Category: 7524-52-9

Chartier, Magali; Desgagne, Michael; Sousbie, Marc; Rumsby, Charles; Chevillard, Lucie; Theroux, Lea; Haroune, Lounes; Cote, Jerome; Longpre, Jean-Michel; Boudreault, Pierre-Luc; Marsault, Eric; Sarret, Philippe published the article 《Pharmacodynamic and pharmacokinetic profiles of a neurotensin receptor type 2 (NTS2) analgesic macrocyclic analog》. Keywords: neurotensin receptor cyclic peptide pharmacodynamic pharmacokinetic profile analgesic; Analgesia; Macrocycle; Metabolic stability; Opioid-sparing effects; Pain.They researched the compound: H-Trp-OMe.HCl( cas:7524-52-9 ).Quality Control of H-Trp-OMe.HCl. 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:7524-52-9) here.

The current opioid crisis highlights the urgent need to develop safe and effective pain medications. Thus, neurotensin (NT) compounds represent a promising approach, as the antinociceptive effects of NT are mediated by activation of the two G protein-coupled receptor subtypes (i.e., NTS1 and NTS2) and produce potent opioid-independent analgesia. Here, we describe the synthesis and pharmacodynamic and pharmacokinetic properties of the first constrained NTS2 macrocyclic NT(8-13) analog. The Tyr11 residue of NT(8-13) was replaced with a Trp residue to achieve NTS2 selectivity, and a rationally designed side-chain to side-chain macrocyclization reaction was applied between Lys8 and Trp11 to constrain the peptide in an active binding conformation and limit its recognition by proteolytic enzymes. The resulting macrocyclic peptide, CR-01-64, exhibited high-affinity for NTS2 (Ki 7.0 nM), with a more than 125-fold selectivity over NTS1, as well as an improved plasma stability profile (t1/2 > 24 h) compared with NT (t1/2 ∼ 2 min). Following intrathecal administration, CR-01-64 exerted dose-dependent and long-lasting analgesic effects in acute (ED50 = 4.6 μg/kg) and tonic (ED50 = 7.1 μg/kg) pain models as well as strong mech. anti-allodynic effects in the CFA-induced chronic inflammatory pain model. Of particular importance, this constrained NTS2 analog exerted potent nonopioid antinociceptive effects and potentiated opioid-induced analgesia when combined with morphine. At high doses, CR-01-64 did not cause hypothermia or ileum relaxation, although it did induce mild and short-term hypotension, all of which are physiol. effects associated with NTS1 activation. Overall, these results demonstrate the strong therapeutic potential of NTS2-selective analogs for the management of pain.

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In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called Incorporation of the pentafluorosulfanyl group through common synthetic transformations, published in 2021-04-30, which mentions a compound: 7524-52-9, mainly applied to amino acid pentafluorosulfanyl synthesis synthon; amide coupling reaction mechanism reductive amination; Click chem azide alkyne cycloaddition copper catalyst, Related Products of 7524-52-9.

The incorporation of SF5 group into model amino acids has been achieved using com. available synthons substituted with this group. This work investigates the influence of the -SF5 group on a variety of common synthetic transformations utilized in fields of bioconjugation and drug development, namely, amide coupling, reductive amination, diazo-coupling, and CuAAC “”Click”” reactions. The influence of the novel substituent on the success of these common transformations is presented, and alternative approaches for those which proved unsatisfactory are proposed herein.

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Recommanded Product: 7524-52-9. 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: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about KI-assisted Sulfur Activation/Insertion/Denitration Strategy towards Dual C-S Bond Formation for One-pot Synthesis of β-Carboline-tethered 2-Acylbenzothiophenes. Author is Singh, Manpreet; Jamra., Rahul; Paul, Avijit K.; Malakar, Chandi C.; Singh, Virender.

A simple and efficient KI promoted sulfur activation-insertion/de-nitration strategy has been developed for the synthesis of β-carboline C1 tethered 2-acylbenzothiophenes via one-pot assembly of 1-acetyl β-carbolines (an alkaloid based scaffold), 2-nitrobenzaldehydes and elemental sulfur. This expeditious reaction proceeds through the formation of β-carboline linked nitro-chalcones followed by embodiment of elemental sulfur to generate the multifunctional β-carboline linked benzothiophene derivatives The highlighted features of this efficient methodol. are transition metal-free conditions, use of inexpensive and non-toxic catalyst, easy procedure, short reaction time, and broad substrate scope with good yields. The scope of this protocol has been extended for the synthesis of a range of novel compounds with significant diversity.

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The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: H-Trp-OMe.HCl( cas:7524-52-9 ) is researched.Product Details of 7524-52-9.Dong, Weizhe; Badir, Shorouk O.; Zhang, Xuange; Molander, Gary A. published the article 《Accessing Aliphatic Amines in C-C Cross-Couplings by Visible Light/Nickel Dual Catalysis》 about this compound( cas:7524-52-9 ) in Organic Letters. Keywords: trimethylsilylmethanamine aryl bromide nickel catalyst regioselective aminoalkylation; aryl methanamine preparation. Let’s learn more about this compound (cas:7524-52-9).

A general aminoalkylation of aryl halides were developed, overcoming intolerance of free amines in nickel-mediated C-C coupling. This transformation features broad functional group tolerance and high efficiency. Taking advantage of the fast desilylation of α-silylamines upon single-electron transfer (SET) facilitated by carbonate, α-amino radicals were generated regioselectively, which then engage in nickel-mediated C-C coupling. The reaction displays high chemoselectivity for C-C over C-N bond formation. Highly functionalized pharmacophores and peptides were also amenable.

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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 Copper-promoted N-arylation of the imidazole side chain of protected histidine by using triarylbismuth reagents, published in 2021-09-20, which mentions a compound: 7524-52-9, Name is H-Trp-OMe.HCl, Molecular C12H15ClN2O2, Electric Literature of C12H15ClN2O2.

The N-arylation of the side chain of histidine by using triarylbismuthines is reported. The reaction is promoted by copper(II) acetate in dichloromethane at 40°C under oxygen in the presence of diisopropylethylamine and 1,10-phenanthroline and allows the transfer of aryl groups with substituents at any position of the aromatic ring. The reaction shows excellent functional group tolerance and is applicable to dipeptides where the histidine is located at the N terminus. A histidine-guided backbone N-H arylation was observed in dipeptides where the histidine occupies the C terminus.

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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: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Unprecedented Intramolecular Association-Induced Fluorescence in Tryptophan-Conjugated Peptidomimetics.Electric Literature of C12H15ClN2O2.

We report herewith tryptophan (Trp)-conjugated peptidomimetics that show intramol. through-space association between the Trp units. Our investigation revealed that the proximal placement of Trp can lead to the emergence of a new and unanticipated fluorescent entity constituting a Trp-Trp dimer. Proton-induced modulation of fluorescence is a consequence of this work. Investigations with control compounds unequivocally revealed that the fluorescence property is not originated from the localized excited state but from the unprecedented Trp-Trp intramol. dimer in the ground state itself. The present findings will initiate the biophys. scientists to have a relook at the fluorescence properties of Trp-containing proteins.

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1,3-Benzodioxole – Wikipedia,
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Formula: C12H15ClN2O2. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Cu-Catalyzed site-selective C(sp2)-H radical trifluoromethylation of tryptophan-containing peptides. Author is Guerrero, Itziar; Correa, Arkaitz.

Site-selective functionalization of C-H bonds within a peptide framework poses a challenging task of paramount synthetic relevance. Herein, we report an operationally simple C(sp2)-H trifluoromethylation of tryptophan (Trp)-containing peptides. This fluorination technique is characterized by its chirality preservation, tolerance of functional groups, and scalability and exhibits chemoselectivity for Trp residues over other amino acid and heterocyclic units. As a result, it represents a sustainable tool toward the late-stage peptide modification and protein engineering.

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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: 7524-52-9, is researched, Molecular C12H15ClN2O2, about Pharmacodynamic and pharmacokinetic profiles of a neurotensin receptor type 2 (NTS2) analgesic macrocyclic analog, the main research direction is neurotensin receptor cyclic peptide pharmacodynamic pharmacokinetic profile analgesic; Analgesia; Macrocycle; Metabolic stability; Opioid-sparing effects; Pain.Application In Synthesis of H-Trp-OMe.HCl.

The current opioid crisis highlights the urgent need to develop safe and effective pain medications. Thus, neurotensin (NT) compounds represent a promising approach, as the antinociceptive effects of NT are mediated by activation of the two G protein-coupled receptor subtypes (i.e., NTS1 and NTS2) and produce potent opioid-independent analgesia. Here, we describe the synthesis and pharmacodynamic and pharmacokinetic properties of the first constrained NTS2 macrocyclic NT(8-13) analog. The Tyr11 residue of NT(8-13) was replaced with a Trp residue to achieve NTS2 selectivity, and a rationally designed side-chain to side-chain macrocyclization reaction was applied between Lys8 and Trp11 to constrain the peptide in an active binding conformation and limit its recognition by proteolytic enzymes. The resulting macrocyclic peptide, CR-01-64, exhibited high-affinity for NTS2 (Ki 7.0 nM), with a more than 125-fold selectivity over NTS1, as well as an improved plasma stability profile (t1/2 > 24 h) compared with NT (t1/2 ∼ 2 min). Following intrathecal administration, CR-01-64 exerted dose-dependent and long-lasting analgesic effects in acute (ED50 = 4.6 μg/kg) and tonic (ED50 = 7.1 μg/kg) pain models as well as strong mech. anti-allodynic effects in the CFA-induced chronic inflammatory pain model. Of particular importance, this constrained NTS2 analog exerted potent nonopioid antinociceptive effects and potentiated opioid-induced analgesia when combined with morphine. At high doses, CR-01-64 did not cause hypothermia or ileum relaxation, although it did induce mild and short-term hypotension, all of which are physiol. effects associated with NTS1 activation. Overall, these results demonstrate the strong therapeutic potential of NTS2-selective analogs for the management of pain.

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1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem

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: 7524-52-9, is researched, SMILESS is N[C@@H](CC1=CNC2=CC=CC=C12)C(OC)=O.[H]Cl, Molecular C12H15ClN2O2Journal, Article, Langmuir called Rational Design of Chiral Nanohelices from Self-Assembly of Meso-tetrakis (4-Carboxyphenyl) Porphyrin-Amino Acid Conjugates, Author is Yang, Xuejiao; Shen, Yuhe; Liu, Jiayu; Wang, Yuefei; Qi, Wei; Su, Rongxin; He, Zhimin, the main research direction is chiral nanohelices mesotetrakiscarboxyphenyl Porphyrin Amino Acid Conjugates.Recommanded Product: 7524-52-9.

In this article, meso-tetrakis (4-carboxyphenyl) porphyrins modified with different amino acids were designed, synthesized, and researched. The chiral self-assembly behavior of these porphyrin-amino acid mols. can be precisely controlled by adjusting the pH, constituent amino acids, and temperature, thereby giving rise to chiral nanostructures with precisely tailored helical pitch and handedness. This research provides a certain reference for the design and preparation of chiral nanomaterials and has potential application prospects in chiral resolution and chiral catalysis.

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SDS of cas: 7524-52-9. 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: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Synthesis of Four Optical Isomers of Antiviral Agent NK0209 and Determination of Their Configurations and Activities against a Plant Virus.

Previously, we reported for the first time that harmala alkaloids harmine and tetrahydroharmine exhibit activity against plant viruses, and we developed an analog, designated NK0209, that efficiently prevents and controls plant virus diseases. Here, to investigate the influence of the spatial configuration of NK0209 on its antiviral activities, we synthesized its four optical isomers, determined their configurations, and evaluated their activities against tobacco mosaic virus. All four isomers were significantly more active than ningnanmycin, which is one of the most successful com. antiviral agents, with in vivo inactivation, cure, and protection rates of 57.3±1.9%, 54.2±3.3%, 55.0±4.1% at 500μg/mL. Furthermore, anal. of structure-activity relationships demonstrated for the first time that the spatial conformation of NK0209 is an important determinant of its antiviral activity, and our results provide information about the possible optimum configuration for interaction of this mol. with its target protein.

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1,3-Benzodioxole – Wikipedia,
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