Tag: 0-100

In 2022,Yang, Zeqiu; Wu, Jianbing; Wu, Keling; Luo, Jingyi; Li, Cunrui; Zhang, Jiaming; Zhao, Minglei; Mei, Tingfang; Liu, Xinqi; Shang, Bizhi; Zhang, Yihua; Zhao, Ling; Huang, Zhangjian published an article in Journal of Medicinal Chemistry. The title of the article was 《Identification of Nitric Oxide-Donating Ripasudil Derivatives with Intraocular Pressure Lowering and Retinal Ganglion Cell Protection Activities》.Category: alcohols-buliding-blocks The author mentioned the following in the article:

Based on the synergistic therapeutic effect of nitric oxide (NO) and Rho-associated protein kinase (ROCK) inhibitors on glaucoma, a new group of NO-donating ripasudil derivatives RNO-1-RNO-6 was designed, synthesized, and biol. evaluated. The results demonstrated that the most active compound RNO-6 maintained potent ROCK inhibitory and NO releasing abilities, reversibly depolymerized F-actin, and suppressed mitochondrial respiration in human trabecular meshwork (HTM) cells. Topical administration of RNO-6 (0.26%) in chronic ocular hypertension glaucoma mice exhibited significant IOP lowering and visual function and retinal ganglion cell (RGC) protection activities, superior to an equal molar dose of ripasudil. RNO-6 could be a promising agent for glaucoma or ocular hypertension, warranting further investigation. The results came from multiple reactions, including the reaction of 3-Aminopropan-1-ol(cas: 156-87-6Category: alcohols-buliding-blocks)

3-Aminopropan-1-ol(cas: 156-87-6) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Category: alcohols-buliding-blocks

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

An, Ju Hyeon; Kim, Kyu Dong; Lee, Jun Hee published their research in Journal of Organic Chemistry in 2021. The article was titled 《Highly Chemoselective Deoxygenation Of N-Heterocyclic N-Oxides Using Hantzsch Esters As Mild Reducing Agents》.COA of Formula: C3H6O2 The article contains the following contents:

A highly chemoselective room-temperature deoxygenation method applicable to various functionalized N-heterocyclic N-oxides via visible light-mediated metallaphotoredox catalysis using Hantzsch esters as the sole stoichiometric reductant to afford deoxygenated N-heterocycles I [R = 6-OMe, 6-Cl, 2-Ph, etc.], II [R1 = H, 5-Br; X = CH, N] and III [R2 = 3-Ph, 2,6-Cl2, pyridin-2-yl, etc.] were reported. Despite the feasibility of catalyst-free conditions, most of these deoxygenations could be completed within a few minutes using only a tiny amount of a catalyst. This technol. also allowed for multigram-scale reactions even with an extremely low catalyst loading of 0.01 mol %. The scope of this scalable and operationally convenient protocol encompassed a wide range of functional groups, such as amides, carbamates, esters, ketones, nitrile groups, nitro groups and halogens, which provided access to the corresponding compounds I, II and III in good to excellent yields (an average of an 86.8% yield for a total of 45 examples). In the experiment, the researchers used Oxetan-3-ol(cas: 7748-36-9COA of Formula: C3H6O2)

Oxetan-3-ol(cas: 7748-36-9) is used as a reagent in the synthesis of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. It is also used as a reagent in the synthesis of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors.COA of Formula: C3H6O2

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

《Transdermal siRNA delivery by pH-switchable micelles with targeting effect suppress skin melanoma progression》 was written by Wang, Mao-Ze; Niu, Jie; Ma, Hui-Jian; Dad, Haseeb Anwar; Shao, Hai-Tao; Yuan, Tie-Jun; Peng, Li-Hua. Recommanded Product: 156-87-6 And the article was included in Journal of Controlled Release in 2020. The article conveys some information:

Melanoma is an aggressive disease with rapid progression and fast relapse, representing one of the formidable challenges in clinic. Current systemic therapies for melanoma exhibit limited anticancer potential due to the lack of specificity and limited efficacy. Herein, we design a cationic polymer (SCP-HA-PAE) by conjugating skin/cell penetrating peptide (SCP) and hyaluronic acid (HA) to the amphipathic polymer (poly β-amino esters, PAE), then fabricate the nanocarriers (SHP) composed by SCP-HA-PAE for delivering siRNA to skin melanoma by transdermal application. SHP not only manifests the excellent ability in penetrating through skin stratum corneum (SC), targeting melanoma and being sensitive to pH, but also expresses the advantages in compacting the vector/siRNAs nanocomplexes and stimulating their endosome escape inside cells, which ensure the enhanced siRNA delivery efficiency. SHP/siRNA induce the strong efficacy in retarding the progression and relapse of skin melanoma through the enhanced apoptosis effect both in vitro & in vivo. This study provides a proof-of-concept design of pH-switchable cationic micelles as transdermal gene delivery nanoplatforms with targeting effect for melanoma therapy, which may be adapted widely in the treatment of various superficial tumors and skin genetic diseases. The results came from multiple reactions, including the reaction of 3-Aminopropan-1-ol(cas: 156-87-6Recommanded Product: 156-87-6)

3-Aminopropan-1-ol(cas: 156-87-6) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Recommanded Product: 156-87-6

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

《Design, Synthesis, and Biological Evaluation of Linear Aliphatic Amine-Linked Triaryl Derivatives as Potent Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Cell Death-Ligand 1 Interaction with Promising Antitumor Effects In Vivo》 was written by Guo, Jialin; Luo, Longlong; Wang, Zhihong; Hu, Naijing; Wang, Wei; Xie, Fei; Liang, Erguang; Yan, Xinlin; Xiao, Junhai; Li, Song. Name: 2-Aminopropane-1,3-diol And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:

A series of novel linear aliphatic amine-linked triaryl derivatives as inhibitors of PD-1/PD-L1 were designed, synthesized, and evaluated in vitro and in vivo. In this chem. series, compound I showed the most potent inhibitory activity and binding affinity with hPD-L1, with an IC50 value of 12 nM and a KD value of 16.2 pM, showing a binding potency approx. 2000-fold that of hPD-1. Compound I could bind with hPD-L1 on the cellular surface and competitively block the interaction of hPD-1 with hPD-L1. In a T cell function assay, I restored the T cell function, leading to increased IFN-γ secretion. Moreover, in a humanized mouse model, compound I significantly inhibited tumor growth without obvious toxicity and showed moderate PK properties after i.v. injection. These results indicated that I is a promising lead for further development of small-mol. PD-1/PD-L1 inhibitors for cancer therapy. The experimental part of the paper was very detailed, including the reaction process of 2-Aminopropane-1,3-diol(cas: 534-03-2Name: 2-Aminopropane-1,3-diol)

2-Aminopropane-1,3-diol(cas: 534-03-2) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Name: 2-Aminopropane-1,3-diol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Name: 2-Aminopropane-1,3-diolIn 2022 ,《A robust and self-healing elastomer achieved by a thio-β-diketone-Cu(II) coordination and H-bonding dual crosslinked system》 was published in Materials Chemistry Frontiers. The article was written by An, Xiaoming; Liu, Jie; Zhang, Jia-Han; Huang, Xinxin; Zhu, Tangsong; Yan, Hongping; Jia, Xudong; Zhang, Qiuhong. The article contains the following contents:

Elastomers possessing good mech. strength and self-healing capability are showing great importance in stretchable electronics, since they can play the role of robust substrates for devices, and prolong the service life of devices. However, it is hard to balance the trade-off between the high mech. strength and self-healing ability. Here we propose the synergetic strategy via combining thio-β-diketone-Cu2+ metal-ligand (M-L) coordination with hydrogen bonds in one system, through which high mech. strength, good elasticity and self-healing ability are achieved. The elastomer displays excellent mech. performances (with a fracture strength of 4.35 MPa and a fracture strain of 3400%). Meanwhile, the elastomer can realize a high self-healing efficiency (94%) within only 3 h at 80 °C. X-ray absorption fine structure (XAFS) anal. demonstrates the reconfiguration of M-L coordination at the mol. level, and small angle X-ray scattering (SAXS) during stretching demonstrates the microphase structure change of the polymer at the nanoscale level. Based on the elastomer, a self-healable pressure sensor and a self-healable strain sensor are fabricated.2-Aminopropane-1,3-diol(cas: 534-03-2Name: 2-Aminopropane-1,3-diol) was used in this study.

2-Aminopropane-1,3-diol(cas: 534-03-2) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Name: 2-Aminopropane-1,3-diol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Electric Literature of C3H9NOIn 2020 ,《Synthesis, Characterization, Antibacterial Properties and DFT Studies of Two New Polypyrazolic Macrocycles》 was published in Polycyclic Aromatic Compounds. The article was written by Harit, Tarik; Cherfi, Mounir; Abouloifa, Houssam; Isaad, Jalal; Bouabdallah, Ibrahim; Rahal, Mahmoud; Asehraou, Abdeslam; Malek, Fouad. The article contains the following contents:

Two novel sym. macrocycles I [R = CHMe2, (CH2)3OH] containing four pyrazolic units, with two different side arms were synthesized and characterized. Their antibacterial activity was investigated by determining the inhibition zone diameter in agar gel and minimal inhibitory concentration The obtained results showed that the tetrapyrazolic macrocycle with a hydroxyl group in its side chain presented the best inhibitory effect against all tested bacterial strain. Mol. geometries, HOMO-LUMO anal. and mol. electrostatic potential of macrocycles were investigated by theor. calculations with B3LYP/6-31G* level. The mol. electrostatic potential surface showed that the presence of electrophile site in the lateral arms of these macrocycles enhances the antibacterial activity of such compounds In addition to this study using 3-Aminopropan-1-ol, there are many other studies that have used 3-Aminopropan-1-ol(cas: 156-87-6Electric Literature of C3H9NO) was used in this study.

3-Aminopropan-1-ol(cas: 156-87-6) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Electric Literature of C3H9NO

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

Electric Literature of C3H6O2In 2022 ,《Electrosynthesis of ortho-Amino Aryl Ketones by Aerobic Electrooxidative Cleavage of the C(2)=C(3)/C(2)-N Bonds of N-Boc Indoles》 was published in Advanced Synthesis & Catalysis. The article was written by Wu, Jintao; Peng, Zehui; Shen, Tong; Liu, Zhong-Quan. The article contains the following contents:

An electrochem.-driven aerobic cleavage of C(2)=C(3)/C(2)-N bonds of indoles was reported. Through an undivided cell, various indoles and its derivatives were converted into the corresponding ortho-amino aryl ketones. This method featured metal-free, air-as-oxidant and easy scalability. In addition to this study using Oxetan-3-ol, there are many other studies that have used Oxetan-3-ol(cas: 7748-36-9Electric Literature of C3H6O2) was used in this study.

Oxetan-3-ol(cas: 7748-36-9) is used as a reagent in the synthesis of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. It is also used as a reagent in the synthesis of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors.Electric Literature of C3H6O2

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

《Deep eutectic solvents consisting of 1-ethyl-3-methylimidazolium chloride and glycerol derivatives for highly efficient and reversible SO2 capture》 was written by Long, Guangcai; Yang, Chunliang; Yang, Xiaoqing; Zhao, Tianxiang; Xu, Meisong. Computed Properties of C3H9NO2 And the article was included in Journal of Molecular Liquids in 2020. The article conveys some information:

Development of eco-friendly materials for the removal of SO2 is a significant topic in sustainable chem. engineering process. In this work, we describe an efficient protocol for highly efficient and reversible SO2 capture by deep eutectic solvents (DESs) consisting of 1-ethyl-3-methylimidazolium chloride (EmimCl) and glycerol derivatives The presented DESs exhibit an equal or much higher absorption capacity than previously reported DESs or ionic liquids in the same conditions. Particularly, EmimCl-glycerol (molar ratio 2:1) shows excellent reversible absorption through phys. interactions supporting by FTIR and NMR spectroscopic experiments, thus presenting good potential as a candidate absorbent for the removal of SO2. In the experiment, the researchers used many compounds, for example, 2-Aminopropane-1,3-diol(cas: 534-03-2Computed Properties of C3H9NO2)

2-Aminopropane-1,3-diol(cas: 534-03-2) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Computed Properties of C3H9NO2

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

《Clay-based hybrids for controlled release of 7-azaindole derivatives as neuroprotective drugs in the treatment of Alzheimer’s disease》 was published in Applied Clay Science in 2020. These research results belong to Garcia-Vazquez, Rocio; Rebitski, Ediana P.; Viejo, Lucia; de los Rios, Cristobal; Darder, Margarita; Garcia-Frutos, Eva M.. Related Products of 7748-36-9 The article mentions the following:

Hybrid systems based on clay minerals and 7-azaindole derivatives, which show an interesting neuroprotective profile in several in vitro models of neurodegeneration, were developed in order to facilitate the oral administration of these drugs in the treatment of Alzheimer’s disease and provide a controlled release. Two 7-azaindole derivatives with different substitution at position 5 (-OCH3, -H) were synthesized and adsorbed on nanocarriers of different morphol., the lamellar clay montmorillonite (MMT) and the halloysite nanotubes (HNT). Studies carried out in cultures of human neuroblastoma cells confirmed the lack of toxicity of the hybrids and their neuroprotective effect against okadaic acid (OA), the inhibitor of the protein phosphatase 2A (PP2A), similarly to the non-encapsulated drugs. The release assays carried out in systems that simulate the gastrointestinal tract show a rapid release of the drugs from the hybrid materials, making necessary their encapsulation in a protective biopolymer matrix to slow down the release kinetics. A blend of alginate and zein was chosen for this purpose, exploiting the gelation of alginate with calcium ions to process the material as microbeads and the hydrophobic character of zein to reduce the water uptake of the material. Therefore, these bio-nanocomposite systems integrating the drug/clay hybrids seem promising for the oral administration of drugs with multitarget activity for the treatment of Alzheimer’s disease. In addition to this study using Oxetan-3-ol, there are many other studies that have used Oxetan-3-ol(cas: 7748-36-9Related Products of 7748-36-9) was used in this study.

Oxetan-3-ol(cas: 7748-36-9) is used as a reagent in the synthesis of 5-fluoro-4,6-dialkoxypyrimidine GPR119 agonists. It is also used as a reagent in the synthesis of cyclic sulfone hydroxyethylamines as potent and selective β-site APP-cleaving enzyme 1 (BACE1) inhibitors.Related Products of 7748-36-9

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

The author of 《Folate-conjugated chitosan-pluronic P123 nanogels: synthesis and characterizations towards dual drug delivery》 were Nguyen, Van Toan; Nguyen, Thi Huong; Dang, Le Hang; Vu-Quang, Hieu; Tran, Ngoc Quyen. And the article was published in Journal of Nanomaterials in 2019. Reference of 4-Aminobutan-1-ol The author mentioned the following in the article:

In this study, a self-assembled nanogel-based pluronic P123-grafted chitosan-folate (CP-FA) was fabricated as a paclitaxel/curcumin codelivery system. 1H-NMR and TGA proved that the fabricating method of CP-FA was successful. Dynamic light scattering (DLS), zeta potentials, and transmission electron microscopy (TEM) exposed that CP-FA nanoparticles had a uniform size with a diameter of around 16.27 ± 2.01 nm in the colloidal solution and had better sustainable stability at a lower concentration than P123 due to the moderate pos. potential value (39.43 ± 3.45 mV) and the lower critical micelle concentration (0.036 mg/mL). Dual drugs were loaded with CP-FA nanogels via self-assembly by the hydrophobic interaction between both hydrophobic therapeutic compounds (PTX and Cur) and the hydrophobic segment of the P123 copolymer. The high hydrophobicity of the segment induced a great loading efficacy of up to 98.63 ± 0.42 of PTX and 97.82 ± 0.48 of Cur. In addition, the CP-FA nanogels exposed superior effects in a controlled release of these encapsulated therapeutic compounds for a long period of time. The anticancer activity of the dual-drug delivery system was evaluated using human breast cancer cell lines (MCF-7) via the IC50 value to compare with the PTX-loading CP-FA nanogel. The obtained results suggested that CP-FA/PTX-Cur displayed a remarkable improvement in anticancer activity at an IC50 value of 5.74 ± 0.23 nM which was higher than that of CP-FA/PTX (IC50 = 8.20 ± 1.41 nM) due to the synergistic effect of both PTX and Cur. Thereby, a dual-drug delivery-system-based CP-FA of PTX and Cur has been proposed as a promising candidate in cancer therapy.4-Aminobutan-1-ol(cas: 13325-10-5Reference of 4-Aminobutan-1-ol) was used in this study.

4-Aminobutan-1-ol(cas: 13325-10-5) is used in the synthesis of NSAIDs with anti-inflammatory properties. Also used in the synthesis of polyamine transport ligands with specificity against human cancers allowing easy access to specific cancer cells.Reference of 4-Aminobutan-1-ol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts