Category: chiral-nitrogen-ligands

Product Details of 1663-45-2. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 1,2-Bis(diphenylphosphino)ethane, is researched, Molecular C26H24P2, CAS is 1663-45-2, about Protective cellular immune response induction for cutaneous leishmaniasis by a new immunochemotherapy schedule. Author is Da Silva, Danielle A. M.; Santana, Fabiana R.; Katz, Simone; Garcia, Daniel M.; Teixeira, Daniela; Longo-Maugeri, Ieda M.; Barbieri, Clara L..

The palladacycle complex DPPE 1.2 was previously shown to inhibit Leishmania (Leishmania) amazonensis infection in vitro and in vivo. The present study aimed to evaluate the effect of DPPE 1.2 associated with a recombinant cysteine proteinase, rLdccys1, and the adjuvant Propionibacterium acnes on L. (L.) amazonensis infection in two mouse strains, BALB/c, and C57BL/6. Treatment with this association potentiated the leishmanicidal effect of DPPE 1.2 resulting in a reduction of parasite load in both strains of mice which was higher compared to that found in groups treated with either DPPE 1.2 alone or associated with P. acnes or rLdccys1. The reduction of parasite load in both mice strains was followed by immunomodulation mediated by an increase of memory CD4+ and CD8+ T lymphocytes, IFN-γ levels and reduction of active TGF-β in treated animals. No infection relapse was observed 1 mo after the end of treatment in mice which received DPPE 1.2 associated with rLdccys1 or rLdccys1 plus P. acnes in comparison to that exhibited by animals treated with DPPE 1.2 alone. Evaluation of serum levels of AST, ALT, urea, and creatinine showed no alterations among treated groups, indicating that this treatment schedule did not induce hepato or nephrotoxicity. These data indicate the potential use of this association as a therapeutic alternative for cutaneous leishmaniasis caused by L. (L) amazonensis.

Although many compounds look similar to this compound(1663-45-2)Product Details of 1663-45-2, numerous studies have shown that this compound(SMILES:P(CCP(C1=CC=CC=C1)C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

In general, if the atoms that make up the ring contain heteroatoms, such rings become heterocycles, and organic compounds containing heterocycles are called heterocyclic compounds. An article called Synthesis and characterization of cationic quaternary ammonium geminis (16-s-16) and their role in ninhydrin-[Cu(II)-His]+ reaction, published in 2021, which mentions a compound: 111-24-0, Name is 1,5-Dibromopentane, Molecular C5H10Br2, Related Products of 111-24-0.

Cationic quaternary ammonium gemini surfactants were synthesized by mixing N,N-dimethylcetylamine and α,ω-dibromoalkane. The synthesized products were characterized by C, H, N elemental and 1H NMR analyses. The critical micelle concentration (CMC) of these surfactants with and without additives was calculated by means of the conductivity technique. The role of the synthesized quaternary ammonium geminis in the reaction was investigated by a UV-vis spectroscopy. The rate constant (kψ) was determined at different gemini concentrations and plotted graphically as kψ vs. [16-s-16]. Addnl., the influence of other reaction parameters (viz., reactants, pH, and temperature) was investigated. The binding constants were also determined (KA for [Cu(II)-His]+ and KB for ninhydrin). The resulting kψ-[16-s-16] plot can be understood in terms of a pseudo-phase model of micelles.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 1,5-Dibromopentane, is researched, Molecular C5H10Br2, CAS is 111-24-0, about Efficient synthesis of isosorbide-based polycarbonate with scalable dicationic ionic liquid catalysts by balancing the reactivity of the endo-OH and exo-OH.Formula: C5H10Br2.

In this study, a series of high-activity imidazole-based dicationic ionic liquids (DILs) were designed and prepared as efficient catalysts for balancing the reactivity between the endo-hydroxyl group (endo-OH) and the exo-hydroxyl group (exo-OH) of isosorbide (ISO) to synthesize high mol. weight poly(isosorbide carbonate) (PIC). Meanwhile, the thermal performance of PIC was precisely optimized by regulating the chain configuration. When the trace amounts (4.5 x 10-5 based on the ISO molar amount) of bis-(3-methyl-1-imidazole)-ethylene dibromide ([C2(Min)2][Br]2) were used, the weight average mol. weight (Mw) of PIC reached 98 700 g mol-1. It could be concluded from the results of the experiment and the stimulation that the high catalytic activity of DILs was attributed to the strong electrostatic interaction between the cation and the substrate and the effective balance of the reactivity of the endo-OH and the exo-OH. Furthermore, we found that the reduction of hydroxyl groups in the terminal groups and the increase of endo-endo (a1) structure in the repeating unit improved the thermal properties of PIC. Finally, 1H NMR, Fourier IR spectroscopy, and d. functional theory (DFT) calculations were used to verify the reaction process through anion and cation multi-site synergistic effect and a possible electrophilic-nucleophilic reaction mechanism was successfully obtained.

Although many compounds look similar to this compound(111-24-0)Formula: C5H10Br2, numerous studies have shown that this compound(SMILES:BrCCCCCBr), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Safety of tert-Butyl 4-hydroxy-4-(hydroxymethyl)piperidine-1-carboxylate. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: tert-Butyl 4-hydroxy-4-(hydroxymethyl)piperidine-1-carboxylate, is researched, Molecular C11H21NO4, CAS is 389889-80-9, about Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis. Author is Carpenter, Joseph; Wu, Gang; Wang, Ying; Cook, Erica M.; Wang, Tao; Sitkoff, Doree; Rossi, Karen A.; Mosure, Kathy; Zhuo, Xiaoliang; Cao, Gary G.; Ziegler, Milinda; Azzara, Anthony V.; Krupinski, Jack; Soars, Matthew G.; Ellsworth, Bruce Alan; Wacker, Dean A..

Herein we report the discovery and preclin. biol. evaluation of 6-(2-(5-cyclopropyl-3-(3,5-dichloropyridin-4-yl)isoxazol-4-yl)-7-azaspiro[3.5]non-1-en-7-yl)-4-(trifluoromethyl)quinoline-2-carboxylic acid, compound 1 (BMS-986318), a nonbile acid farnesoid X receptor (FXR) agonist. Compound 1 exhibits potent in vitro and in vivo activation of FXR, has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis. The overall profile of compound 1 supports its continued evaluation.

Although many compounds look similar to this compound(389889-80-9)Safety of tert-Butyl 4-hydroxy-4-(hydroxymethyl)piperidine-1-carboxylate, numerous studies have shown that this compound(SMILES:O=C(N1CCC(CO)(O)CC1)OC(C)(C)C), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Article, Inflammopharmacology called Immunomodulatory properties of characellide A on human peripheral blood mononuclear cells, Author is Marcella, Simone; Afoullouss, Sam; Thomas, Olivier P.; Allcock, A. Louise; Murphy, Paul V.; Loffredo, Stefania, which mentions a compound: 1663-45-2, SMILESS is P(CCP(C1=CC=CC=C1)C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4, Molecular C26H24P2, Computed Properties of C26H24P2.

Marine sponges and their associated microbiota are multicellular animals known to produce metabolites with interesting pharmacol. properties playing a pivotal role against a plethora of pathol. disorders such as infammation, cancer and infections. Characellide A and B belong to a novel class of glycolipopeptides isolated from the deep sea marine sponge Characella pachastrelloides. In this study, we have evaluated the efects of characellide A and B on cytokine and chemokine release from human peripheral blood mononuclear cells (PBMC). Characellide A induces a concentration- and time-dependent CXCL8, IL-6 and TNF-α release from PBMC. This production is mediated by the induction of gene transcription. Moreover, cytokine/chemokine release induced by characellide A from PBMC is CD1d-dependent because a CD1d antagonist, 1,2-bis(diphenylphosphino)ethane [DPPE]-polyethylene glycolmonomethylether [PEG], specifcally inhibits characellide A-induced activation of PBMC. In conclusion, characellide A is a novel modulator of adaptative/innate immune responses. Further studies are needed to understand its potential pharmacol. application.

Although many compounds look similar to this compound(1663-45-2)Computed Properties of C26H24P2, numerous studies have shown that this compound(SMILES:P(CCP(C1=CC=CC=C1)C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Most of the natural products isolated at present are heterocyclic compounds, so heterocyclic compounds occupy an important position in the research of organic chemistry. A compound: 3411-48-1, is researched, SMILESS is C1=CC2=C(C=C1)C(=CC=C2)P(C1=CC=CC2=C1C=CC=C2)C1=CC=CC2=C1C=CC=C2, Molecular C30H21PJournal, Article, Research Support, Non-U.S. Gov’t, Journal of Medicinal Chemistry called Synthesis and structure-activity analysis of new phosphonium salts with potent activity against african trypanosomes, Author is Taladriz, Andrea; Healy, Alan; Flores Perez, Eddysson J.; Herrero Garcia, Vanessa; Rios Martinez, Carlos; Alkhaldi, Abdulsalam A. M.; Eze, Anthonius A.; Kaiser, Marcel; de Koning, Harry P.; Chana, Antonio; Dardonville, Christophe, the main research direction is phosphonium salt diphosphonium benzyl phenethyl bridged preparation trypanosomicide agent; quaternization diphosphonium salt preparation trypanosomicide activity QSAR field analysis; benzyl phenethyl halide preparation quaternization phosphine phosphonium trypanosomicide activity.Application In Synthesis of Tri(naphthalen-1-yl)phosphine.

A series of 73 bisphosphonium salts [R1R2R3P+(CH2)n-1,4-C6H4-L-1,4-C6H4(CH2)nP+R1R2R3]X2 and 10 monophosphonium salt derivatives [Ph-L-1,4-C6H4CH2PR1R2R3]Br, [4-MeC6H4CH2P+Ph3]X (R1-R3 = alkyl, Ph, substituted Ph, 2-thienyl, 2-furyl, 1-naphthyl; L = CO, CH2, O, SO2, NAc; X = Cl, Br) were synthesized and tested in vitro against several wild type and resistant lines of Trypanosoma brucei (T. b. rhodesiense STIB900, T. b. brucei strain 427, TbAT1-KO, and TbB48). More than half of the compounds tested showed a submicromolar EC50 against these parasites. The compounds did not display any cross-resistance to existing diamidine therapies, such as pentamidine. In most cases, the compounds displayed a good selectivity index vs. human cell lines. None of the known T. b. brucei drug transporters were required for trypanocidal activity, although some of the bisphosphonium compounds inhibited the low affinity pentamidine transporter. It was found that phosphonium drugs act slowly to clear a trypanosome population but that only a short exposure time is needed for irreversible damage to the cells. A comparative mol. field anal. model (CoMFA) was generated to gain insights into the SAR of this class of compounds, identifying key features for trypanocidal activity.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Reference of 2-Aminoquinazolin-4(3H)-one. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 2-Aminoquinazolin-4(3H)-one, is researched, Molecular C8H7N3O, CAS is 20198-19-0, about Quinazolines as inhibitors of dihydrofolate reductase. 1.

2,4-Diaminoquinazolines were potent in vitro inhibitors of rat liver dihydrofolate reductase [9002-03-3]. The most potent compound, 6-bromo-5-chloro-2,4-diaminoquinazoline (I) [41934-85-4], produced 50% inhibition at 0.10 μM, and was thus nearly as effective an inhibitor as pyrimethamine. I was prepared from 5-chloro-2,4,6-triaminoquinazoline [17511-20-5] by diazotization of the 6-amino group in 2N MeSO3H and reaction with CuBr in 50% HBr.

Although many compounds look similar to this compound(20198-19-0)Reference of 2-Aminoquinazolin-4(3H)-one, numerous studies have shown that this compound(SMILES:O=C1NC(N)=NC2=C1C=CC=C2), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Category: chiral-nitrogen-ligands. The protonation of heteroatoms in aromatic heterocycles can be divided into two categories: lone pairs of electrons are in the aromatic ring conjugated system; and lone pairs of electrons do not participate. Compound: 2-Aminoquinazolin-4(3H)-one, is researched, Molecular C8H7N3O, CAS is 20198-19-0, about Synthesis and in vitro evaluation of 2-aminoquinazolin-4(3H)-one-based inhibitors for tRNA-guanine transglycosylase (TGT). Author is Meyer, Emmanuel A.; Furler, Maya; Diederich, Francois; Brenk, Ruth; Klebe, Gerhard.

TRNA-Guanine transglycosylase (TGT) plays a key role in the post-transcriptional modification of tRNA. It has been linked with the pathogenicity of shigellae, the causative agents of bacillary dysentery (shigellosis). Here, we report structure-activity relationships (SARs) for a new series of 2-aminoquinazolin-4(3H)-one-based inhibitors of TGT, resulting from structure-based design (Fig. 2). Versatile synthetic protocols allow selective functionalization of the 2-aminoquinazolin-4(3H)-one core (Schemes 1-6) with H-bond-donor groups in position 6 (for H-bonding to the C = O group of Leu231) and lipophilic residues in position 8 for reaching into a shallow, newly discovered lipophilic pocket lined by Val282, Val45, and Leu68. The binding mode of several of these ligands in the active site of TGT was established by crystal structure analyses (Figs. 4 and 6). A dramatic S effect was observed, with the replacement of the S-atom in the (phenylsulfanyl)methyl residue in position 8 of inhibitor 1c (Ki = 100 nM) by the O-atom (in 1h, Ki = 5.6 μM) or CH2 (in 1i, Ki = 3.6 μM), resulting in a massive loss of activity (Fig. 3). Crystal structure anal. showed that the lipophilic Me group points into a highly polar region of the active site encompassed by the side chains of Asp280 and Asp102 and collides directly (d(C…O) = 3.1 Å) with one of the O-atoms of the carboxylate of Asp102. Similarly, lipophilic linkers departing from position 8 and orienting residues in the shallow hydrophobic pocket presumably encounter analogous unfavorable contacts, accounting for the modest contribution to the binding free enthalpy upon introduction of these residues. These findings provide a valuable starting point for future structure-based lead optimization cycles leading to TGT inhibitors with increased in vitro potency.

Although many compounds look similar to this compound(20198-19-0)Category: chiral-nitrogen-ligands, numerous studies have shown that this compound(SMILES:O=C1NC(N)=NC2=C1C=CC=C2), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 6684-39-5, is researched, Molecular C5H3Cl2NO2S, about Antidiabetic Disruptors of the Glucokinase-Glucokinase Regulatory Protein Complex Reorganize a Coulombic Interface, the main research direction is antidiabetic interaction coulombic interface glucokinase complex regulatory protein GKRP.SDS of cas: 6684-39-5.

The glucokinase regulatory protein (GKRP) plays an essential role in glucose homeostasis by acting as a competitive inhibitor of glucokinase (GCK) and triggering its localization to the hepatocyte nucleus upon glucose deprivation. Metabolites such as fructose 6-phosphate and sorbitol 6-phosphate promote assembly of the GCK-GKRP complex, whereas fructose 1-phosphate and functionalized piperazines with potent in vivo antidiabetic activity disrupt the complex. Here, we establish the mol. basis by which these natural and synthetic ligands modulate the GCK-GKRP interaction. We demonstrate that a small-mol. disruptor of the protein-protein interaction utilizes a two-step conformational selection mechanism to associate with a rare GKRP conformation constituting 3% of the total population. Conformational heterogeneity of GKRP is localized to the N-terminus and deleting this region eliminates the ability of sorbitol 6-phosphate to promote the GCK-GKRP interaction. Stabilizing ligands favor an extended N-terminus, which sterically positions two arginine residues for optimal coulombic interaction with a pair of carboxylate side chains from GCK. Conversely, disruptors promote a more compact N-terminus in which an interfacial arginine residue is stabilized in an unproductive orientation through a cation-π interaction with tyrosine 75. Eliminating the ability to sample this binding impaired conformation enhances the intrinsic inhibitory activity of GKRP. Elucidating the mol. basis of ligand-mediated control over the GCK-GKRP interaction is expected to impact the development and future refinement of therapeutic agents for diabetes and cardiovascular disease, which result from improper GKRP regulation of GCK.

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Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis

Anamika; Yadav, Dharmendra Kumar; Manar, Krishna K.; Yadav, Chote Lal; Kumar, Kamlesh; Ganesan, Vellaichamy; Drew, Michael G. B.; Singh, Nanhai published the article 《New heteroleptic [Ni(II) 1,1-dithiolate-phosphine] complexes: synthesis, characterization and electrocatalytic oxygen evolution studies》. Keywords: nickel dithiolatophenylcyclohexanedione bisdiphenylphosphinoethane diphenylphosphinomonosulfidemethane complex preparation redox potential; crystal structure nickel dithiolatophenylcyclohexanedione bisdiphenylphosphinoethane diphenylphosphinomonosulfidemethane complex.They researched the compound: 1,2-Bis(diphenylphosphino)ethane( cas:1663-45-2 ).Quality Control of 1,2-Bis(diphenylphosphino)ethane. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:1663-45-2) here.

Four new heteroleptic Ni() complexes with general formula [Ni()(LL’)], L = 2-(methylene-1,1′-dithiolato)-5-phenylcyclohexane-1,3-dione (L1) and 2-(methylene-1,1′-dithiolato)-5,5′-dimethylcyclohexane-1,3-dione (L2); L’ = 1,2-bis(diphenylphosphino)ethane (dppe) and bis(diphenylphosphino)monosulfide methane (dppms) were synthesized and characterized by elemental anal. and spectroscopy (IR, UV-Vis, 1H, 13C{1H} and 31P{1H} NMR). All complexes 1-4 were characterized by PXRD and single crystal X-ray crystallog. The solid state mol. structures revealed distorted square planar geometry about the four-coordinate Ni(II) metal center together with rare Ni···H-C intra/intermol. anagostic interactions in axial positions. In these complexes supramol. structures were sustained by non-covalent C-H···O, C-O···H-O, C-H···π, C-H···π (NiCS2, chelate), π···π and H···H interactions. Their electrocatalytic properties were investigated for oxygen evolution reaction (OER) in which complex 2 showed the highest activity with 10 mA cm-2 at the potential of 1.58 V vs. In addition, complex 2 also exhibits an OER onset potential at 1.52 V vs.

Although many compounds look similar to this compound(1663-45-2)Quality Control of 1,2-Bis(diphenylphosphino)ethane, numerous studies have shown that this compound(SMILES:P(CCP(C1=CC=CC=C1)C2=CC=CC=C2)(C3=CC=CC=C3)C4=CC=CC=C4), has unique advantages. If you want to know more about similar compounds, you can read my other articles.

Reference:
Chiral nitrogen ligands in late transition metal-catalysed asymmetric synthesis—I. Addressing the problem of ligand lability in rhodium-catalysed hydrosilations,
Nitrogen-Containing Ligands for Asymmetric Homogeneous and Heterogeneous Catalysis