,6-diones in high yields. Attempts to generate optically enriched DACPs were not successful because their populations having the R and S configurations formed with a chiral dirhodium catalyst are quite similar, and the loss of enantiocontrol likely originates from the DACP ring forming step which is reversible with its intermediate metal carbene.

Application In Synthesis of Benzyl Alcohol. About Benzyl Alcohol, If you have any questions, you can contact Marichev, KO; Wang, K; Greco, N; Dong, KY; Chen, JZ; Lei, JP; Doyle, 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

Recently I am researching about ONE-POT SYNTHESIS; SOLVENT PROMOTED ADDITION; EFFICIENT SYNTHESIS; QUINAZOLIN-4(3H)-ONES; DERIVATIVES; CONVENIENT; OXIDE, Saw an article supported by the University of Newcastle Postgraduate Research Scholarship (UNPRS); Australian Research Council (ARC Discovery Project)Australian Research Council [DP180101781]; Australian Cancer Research Foundation; Ramaciotti Foundation. HPLC of Formula: C7H6O2. Published in CSIRO PUBLISHING in CLAYTON ,Authors: O’Brien, NS; McCluskey, A. The CAS is 100-83-4. Through research, I have a further understanding and discovery of 3-Hydroxybenzaldehyde

An elegantly simple, facile, and robust approach to a scaffold of biological importance, 2,3-dihydroquinazolin-4(1H)-ones, is reported. A catalytic 1% SnCl2/microwave-mediated approach afforded access to pure material, collected by cooling and filtration after 20-min microwave irradiation at 120 degrees C. Atotal of 41 analogues were prepared in isolated yields of 17-99 %. This process was highly tolerant of aliphatic, aromatic, heterocyclic, and acyclic aldehydes, but furan, pyrrole, and thiophene aldehyde reactivity correlated with propensity towards electrophilic addition and/or Diels-Alder addition. As a result, thiophene afforded high yields (80 %) whereas pyrrole carboxaldehyde failed to react. With simple cinnamaldehydes, and in the SbCl3-mediated reaction, and with alpha,beta-unsaturated aldehydes the equivalent quinazolin-4(3H)-ones, and not the 2,3-dihydroquinazolin-4(1H)-ones, was favoured.

HPLC of Formula: C7H6O2. About 3-Hydroxybenzaldehyde, If you have any questions, you can contact O’Brien, NS; McCluskey, 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