Category: 51644-96-3

《Solid-phase synthesis of substrate-based dipeptides and heterocyclic pseudo-dipeptides as potential NO synthase inhibitors》 was written by Touati-Jallabe, Youness; Tintillier, Thibault; Mauchauffee, Elodie; Boucher, Jean-Luc; Leroy, Jeremy; Ramassamy, Booma; Hamze, Abdallah; Mezghenna, Karima; Bouzekrini, Amine; Verna, Claudia; Martinez, Jean; Lajoix, Anne-Dominique; Hernandez, Jean-Francois. Related Products of 51644-96-3 And the article was included in ChemMedChem in 2020. The article conveys some information:

More than 160 arginine analogs modified on the C-terminus via either an amide bond or a heterocyclic moiety (1,2,4-oxadiazole, 1,3,4-oxadiazole and 1,2,4-triazole) were prepared as potential inhibitors of NO synthases (NOS). A methodol. involving formation of a thiocitrulline intermediate linked through its side-chain on a solid support followed by modification of its carboxylate group was developed. Finally, the side-chain thiourea group was either let unchanged, S-alkylated (Me, Et) or guanidinylated (Me, Et) to yield resp. after TFA treatment the corresponding thiocitrulline, S-Me/Et-isothiocitrulline and N-Me/Et-arginine substrate analogs. They all were tested against three recombinant NOS isoforms. Several compounds containing a S-Et- or a S-Me-Itc moiety and mainly belonging to both the dipeptide-like and 1,2,4-oxadiazole series were shown to inhibit nNOS and iNOS with IC50 in the 1-50μM range. Spectral studies confirmed that these new compounds interacted at the heme active site. The more active compounds were found to inhibit intra-cellular iNOS expressed in RAW264.7 and INS-1 cells with similar efficiency than the reference compounds L-NIL and SEIT. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Related Products of 51644-96-3)

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).Related Products of 51644-96-3

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

The author of 《Molecular-docking-guided design and synthesis of new IAA-tacrine hybrids as multifunctional AChE/BChE inhibitors》 were Cheng, Zhi-Qiang; Zhu, Kong-Kai; Zhang, Juan; Song, Jia-Li; Muehlmann, Luis Alexandre; Jiang, Cheng-Shi; Liu, Chang-Liang; Zhang, Hua. And the article was published in Bioorganic Chemistry in 2019. Name: tert-Butyl (5-aminopentyl)carbamate The author mentioned the following in the article:

A series of new indole-3-acetic acid (IAA)-tacrine hybrids as dual acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) inhibitors were designed and prepared based on the mol. docking mode of AChE with an IAA derivative (1a), a moderate AChE inhibitor identified by screening our compound library for anti-Alzheimer’s disease (AD) drug leads. The enzyme assay results revealed that some hybrids, e.g. 5d and 5e, displayed potent dual in vitro inhibitory activities against AChE/BChE with IC50 values in low nanomolar range. Mol. modeling studies in tandem with kinetic anal. suggest that these hybrids target both catalytic active site and peripheral anionic site of cholinesterase (ChE). Mol. dynamic simulations and Mol. Mechanics/Poisson-Boltzmann Surface Area (MM-PBSA) calculations indicate that 5e has more potent binding affinity than hit 1a, which may explain the stronger inhibitory effect of 5e on AChE. Furthermore, their predicted pharmacokinetic properties and in vitro influences on mouse brain neural network elec. activity were discussed. Taken together, compound 5e can be highlighted as a lead compound worthy of further optimization for designing new anti-AD drugs. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Name: 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).Name: tert-Butyl (5-aminopentyl)carbamate

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

The author of 《Synthesis of new lophine-carbohydrate hybrids as cholinesterase inhibitors: cytotoxicity evaluation and molecular modeling》 were Lopes, Joao Paulo Bizarro; Silva, Luana; Ceschi, Marco Antonio; Ludtke, Diogo Seibert; Zimmer, Aline Rigon; Ruaro, Thais Carine; Dantas, Rafael Ferreira; de Salles, Cristiane Martins Cardoso; Silva-Jr, Floriano Paes; Senger, Mario Roberto; Barbosa, Gisele; Lima, Lidia Moreira; Guedes, Isabella Alvim; Dardenne, Laurent Emmanuel. And the article was published in MedChemComm in 2019. Application of 51644-96-3 The author mentioned the following in the article:

In this study, we synthesized nine novel hybrids derived from D-xylose, D-ribose, and D-galactose sugars connected by a methylene chain with lophine. The compounds were synthesized by a four-component reaction to afford the substituted imidazole moiety, followed by the displacement reaction between sugar derivatives with an appropriate N-alkylamino-lophine. All the compounds were found to be the potent and selective inhibitors of BuChE activity in mouse serum, with compound 9a (a D-galactose derivative) being the most potent inhibitor (IC50 = 0.17μM). According to the mol. modeling results, all the compounds indicated that the lophine moiety existed at the bottom of the BuChE cavity and formed a T-stacking interaction with Trp231, a residue accessible exclusively in the BuChE cavity. Noteworthily, only one compound exhibited activity against AChE (8b; IC50 = 2.75μM). Moreover, the in silico ADME predictions indicated that all the hybrids formulated in this study were drug-likely, orally available, and able to reach the CNS. Further, in vitro studies demonstrated that the two most potent compounds against BuChE (8b and 9a) had no cytotoxic effects in the Vero (kidney), HepG2 (hepatic), and C6 (astroglial) cell lines. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Application of 51644-96-3)

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).Application of 51644-96-3

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

In 2017,Duan, Sujuan; Guo, Lu; Shi, Dandan; Shang, Mengmeng; Meng, Dong; Li, Jie published 《Development of a novel folate-modified nanobubbles with improved targeting ability to tumor cells》.Ultrasonics Sonochemistry published the findings.HPLC of Formula: 51644-96-3 The information in the text is summarized as follows:

Conjugation of folate (FOL) to nanobubbles could enhance the selective targeting to tumors expressing high levels of folate receptor (FR). To further improve the selective targeting ability of FOL-modified nanobubbles, a novel FOL-targeted nanobubble ((FOL)2-NB) with increasing FOL content (accomplished by linking two FOL mols. per DSPE-PEG2000 chain) was synthesized, through the methods of mech. shaking and low-speed centrifugation based on lipid-stabilized perfluoropropane. The bubble size and distribution range were measured by dynamic light scattering (DLS). Enhanced imaging ability was evaluated using a custom-made agarose mold with a clin. US imaging system at mech. indexes of up to 0.12 at a center frequency of 9.0 MHz. Targeted ability was also carried out in human breast cancer MCF-7 cells, which over-express the FR, by fluorescence activated cell sorting (FACS) and fluorescence microscopy, resp. (FOL)2-NB with a particle size of 286.87 ± 22.96 nm were successfully prepared, and they exhibited superior contrast imaging effect. FACS and fluorescence microscopy studies showed greater cellular targeting ability in the group of (FOL)2-NB than in their control group of Non-targeted-NB (no FOL targeted nanobubbles) and FOL-NB (one FOL mol. per DSPE-PEG2000 chain). These results suggest that a new type of stronger targeted nanobubble was successfully prepared by increasing the FOL content per DSPE-PEG2000 chain. This novel (FOL)2-NBs are potentially useful for ultrasound mol. imaging and treatment of FR-pos. tumors and are worthy for further investigation. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3HPLC of Formula: 51644-96-3)

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).HPLC of Formula: 51644-96-3

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

In 2017,Lv, Wei; Zhang, Guangming; Barinka, Cyril; Eubanks, James H.; Kozikowski, Alan P. published 《Design and Synthesis of Mercaptoacetamides as Potent, Selective, and Brain Permeable Histone Deacetylase 6 Inhibitors》.ACS Medicinal Chemistry Letters published the findings.Related Products of 51644-96-3 The information in the text is summarized as follows:

A series of non-hydroxamate HDAC6 inhibitors were prepared in our effort to develop potent and selective compounds for possible use in Central Nervous System (CNS) disorders, thus obviating the genotoxicity often associated with the hydroxamates. Halogens are incorporated in the cap groups of the designed mercaptoacetamides in order to increase brain accessibility. The indole analog and quinoline analog displayed potent HDAC6 inhibitory activity (IC50 11 nM and 2.8 nM) and excellent selectivity against HDAC1. Both compounds, together with their ester prodrug and disulfide prodrugs were found to be effective in promoting tubulin acetylation in HEK cells. The disulfide prodrugs also released a stable concentration of the indole and quinoline analogs upon microsomal incubation. Administration of disulfide prodrugs in vivo was found to trigger an increase of tubulin acetylation in mouse cortex. These results suggest that further exploration of these com-pounds for the treatment of CNS disorders is warranted. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Related Products of 51644-96-3)

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).Related Products of 51644-96-3

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

Liu, Jin; Yuan, Lin; Ruan, Yong; Deng, Bulian; Yang, Zicao; Ren, Yichang; Li, Ling; Liu, Ting; Zhao, Huiting; Mai, Ruiyao; Chen, Jianjun published an article in 2022. The article was titled 《Novel CRBN-Recruiting Proteolysis-Targeting Chimeras as Degraders of Stimulator of Interferon Genes with In Vivo Anti-Inflammatory Efficacy》, and you may find the article in Journal of Medicinal Chemistry.Category: esters-buliding-blocks The information in the text is summarized as follows:

The activation of the cyclic GMP-AMP synthase-stimulator of interferon gene (STING) pathway has been associated with the pathogenesis of many autoimmune and inflammatory disorders, and small mols. targeting STING have emerged as a new therapeutic strategy for the treatment of these diseases. While several STING inhibitors have been identified with potent anti-inflammatory effects, we would like to explore STING degraders based on the proteolysis-targeting chimera (PROTAC) technol. as an alternative strategy to target the STING pathway. Thus, we designed and synthesized a series of STING protein degraders based on a small-mol. STING inhibitor (C-170) and pomalidomide (a CRBN ligand). These compounds demonstrated moderate STING-degrading activities. Among them, SP23 (I) achieved the highest degradation potency with a DC50 of 3.2μM. Importantly, SP23 exerted high anti-inflammatory efficacy in a cisplatin-induced acute kidney injury mouse model by modulating the STING signaling pathway. Taken together, SP23 represents the first PROTAC degrader of STING deserving further investigation as a new anti-inflammatory agent. In addition to this study using tert-Butyl (5-aminopentyl)carbamate, there are many other studies that have used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Category: esters-buliding-blocks) 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).Category: esters-buliding-blocks

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

In 2018,Yang, Xue; Michiels, Thomas J. M.; de Jong, Coen; Soethoudt, Marjolein; Dekker, Niek; Gordon, Euan; van der Stelt, Mario; Heitman, Laura H.; van der Es, Daan; IJzerman, Adriaan P. published 《An Affinity-Based Probe for the Human Adenosine A2A Receptor》.Journal of Medicinal Chemistry published the findings.Application In Synthesis of tert-Butyl (5-aminopentyl)carbamate The information in the text is summarized as follows:

Using activity-based protein profiling (ABPP), functional proteins can be interrogated in their native environment. Despite their pharmaceutical relevance, G protein-coupled receptors (GPCRs) have been difficult to address through ABPP. In the current study, the authors took the prototypical human adenosine A2A receptor (hA2AR) as the starting point for the construction of a chem. toolbox allowing two-step affinity-based labeling of GPCRs. First, the authors equipped an irreversibly binding hA2AR ligand with a terminal alkyne to serve as probe. The authors showed that the probe irreversibly and concentration-dependently labeled purified hA2AR. Click-ligation with a sulfonated cyanine-3 fluorophore allowed us to visualize the receptor on SDS-PAGE. The authors further demonstrated that labeling of the purified hA2AR by the probe could be inhibited by selective antagonists. Lastly, the authors showed successful labeling of the receptor in cell membranes overexpressing hA2AR, making the probe a promising affinity-based tool compound that sets the stage for the further development of probes for GPCRs. The experimental process involved the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Application In Synthesis 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).Application In Synthesis of tert-Butyl (5-aminopentyl)carbamate

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

In 2018,Fernandes, Carlos; Benfeito, Sofia; Amorim, Ricardo; Teixeira, Jose; Oliveira, Paulo J.; Remiao, Fernando; Borges, Fernanda published 《Desrisking the Cytotoxicity of a Mitochondriotropic Antioxidant Based on Caffeic Acid by a PEGylated Strategy》.Bioconjugate Chemistry published the findings.Recommanded Product: tert-Butyl (5-aminopentyl)carbamate The information in the text is summarized as follows:

Mitochondrial oxidative damage is related to diverse pathologies, including cancer and neurodegenerative diseases. Shielding mitochondria from oxidative damage with mitochondriotropic antioxidants is by now considered an effective therapeutic strategy. Despite the success of the approach, some concerns related with cytotoxicity have been reported. For instance, AntiOxCIN6 is a mitochondriotropic antioxidant based on caffeic acid (CAF) that is cytotoxic in hepatocarcinoma (HepG2) cell lines. PEGylation, often used to enhance drug pharmacol. and pharmaceutical properties, was herein applied to modulate AntiOxCIN6 toxicity drawbacks. So, a dual-functionalization of polyethylene glycol (PEG) with TPP+ and CAF as targeting and antioxidant arms, resp., was performed by a two-step amidation strategy using Et chloroformate and EDC/NHS as coupling reagents. The data showed that the antioxidant properties related with CAF moiety were maintained in the CAF-PEG-TPP conjugate (CPTPP) and that PEGylation process reverted the loss of ability to chelate iron observed with AntiOxCIN6.. In cellular studies, CPTPP was nontoxic to human HepG2 and neuronal (SH-SY5Y) cells, while both CAF and AntiOxCIN6 demonstrated harmful effects in the same cell lines. The lack of cytotoxic events linked to oxidative stress levels observed with CPTPP suggested that PEGylation process somehow modulates the putative toxicity related with the presence of a catechol moiety and/or the TPP+ cation. In addition, the mitochondrial oxygen consumption was not significantly affected by CPTPP treatment in SH-SY5Y cells when compared with nontreated cells. CPTPP showed remarkable antioxidant effects in cell-based assays against several oxidative stress-induced agents (H2O2, t-BHP, and FeNTA). From the data it can be concluded that PEGylation technol. can modulate the toxicity of mitochondriotropic antioxidants without disturbing the antioxidant profile of the core antioxidant. PEGylation can be considered a relevant tool to hasten the difficulties related to the design and development of mitochondrial nontoxic and operative drug candidates. 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

In 2022,Yu, Xufen; Cheng, Meng; Lu, Kaylene; Shen, Yudao; Zhong, Yue; Liu, Jing; Xiong, Yue; Jin, Jian published an article in Journal of Medicinal Chemistry. The title of the article was 《Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras》.Category: esters-buliding-blocks The author mentioned the following in the article:

Several epidermal growth factor receptor (EGFR) proteolysis-targeting chimeras (PROTACs), including MS39 and MS154 developed by us, have been reported to effectively degrade the mutant but not the wild-type (WT) EGFR. However, the mechanism underlying the selectivity in degrading the mutant over the WT EGFR has not been elucidated. Here, we report comprehensive structure-activity relationship studies that led to the discovery of two novel EGFR degraders, 31 (MS9449) and 72 (MS9427), and mechanistic studies of these EGFR degraders. Compounds 31 (I) and 72(II) selectively degraded the mutant but not the WT EGFR through both ubiquitination/proteasome and autophagy/lysosome pathways. Interestingly, we found that the mutant but not the WT EGFR can effectively form EGFR-PROTAC-E3 ligase ternary complexes. Furthermore, we found that PI3K inhibition sensitized WT EGFR to PROTAC-induced degradation and combination treatment with a PI3K inhibitor enhanced antiproliferation activities of EGFR degraders in cancer cells harboring WT EGFR, providing a potential therapeutic strategy for patients with WT EGFR overexpression. The results came from multiple reactions, including the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Category: esters-buliding-blocks)

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).Category: esters-buliding-blocks

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

Formula: C10H22N2O2In 2017 ,《Comparative Structural Studies of Four Homologous Thioamidic Unclosed Crytpands: Self-Encapsulation of Lariat Arm, Odd-Even Effects, Anomalously Short S···S Chalcogen Bonding, and More》 was published in Crystal Growth & Design. The article was written by Dabrowa, Kajetan; Ceborska, Magdalena; Pawlak, Marcin; Jurczak, Janusz. The article contains the following contents:

Unclosed cryptands (UCs) 4a-d containing flexible (CH2)n spacers (n = 2-5) and a fixed p-nitrophenyl thioamide substituent (lariat arm) were synthesized and characterized by single crystal X-ray anal. Comparative anal. of their crystal structures provided an opportunity to recognize that conformation of 4a-d and occurrence of lattice solvent strictly depend on the length and parity of aliphatic linkers. Namely, the degree of self-inclusion of the lariat arm within the macrocyclic cavity was found to increase with greater elongation of the CH2 spacer. Odd-membered UCs (4b and 4d) showed a tendency to crystallize without lattice solvent, while even-membered UCs (4a and 4c) crystallized as various solvates. For two solvates of UC 4c anomalously short and highly directional C=S···S=C chalcogen interactions (dS···S = 3.21-3.35 Å) were observed between adjacent UC mols., forming a dimeric cube-like supramol. assembly. Packing of dimers and the length of homo-chalcogen interaction were affected by lattice solvent. Evaluation of data on C=S···S=C contacts retrieved from Cambridge Structural Database suggests that a precisely positioned external H-bond donor (NH or water) is important for stabilization of this type of noncovalent interaction.tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Formula: 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).Formula: C10H22N2O2

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