Month: October 2022

Akins, Nicholas S.; Mishra, Nisha; Harris, Hannah M.; Dudhipala, Narendar; Kim, Seong Jong; Keasling, Adam W.; Majumdar, Soumyajit; Zjawiony, Jordan K.; Paris, Jason J.; Ashpole, Nicole M.; Le, Hoang V. published the artcile< C2-Salvinorin Ester 6,5-Fused Ring, Dual Kappa and Mu Opioid Receptor Agonists as Analgesics Devoid of Anxiogenic Effects>, Recommanded Product: 5-Fluoroindole-2-carboxylic acid, the main research area is methoxycarbonyl hydroxy dimethyl dioxobenzoisochromene aryl ester opioid receptor agonist.

Current common analgesics are mediated through the mu or kappa opioid receptor agonism. Unfortunately, selective mu or kappa receptor agonists often cause harmful side effects. However, ligands exhibiting dual agonism to the opioid receptors, such as to mu and kappa, or to mu and delta, have been suggested to temper undesirable adverse effects while retaining analgesic activity. Herein we report an introduction of various 6,5-fused rings to C2 of the salvinorin scaffold via an ester linker. In vitro studies showed that many of these compounds have dual agonism on kappa and mu opioid receptors. In vivo studies on the lead dual kappa and mu opioid receptor agonist demonstrated supraspinal thermal analgesic activity while avoiding anxiogenic effects in male mice, thus providing further strong evidence in support of the therapeutic advantages of dual opioid receptor agonists over selective opioid receptor agonists.

ChemMedChem published new progress about Analgesics. 399-76-8 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Recommanded Product: 5-Fluoroindole-2-carboxylic acid.

Referemce:
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

Cheng, Guangsheng; Deng, Hongmei; He, Xiang; Gao, Yu; Li, Chunju; Jia, Xueshun; Li, Jian published the artcile< Isocyanide-Based Multicomponent Reaction To Furnish N-Functionalized Indoles by using N-Acyliminium Ions as Key Intermediates>, Product Details of C10H9NO, the main research area is indolyl pyrrolidinone preparation.

The present work discloses an efficient multicomponent reaction of isocyanides, allenoates, and indoles. This protocol provides rapid and direct access to N-functionalized indoles from readily available starting materials, in the absence of any catalyst. The strategy also features a broad substrate scope and mild conditions.

European Journal of Organic Chemistry published new progress about Allenes Role: RCT (Reactant), RACT (Reactant or Reagent). 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, Product Details of C10H9NO.

Referemce:
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

Xing, Fei; Zhang, Qilong; Gao, Lingfeng; Zheng, Gengxiu published the artcile< Fabrication of a fluorescent probe for in-situ and ratiometric visualization of autophagy>, Recommanded Product: 2-(2-Aminoethyl)-3′,6′-bis(diethylamino)spiro[isoindoline-1,9′-xanthen]-3-one, the main research area is fluorescent probe autophagy; Autophagy; Fluorescent probe; Ratiometric; pH sensitive.

In situ and real-time visualization of autophagy process is of vital importance for fundamental researches in biol. However, fluorescent probes for autophagy were rarely reported, which greatly hindered the study on autophagy. A fluorescent probe was rationally designed and fabricated for the ratiometric visualization of autophagy. The probe targeted non-lysosome organelles in healthy cells, and gave blue emission. During autophagy, the organelles together with the probe were delivered into acid lysosomes, and gave red fluorescence. In this way, the autophagy process could be monitored in ratiometric manner. The starvation induced autophagy was successfully visualized by the probe, and the inhibition effect of chloroquine to autophagy was also observed The authors expect that the probe can serve as powerful tool for the study of autophagy and relative areas.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy published new progress about Autophagy. 950846-89-6 belongs to class indole-building-block, and the molecular formula is C30H36N4O2, Recommanded Product: 2-(2-Aminoethyl)-3′,6′-bis(diethylamino)spiro[isoindoline-1,9′-xanthen]-3-one.

Referemce:
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

Heath-Brown, B.; Philpott, P. G. published the artcile< The indole series. I. Indolylalkylamines>, Computed Properties of 4771-48-6, the main research area is .

The preparation of a large series of indolylalkylamines is described, including α-alkyl-, α,α-dialkyl-, and N-alkyltryptamines. New methods include a modification of the Abramovich synthesis giving α,N-dimethyltryptamines directly.

Journal of the Chemical Society published new progress about 4771-48-6. 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, Computed Properties of 4771-48-6.

Referemce:
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

Kroeger, A. Pia P.; Paats, Jan-Willem D.; Boonen, Roy J. E. A.; Hamelmann, Naomi M.; Paulusse, Jos M. J. published the artcile< Pentafluorophenyl-based single-chain polymer nanoparticles as a versatile platform towards protein mimicry>, COA of Formula: C30H36N4O2, the main research area is pentafluorophenyl single chain polymer nanoparticle protein mimicry versatile platform.

Proteins are biopolymers folded into 3D-structures and are omnipresent in biol. systems, where they fulfil a wide array of complex functions. Mimicking the exceptional characteristics of proteins with synthetic analogs may likewise give unprecedented control over a nanomaterial’s pharmacokinetic behavior, enabling controlled delivery of therapeutics or imaging agents. Recent advances in polymer science have enabled the formation of bio-inspired single-chain polymer nanoparticles (SCNPs), which are formed by intramol. collapse of individual polymer chains, and display sizes ranging from 5-20 nm. Here, we describe the preparation of SCNPs containing activated ester moieties, facilitating SCNP functionalization without altering its backbone structure. Pentafluorophenyl-functional SCNPs were prepared through intramol. thiol-Michael addition crosslinking of thiol-functional precursor copolymers. Post-formation functionalization of the resulting SCNPs through substitution of the activated pentafluorophenyl esters with a variety of amines resulted in a series of water-soluble SCNPs with fluorescent labels, ‘click’ functionality, amino acids and even peptides. This synthetic strategy offers a straightforward method towards SCNP modification and SCNP-protein hybrids, giving access to easily adjustable physicochem. properties and protein mimicry.

Polymer Chemistry published new progress about Cytotoxicity. 950846-89-6 belongs to class indole-building-block, and the molecular formula is C30H36N4O2, COA of Formula: C30H36N4O2.

Referemce:
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

Boldron, Christophe; Besse, Angelina; Bordes, Marie-Francoise; Tissandie, Stephanie; Yvon, Xavier; Gau, Benjamin; Badorc, Alain; Rousseaux, Tristan; Barre, Guillaume; Meneyrol, Jerome; Zech, Gernot; Nazare, Marc; Fossey, Valerie; Pflieger, Anne-Marie; Bonnet-Lignon, Sandrine; Millet, Laurence; Briot, Christophe; Dol, Frederique; Herault, Jean-Pascal; Savi, Pierre; Lassalle, Gilbert; Delesque, Nathalie; Herbert, Jean-Marc; Bono, Francoise published the artcile< N-[6-(4-Butanoyl-5-methyl-1H-pyrazol-1-yl)pyridazin-3-yl]-5-chloro-1-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-1H-indole-3-carboxamide (SAR216471), a Novel Intravenous and Oral, Reversible, and Directly Acting P2Y12 Antagonist>, Safety of 5-Fluoro-1H-indole-3-carboxylic acid, the main research area is indolecarboxamide preparation purinoceptor antagonist anticoagulant antithrombotic thrombosis blood coagulation.

In the search of a potential backup for clopidogrel, the authors have initiated a HTS campaign designed to identify novel reversible P2Y12 antagonists. Starting from a hit with low micromolar binding activity, the authors report here the main steps of the optimization process leading to the identification of the preclin. candidate SAR216471, I. It is a potent, highly selective, and reversible P2Y12 receptor antagonist and by far the most potent inhibitor of ADP-induced platelet aggregation among the P2Y12 antagonists described in the literature. I displays potent in vivo antiplatelet and antithrombotic activities and has the potential to differentiate from other antiplatelet agents.

Journal of Medicinal Chemistry published new progress about Anticoagulants. 23077-43-2 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Safety of 5-Fluoro-1H-indole-3-carboxylic acid.

Referemce:
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

Hopkins, Megan D.; Abebe, Felagot A.; Scott, Kristina A.; Ozmer, Garett L.; Sheir, Alec A.; Schroeder, Lucas J.; Sheaff, Robert J.; Lamar, Angus A. published the artcile< Synthesis and identification of heteroaromatic N-benzyl sulfonamides as potential anticancer agents>, SDS of cas: 4771-48-6, the main research area is heteroaromatic Nbenzyl sulfonamide preparation anticancer.

A new approach for regioselective incorporation of a sulfonamide unit to heteroarene scaffolds has been developed and is reported within. As a result, a variety of primary benzylic N-alkylsulfonamides have been prepared via a two-step (one pot) formation from the in situ reduction of an intermediate N-sulfonyl imine under mild, practical conditions. The compounds have been screened against a variety of cell lines for cytotoxicity effects using a Cell Titer Blue assay. The cell viability investigation identifies a subset of N-benzylic sulfonamides derived from the indole scaffold to be targeted for further development into novel mols. with potential therapeutic value. The most cytotoxic of the compounds prepared, I (R1 = Me, R2,R3 = H; R4 = 4-ClC6H4), exhibited higher potency than other well-known anticancer agents Indisulam and ABT-751.

Organic & Biomolecular Chemistry published new progress about Antitumor agents. 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, SDS of cas: 4771-48-6.

Referemce:
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

Lin, Hui-Shan; Chen, Shu-Jun; Huang, Jing-Mei published the artcile< Electrosynthesis of (hetero)aryl nitriles from α-imino-oxy acids via oxidative decarboxylation/N-O cleavage>, Category: indole-building-block, the main research area is indolylemthyliminooxy acid electrochem oxidative decarboxylation cleavage; indolyl carbonitrile preparation.

A new method for the synthesis of (hetero)aryl nitriles via iminyl radicals was developed through the electrochem. oxidative decarboxylation of α-imino-oxy acids. This protocol provides an efficient approach to nitriles with a broad range of functional-group tolerance under ambient conditions and can be applied for one-pot gram-scale synthesis.

Chemical Communications (Cambridge, United Kingdom) published new progress about Aromatic nitriles Role: SPN (Synthetic Preparation), PREP (Preparation). 4771-48-6 belongs to class indole-building-block, and the molecular formula is C10H9NO, Category: indole-building-block.

Referemce:
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

Morigi, Rita; Locatelli, Alessandra; Leoni, Alberto; Rambaldi, Mirella; Bortolozzi, Roberta; Mattiuzzo, Elena; Ronca, Roberto; Maccarinelli, Federica; Hamel, Ernest; Bai, Ruoli; Brancale, Andrea; Viola, Giampietro published the artcile< Synthesis, in-vitro and in-vivo biological evaluation of substituted 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones as new potent anticancer agents>, Related Products of 20870-77-3, the main research area is imidazothiazolylmethylene indolinone preparation antitumor activity SAR cytotoxicity apoptosis; 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones; Antiproliferative; Antitumor; Apoptosis; Synthesis.

A small library of 3-(5-imidazo[2,1-b]thiazolylmethylene)-2-indolinones were synthesized and screened according to protocols available at the National Cancer Institute (NCI). Some derivatives were potent antiproliferative agents, showing GI50 values in the nanomolar range. Remarkably, when most active compounds against leukemia cells were tested in human peripheral blood lymphocytes from healthy donors, were 100-200 times less cytotoxic. Some compounds, selected by the Biol. Evaluation Committee of NCI, were examined to determine tubulin assembly inhibition. Furthermore, flow cytometric studies performed on HeLa, HT-29, and A549 cells, showed that compounds and caused a block in the G2/M phase. Interestingly, these derivatives induced apoptosis through the mitochondrial death pathway, causing in parallel significant activation of both caspase-3 and -9, PARP cleavage and down-regulation of the anti-apoptotic proteins Bcl-2 and Mcl-1. Finally, compound was also tested in-vivo in the murine BL6-B16 melanoma and E0771 breast cancer cells, causing in both cases a significant reduction in tumor volume

European Journal of Medicinal Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 20870-77-3 belongs to class indole-building-block, and the molecular formula is C8H6ClNO, Related Products of 20870-77-3.

Referemce:
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

Cockerill, G. Stuart; Angell, Richard M.; Bedernjak, Alexandre; Chuckowree, Irina; Fraser, Ian; Gascon-Simorte, Jose; Gilman, Morgan S. A.; Good, James A. D.; Harland, Rachel; Johnson, Sara M.; Ludes-Meyers, John H.; Littler, Edward; Lumley, James; Lunn, Graham; Mathews, Neil; McLellan, Jason S.; Paradowski, Michael; Peeples, Mark E.; Scott, Claire; Tait, Dereck; Taylor, Geraldine; Thom, Michelle; Thomas, Elaine; Villalonga Barber, Carol; Ward, Simon E.; Watterson, Daniel; Williams, Gareth; Young, Paul; Powell, Kenneth published the artcile< Discovery of Sisunatovir (RV521), an Inhibitor of Respiratory Syncytial Virus Fusion>, Reference of 20870-77-3, the main research area is Sisunatovir analog drug discovery synthesis RSV antiviral.

RV521 is an orally bioavailable inhibitor of respiratory syncytial virus (RSV) fusion that was identified after a lead optimization process based upon hits that originated from a phys. property directed hit profiling exercise at Reviral. This exercise encompassed collaborations with a number of contract organizations with collaborative medicinal chem. and virol. during the optimization phase in addition to those utilized as the compound proceeded through preclin. and clin. evaluation. RV521 exhibited a mean IC50 of 1.2 nM against a panel of RSV A and B laboratory strains and clin. isolates with antiviral efficacy in the Balb/C mouse model of RSV infection. Oral bioavailability in preclin. species ranged from 42 to >100% with evidence of highly efficient penetration into lung tissue. In healthy adult human volunteers exptl. infected with RSV, a potent antiviral effect was observed with a significant reduction in viral load and symptoms compared to placebo.

Journal of Medicinal Chemistry published new progress about Antiviral agents. 20870-77-3 belongs to class indole-building-block, and the molecular formula is C8H6ClNO, Reference of 20870-77-3.

Referemce:
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