Tag: 200-300

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 an article in 2021. The article was titled 《Pharmacodynamic and pharmacokinetic profiles of a neurotensin receptor type 2 (NTS2) analgesic macrocyclic analog》, and you may find the article in Biomedicine & Pharmacotherapy.Application In Synthesis of H-Trp-OMe.HCl The information in the text is summarized as follows:

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. In the experiment, the researchers used H-Trp-OMe.HCl(cas: 7524-52-9Application In Synthesis of H-Trp-OMe.HCl)

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.Application In Synthesis of H-Trp-OMe.HCl

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Fan, Yan-Ru; Wang, Bo-Jin; Jia, Deng-Guo; Yang, Xin-Bin; Huang, Yu published an article in 2021. The article was titled 《Synthesis, electrochemistry, DNA binding and in vitro cytotoxic activity of tripodal ferrocenyl bis-naphthalimide derivatives》, and you may find the article in Journal of Inorganic Biochemistry.Recommanded Product: tert-Butyl (5-aminopentyl)carbamate The information in the text is summarized as follows:

Tripodal ferrocenyl bis-naphthalimide derivatives were synthesized and characterized. All of the bis-naphthalimide derivatives exhibited good DNA binding ability which was confirmed by ethidium bromide (EB) displacement experiment and UV-visible absorption titration The binding mode of these compounds is a hybrid binding mode. The cytotoxicity of the synthesized compounds against 4 different human cancer cell lines (EC109, BGC823, SGC7901 and HEPG2) was evaluated by thiazolyl blue tetrazolium bromide (MTT) assay. All of the bis-naphthalimide derivatives exhibited better anticancer activity than the pos. control drug (amonafide), which was due to the promotion of reactive O species (ROS) level in test cancer cells by the reversible 1-electron redox process of ferrocenyl bis-naphthalimide derivatives Although there was no obvious relation between the binding constants and the chain length between ferrocenyl and naphthalimides, the structure cytotoxicity relation revealed that one compound was the best choice for the tested tripodal bis-naphthalimide derivatives In the experiment, the researchers used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Recommanded Product: tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Recommanded Product: tert-Butyl (5-aminopentyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Kuriyama, Yuse; Sasano, Yusuke; Hoshino, Yoshihiko; Uesugi, Shun-ichiro; Yamaichi, Aoto; Iwabuchi, Yoshiharu published an article in 2021. The article was titled 《Highly Regioselective 5-endo-tet Cyclization of 3,4-Epoxy Amines into 3-Hydroxypyrrolidines Catalyzed by La(OTf)3》, and you may find the article in Chemistry – A European Journal.Synthetic Route of C10H22N2O2 The information in the text is summarized as follows:

Highly regioselective intramol. aminolysis of 3,4-epoxy amines was achieved. Key features of this reaction were (1) chemoselective activation of epoxides in the presence of unprotected aliphatic amines in the same mols. by a La(OTf)3 catalyst and (2) excellent regioselectivity for anti-Baldwin 5-endo-tet cyclization. This reaction afforded 3-hydroxy-2-alkylpyrrolidines stereospecifically in high yields. DFT calculations revealed that the regioselectivity might be attributed to distortion energies of epoxy amine substrates. The use of this reaction was demonstrated by the first enantioselective synthesis of an antispasmodic agent prifinium bromide. The experimental process involved the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Synthetic Route of C10H22N2O2)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Synthetic Route of C10H22N2O2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

《Visible-light mediated tryptophan modification in oligopeptides employing acylsilanes》 was written by Reimler, Jannik; Studer, Armido. Name: H-Trp-OMe.HCl And the article was included in Chemistry – A European Journal in 2021. The article conveys some information:

A method for the selective tryptophan modification and labeling of tryptophan-containing peptides is described. Photoirradiation of acylsilanes generates reactive siloxycarbenes which undergo H-N-insertion into the indole moiety of tryptophan to give stable silyl protected hemiaminals. This method is successfully applied to chem. modify various tryptophan containing oligopeptides. The method enables the selective introduction of alkynes to peptides that are eligible for further alkyne-azide click chem. In addition, the dansyl fluorophore can be conjugated to a peptide using this approach. The results came from multiple reactions, including the reaction of H-Trp-OMe.HCl(cas: 7524-52-9Name: H-Trp-OMe.HCl)

H-Trp-OMe.HCl(cas:7524-52-9) is one of amino acid derivatives. Amino acid derivatives represent an important category of skin penetration promoters. These compounds possess hydrophobic chains attached to an amino acid headgroup via a biodegradable ester bond. Due to the amphiphilic nature of these derivatives, it is possible for them to enter into the SC lipid barrier and significantly disorganize skin membrane lipids.Name: H-Trp-OMe.HCl

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Recommanded Product: tert-Butyl (5-aminopentyl)carbamateIn 2021 ,《Sulfur Oxidation Increases the Rate of HIRE-Type [1.4]Thiazepinone Ring Expansion and Influences the Conformation of a Medium-Sized Heterocyclic Scaffold》 was published in Journal of Organic Chemistry. The article was written by Reutskaya, Elena; Sapegin, Alexander; Peintner, Stefan; Erdelyi, Mate; Krasavin, Mikhail. The article contains the following contents:

The hydrated imidazoline ring expansion (HIRE-type) reaction was investigated for a series of di(hetero)arene-fused [1.4]thiazepinones in comparison with their sulfone counterparts. The sulfones were found to undergo ring expansion at a much higher rate compared to the thioethers, much in line with the current mechanistic understanding of the process. Moreover, the amide bond cis- and trans-isomers of the ring-expanded products were found, in the case of sulfones, to be stabilized through an intramol. hydrogen bond. The latter phenomenon was studied in detail by NMR experiments and corroborated by X-ray crystallog. information. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Recommanded Product: tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Recommanded Product: tert-Butyl (5-aminopentyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Reference of tert-Butyl (5-aminopentyl)carbamateIn 2019 ,《Identification of Diketopiperazine-Containing 2-Anilinobenzamides as Potent Sirtuin 2 (SIRT2)-Selective Inhibitors Targeting the “”Selectivity Pocket””, Substrate-Binding Site, and NAD+-Binding Site》 was published in Journal of Medicinal Chemistry. The article was written by Mellini, Paolo; Itoh, Yukihiro; Elboray, Elghareeb E.; Tsumoto, Hiroki; Li, Ying; Suzuki, Miki; Takahashi, Yukari; Tojo, Toshifumi; Kurohara, Takashi; Miyake, Yuka; Miura, Yuri; Kitao, Yuki; Kotoku, Masayuki; Iida, Tetsuya; Suzuki, Takayoshi. The article contains the following contents:

The NAD+-dependent deacetylase SIRT2 represents an attractive target for drug development. Here, we designed and synthesized drug-like SIRT2-selective inhibitors based on an anal. of the putative binding modes of recently reported SIRT2-selective inhibitors and evaluated their SIRT2-inhibitory activity. This led us to develop a more drug-like diketopiperazine structure as a “”hydrogen bond (H-bond) hunter”” to target the substrate-binding site of SIRT2. Thioamide 53, a conjugate of diketopiperazine and 2-anilinobenzamide which is expected to occupy the “”selectivity pocket”” of SIRT2, exhibited potent SIRT2-selective inhibition. Inhibition of SIRT2 by 53 was mediated by the formation of a 53-ADP-ribose conjugate, suggesting that 53 is a mechanism-based inhibitor targeting the “”selectivity pocket””, substrate-binding site, and NAD+-binding site. Furthermore, 53 showed potent antiproliferative activity toward breast cancer cells and promoted neurite outgrowth of Neuro-2a cells. These findings should pave the way for the discovery of novel therapeutic agents for cancer and neurol. disorders. After reading the article, we found that the author used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Reference of tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Reference of tert-Butyl (5-aminopentyl)carbamate

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2017,Newton, Ana S.; Deiana, Luca; Puleo, David E.; Cisneros, Jose A.; Cutrona, Kara J.; Schlessinger, Joseph; Jorgensen, William L. published 《JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules》.ACS Medicinal Chemistry Letters published the findings.Computed Properties of C10H22N2O2 The information in the text is summarized as follows:

A competitive fluorescence polarization (FP) assay is reported for determining binding affinities of probe mols. with the pseudokinase JAK2 JH2 allosteric site. The syntheses of the fluorescent 5 and 6 used in the assay are reported as well as Kd results for 10 compounds, including JNJ7706621, NVP-BSK805, and filgotinib (GLPG0634). X-ray crystal structures of JAK2 JH2 in complex with NVP-BSK805, filgotinib, and diaminopyrimidine 8 elucidate the binding poses.tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Computed Properties of C10H22N2O2) was used in this study.

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Computed Properties of C10H22N2O2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Korhonen, Ilpo O. O.; Lind, Maija A. published an article in Journal of Chromatography. The title of the article was 《Gas-liquid chromatographic analyses. XLII. Retention behavior of C1-C12 n-alkyl esters of benzoic and pentafluorobenzoic acids on SE-30 and OV-351 capillary columns》.Application In Synthesis of Ethyl 2,3,4,5,6-pentafluorobenzoate The author mentioned the following in the article:

The gas chromatog. separation of a mixture of C1-12 n-alkyl esters of benzoic and pentafluorobenzoic acids on low-polarity (SE-30) and highly polar (OV-351) capillary columns is described. The Kovats’ retention indexes for the fluorinated isomers are given. The results are compared with those reported by K. and L. (1985) for the corresponding n-alkyl benzoates by showing the retention index increments owing to the perfluoro substitution in the acyl chain at a variety of temperatures The results came from multiple reactions, including the reaction of Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4Application In Synthesis of Ethyl 2,3,4,5,6-pentafluorobenzoate)

Ethyl 2,3,4,5,6-pentafluorobenzoate(cas: 4522-93-4) belongs to esters. They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Application In Synthesis of Ethyl 2,3,4,5,6-pentafluorobenzoate They perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Hinkes, Stefan; Wuttke, Andre; Saupe, Sebastian M.; Ivanova, Teodora; Wagner, Sebastian; Knoerlein, Anna; Heine, Andreas; Klebe, Gerhard; Steinmetzer, Torsten published an article in Journal of Medicinal Chemistry. The title of the article was 《Optimization of Cyclic Plasmin Inhibitors: From Benzamidines to Benzylamines》.Product Details of 67877-95-6 The author mentioned the following in the article:

New macrocyclic plasmin inhibitors based on our previously optimized P2-P3 core segment have been developed. In the first series, the P4 residue was modified, whereas the 4-amidinobenzylamide in P1 position was maintained. The originally used P4 benzylsulfonyl residue could be replaced by various sulfonyl- or urethane-like protecting groups. In the second series, the P1 benzamidine was modified and a strong potency and excellent selectivity was retained by incorporation of p-xylenediamine. Several analogs inhibit plasmin in the subnanomolar range, and their potency against related trypsin-like serine proteases including trypsin itself could be further reduced. Selected derivatives have been tested in a plasma fibrinolysis assay and are more effective than the reference inhibitor aprotinin. The crystal structure of one inhibitor was determined in complex with trypsin. The binding mode reveals a sterical clash of the inhibitor’s linker segment with the 99-hairpin loop of trypsin, which is absent in plasmin. In the experiment, the researchers used H-D-Phe(4-NO2)-OMe.HCl(cas: 67877-95-6Product Details of 67877-95-6)

H-D-Phe(4-NO2)-OMe.HCl(cas: 67877-95-6) belongs to esters. They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Product Details of 67877-95-6 Polyesters are important plastics, with monomers linked by ester moieties.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

COA of Formula: C10H22N2O2In 2021 ,《Next generation Glucose-1-phosphate thymidylyltransferase (RmlA) inhibitors: An extended SAR study to direct future design》 was published in Bioorganic & Medicinal Chemistry. The article was written by Xiao, Ganyuan; Alphey, Magnus S.; Tran, Fanny; Pirrie, Lisa; Milbeo, Pierre; Zhou, Yi; Bickel, Jasmine K.; Kempf, Oxana; Kempf, Karl; Naismith, James H.; Westwood, Nicholas J.. The article contains the following contents:

The monosaccharide L-Rhamnose is an important component of bacterial cell walls. The first step in the L-rhamnose biosynthetic pathway is catalyzed by glucose-1-phosphate thymidylyltransferase (RmlA), which condenses glucose-1-phosphate (Glu-1-P) with deoxythymidine triphosphate (dTTP) to yield dTDP-D-glucose. In addition to the active site where catalysis of this reaction occurs, RmlA has an allosteric site that is important for its function. Building on previous reports, SAR studies have explored further the allosteric site, leading to the identification of very potent P. aeruginosa RmlA inhibitors. Modification at the C6-NH2 of the inhibitor′s pyrimidinedione core structure was tolerated. X-ray crystallog. anal. of the complexes of P. aeruginosa RmlA with the novel analogs revealed that C6-aminoalkyl substituents can be used to position a modifiable amine just outside the allosteric pocket. This opens up the possibility of linking a siderophore to this class of inhibitor with the goal of enhancing bacterial cell wall permeability. In the experiment, the researchers used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3COA of Formula: C10H22N2O2)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).COA of Formula: C10H22N2O2

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics