Tag: 200-300

On July 12, 2021, Ma, Yiming; Sun, Mengmeng; Liu, Yanbo; Chen, Mingyang; Wu, Songgu; Wang, Mengwei; Wang, Lingyu; Gao, Zhenguo; Han, Dandan; Liu, Lande; Wang, Jingkang; Gong, Junbo published an article.SDS of cas: 144-80-9 The title of the article was Design of Spherical Crystallization of Active Pharmaceutical Ingredients via a Highly Efficient Strategy: From Screening to Preparation. And the article contained the following:

This work aims to develop a highly efficient spherical crystallization from screening to preparation stage based on liquid-liquid phase separation (LLPS). Mixtures than can undergo an LLPS split into two liquid phases with different phys. properties, and the oil droplets formed during that process make LLPS a promising approach to prepare spherical particles of an active pharmaceutical ingredient (API). In the screening stage, three machine learning (ML) models (artificial neural network, support vector machine, and logistic regression) were established for predicting LLPS for an API. Two linear models, a simple linear model and a machine learning-based linear model, were also constructed to produce further optimization. The ML-based prediction of LLPS was first established in this work and showed high accuracy and reliability. Also, when compared to a method where the screening depended on the results of experiments, the prediction model highly reduced the use of chem. substances and saved labor and time. In the preparation stage, water and ethanol, which have low toxicity to mammals and have environmental advantages over other organic solvents, were applied as the solvents of LLPS-based spherical crystallization The LLPS-based preparation process of spherical particles possesses advantages in terms of reduction of the number of unit operations as well as energy consumption and processing cost. The experimental process involved the reaction of N-((4-Aminophenyl)sulfonyl)acetamide(cas: 144-80-9).SDS of cas: 144-80-9

The Article related to aprepitant design spherical crystallization screening active pharmaceutical ingredient, Pharmaceuticals: Pharmaceutics and other aspects.SDS of cas: 144-80-9

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

On December 31, 2021, Mahmoudabadi, Samane zarei; Pazuki, Gholamreza published an article.Recommanded Product: N-((4-Aminophenyl)sulfonyl)acetamide The title of the article was A predictive PC-SAFT EOS based on COSMO for pharmaceutical compounds. And the article contained the following:

The present study was conducted to develop a predictive type of PC-SAFT EOS by incorporating the COSMO computations. With the proposed model, the phys. adjustable inputs to PC-SAFT EOS were determined from the suggested correlations with dependency to COSMO computation results. Afterwards, we tested the reliability of the proposed predictive PC-SAFT EOS by modeling the solubility data of certain pharmaceutical compounds in pure and mixed solvents and their octanol/water partition coefficients The obtained RMSE based on logarithmic scale for the predictive PC-SAFT EOS was 1.435 for all of the solubility calculations The reported values (1.435) had a lower value than RMSE for COSMO-SAC model (4.385), which is the same as that for RMSE for COSMO-RS model (1.412). The standard RMSE for octanol/water partition coefficient of the investigated pharmaceutical compounds was estimated to be 1.515. The experimental process involved the reaction of N-((4-Aminophenyl)sulfonyl)acetamide(cas: 144-80-9).Recommanded Product: N-((4-Aminophenyl)sulfonyl)acetamide

The Article related to pharmaceutical compound cosmo perturbed chain statistical associating fluid theory, Pharmaceuticals: Pharmaceutics and other aspects.Recommanded Product: N-((4-Aminophenyl)sulfonyl)acetamide

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

On May 15, 2014, Geissler, Jacobo Edward; Zhou, Jiang; Jiang, Yang; Zhou, Li published a patent.Reference of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide The title of the patent was Compositions and methods for affecting mental state and body composition. And the patent contained the following:

Nutritional products and dietary supplements comprise aegeline, consumption of which may result in increased mental stamina, focus, and energy level, improved mood, increased thermogenesis, increased libido, and anabolic effects and increased strength output and(or) muscle mass. The effects may include improved cognition and body composition, with promotion of weight loss, and(or) fitness and well-being. Aegeline may be synthesized by: (a) preparing 2-amino-1-(4-methoxyphenyl)ethanone hydrochloride from 1-(4-methoxyphenyl)ethanone; (b) reacting 2-amino-1-(4-methoxyphenyl)ethanone hydrochloride with cinnamoyl chloride to form N-(2-(4-methoxyphenyl)-2-oxoethyl)cinnamamide intermediate; and (c) reacting the N-(2-(4-methoxyphenyl)-2-oxoethyl)cinnamamide with a reducing agent to form aegeline. The experimental process involved the reaction of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide(cas: 456-12-2).Reference of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide

The Article related to aegeline preparation diet supplement mental activity libido muscle strength, Food and Feed Chemistry: Other and other aspects.Reference of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide

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

On April 30, 2011, Mugabe, Clement; Matsui, Yoshiyuki; So, Alan I.; Gleave, Martin E.; Heller, Markus; Zeisser-Labouebe, Magali; Heller, Lindsay; Chafeeva, Irina; Brooks, Donald E.; Burt, Helen M. published an article.Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione The title of the article was In vitro and in vivo evaluation of intravesical docetaxel loaded hydrophobically derivatized hyperbranched polyglycerols in an orthotopic model of bladder cancer. And the article contained the following:

The objective of this study was to evaluate the tolerability, to establish a dosing regimen, and to evaluate the efficacy of intravesical docetaxel (DTX) formulations in a mouse model of bladder cancer. DTX in com. formulation (Taxotere, DTX in Tween 80) or loaded in hyperbranched polyglycerols (HPGs) was evaluated. The synthesis and characterization of HPGs with hydrophobic cores and derivatized with methoxy poly(ethylene glycol) in the shell and further functionalized with amine groups (HPG-C8/10-MePEG and HPG-C8/10-MePEG-NH2) is described. Intravesical DTX in either com. or HPGs formulations (up to 1.0 mg/mL) was instilled in mice with orthotopic bladder cancer xenografts and was well tolerated with no apparent signs of local or systemic toxicities. Furthermore, a single dose of intravesical DTX (0.5 mg/mL) loaded in HPGs was significantly more effective in reducing the tumor growth in an orthotopic model of bladder cancer than the com. formulation of Taxotere. In addition, DTX-loaded HPG-C8/10-MePEG-NH2 was found to be more effective at lower instillation dose than DTX (0.2 mg/mL)-loaded HPG-C8/10-MePEG. Overall, our data show promising antitumor efficacy and safety in a recently validated orthotopic model of bladder cancer. Further research is warranted to evaluate its safety and efficacy in early phase clin. trials in patients refractory to standard intravesical therapy. The experimental process involved the reaction of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione(cas: 5455-98-1).Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

The Article related to hyperbranched polyglycerol amino peg nanoparticle docetaxel bladder cancer, Pharmaceuticals: Pharmaceutics and other aspects.Application In Synthesis of 2-(Oxiran-2-ylmethyl)isoindoline-1,3-dione

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

On October 1, 2022, Lamaoui, Abderrahman; Karrat, Abdelhafid; Amine, Aziz published an article.Related Products of 144-80-9 The title of the article was Molecularly imprinted polymer integrated into paper-based analytical device for smartphone-based detection: Application for sulfamethoxazole. And the article contained the following:

In this work, we developed a paper-based anal. device (PAD) that utilizes molecularly imprinted polymer (MIP) as the biomimetic receptor and a very simple colorimetric assay combined with a smartphone readout. Sulfamethoxazole was used as a model analyte to evaluate the feasibility of the developed MIP-PAD. After the synthesis of MIP, its adsorption properties (isotherm, kinetic and thermodn.) were scrutinized. Thereafter, The MIP- PAD was fabricated through the vacuum-assisted deposition of MIP suspension onto porous paper forming a 7 mm diameter of MIP layer. The MIP-PAD was characterized by Fourier-transform IR spectroscopy and SEM. The sulfamethoxazole transforms into azo dye through a colorimetric reaction. The smartphone was utilized for the read-out of results. The LOD was 0.21 ppm. The proposed MIP-PAD showed high long-term stability. The determination of SMX was carried out in spiked tap and river water samples to evaluate the applicability of the proposed anal. strategy in real-world applications. The developed MIP-PAD would provide a new platform for real-time, selective, rapid, user-friendly, low-cost, portable, and straightforward colorimetric assays in environmental monitoring, public health, and food control. The experimental process involved the reaction of N-((4-Aminophenyl)sulfonyl)acetamide(cas: 144-80-9).Related Products of 144-80-9

The Article related to molecularly imprinted polymer smartphone sulfamethoxazole, Biochemical Methods: Apparatus and other aspects.Related Products of 144-80-9

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

On March 2, 2021, Li, Chengwei; Zhong, Jialiang; Liu, Baohu; Yang, Tao; Lv, Binhua; Luo, Youfu published an article.Recommanded Product: 1,3-Diphenylurea The title of the article was Study on Typical Diarylurea Drugs or Derivatives in Cocrystallizing with Strong H-Bond Acceptor DMSO. And the article contained the following:

Diarylureas are widely used in self-assembly and supramol. chem. owing to their outstanding characteristics as both H-bond donors and acceptors. Unfortunately, this bonding property is rarely applied in the development of urea-containing drugs. Herein, seven related DMSO complexes were screened from 12 substrates involving sorafenib and regorafenib, mainly considering the substitution effect following a robust procedure. All complexes were structurally confirmed by spectroscopic means and thermal anal. Specially, five cocrystals with three deuterated, named sorafenib·DMSO, donafenib·DMSO, deuregorafenib·DMSO, 6·DMSO, and 7·DMSO were obtained. The crystal structures revealed that all host mols. consistently bonded with DMSO in intermol. interaction in a 1:1 stoichiometry. However, further comparison with documented DMSO complexes and parent motifs presented some arrangement diversities especially for 6·DMSO which offered a counter-example to previous rules. Major changes in the orientation of meta-substituents and the packing stability for sorafenib·DMSO and deuregorafenib·DMSO were rationalized by theory anal. and computational energy calculation Cumulative data implied that the planarization of two aryl planes in diarylureas may play a crucial role in cocrystn. Also, a polymorph study bridged the transformation between these ureas and their DMSO complexes. The experimental process involved the reaction of 1,3-Diphenylurea(cas: 102-07-8).Recommanded Product: 1,3-Diphenylurea

The Article related to diarylurea drug derivative cocrystn dmso, Pharmaceuticals: Pharmaceutics and other aspects.Recommanded Product: 1,3-Diphenylurea

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

Upadhyay, Ravi Kant published an article in 2015, the title of the article was Bel plant: A source of pharmaceuticals and ethno medicines.Category: amides-buliding-blocks And the article contains the following content:

A review. Bel is a holy native tree of India, which has high ethnomedicinal, therapeutic, and pharmaceutical importance. Bel contains many diverse bioactive components in leaves, flowers, fruits, wood, root, and bark which show multiple biol. activity and high therapeutic importance. Plant contains coumarins, marmelosin, marmesin, imperatorin, marmin, alloimperatorin, Me ether, xanthotoxol, scoparone, scopoletin, umbelliferone, psoralen and marmelide and marmenol, aegelin, aegelenine, marmeline, dictamine, fragrine which show anticancer, antioxidant, antimicrobial, anti-plasmodial, and hepatoprotective activities. Plant possesses various polysaccharides such as galactose, arabinose, uronic acid, and L-rhamnose. Its seed oil contains palmitic, stearic, oleic, linoleic, and linolenic acids which possess very high nutritive value. Plant also possesses very high tannin contents (9%) in fruits, pulp leaves. Tannin found in leaves as skimmianine. Marmelosin, skimmianine, and umbelliferone are therapeutically important active principles. Aegle marmelos is also a good source of gum, wound healers, carotenoids, vitamins, sugars, and nutritive oils. The plant is used to cure digestive disorders, ulcers, headache, hypertension, diabetes, constipation, and numerous other ailments. The ripe fruits are used as a laxative, while unripe Bel fruit, promotes digestion, and cures diarrhea. A. marmelos contains plant essential oil which shows chemotypic and seasonal variations. In the present review article, ethnomedicinal, therapeutic, pharmaceuticals, and insecticidal properties of A. marmelos have been described in detail. The experimental process involved the reaction of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide(cas: 456-12-2).Category: amides-buliding-blocks

The Article related to review aegle leaf flower fruit phytochem pharmaceutical ethno medicine, Plant Biochemistry: Reviews and other aspects.Category: amides-buliding-blocks

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

Rawat, Taniya; Uniyal, Sushmita published an article in 2021, the title of the article was A review on phytoconstituents and reported pharmacological activities of rutaceae family plant: Aegle marmelos (L.) correa leaf.Reference of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide And the article contains the following content:

A review. The only plant in the genus Aegle is bael, a slow-growing, resistant subtropical spiky tree. Family: Rutaceae (Citrus family). It’s also known as wood apple, Bengal quince, golden apple, Indian quince, holy fruit, and stone apple in English. In Sanskrit-Bilwa and in Hindi-Bael, bel. The leaf is one of the plant’s most accumulative sections, holding bioactive substances that are generated as secondary metabolites. Traditionally bael is effective in the treatment of dropsy, diarrhoea, dysentery, and intestinal problems. Phenol, flavonoid, tannin, carbohydrate, sterols, Saponin and alkaloid are all found in leaf extract Skimmianine, Aegeline, lupeol, cineol, eugenol, cuminaldehyde, marmesinine, citronella, and essential oils are isolated compounds from bael. The main components were limonene (82.4%) and (Z)-ocimene (5.1%), which together made up 87.5 percent of the leaf oil. Limonene has been shown to be a useful marker for identifying Aegle marmelos oil samples. Reported pharmacol. studies of A.marmelos leaf extract are Learning and memory, Anxiolytic and Antidepressant, Anticonvulsant, Analgesic, Antipyretic, Anti-inflammatory, Immunomodulatory, hepatoprotective, Cardioprotective, Nephrotoxicity, Antiulcer, Antidiarrhoeal, Antimicrobial, Antiobesity, Anti-proliferative, Antidiabetic, Poly cystic ovarian syndrome, Antithroid activity. The experimental process involved the reaction of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide(cas: 456-12-2).Reference of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide

The Article related to review aegle phytoconstituent drug, Plant Biochemistry: Reviews and other aspects.Reference of N-(2-Hydroxy-2-(4-methoxyphenyl)ethyl)cinnamamide

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

On October 15, 2017, Xu, Guangsen; Liu, Tingting; Zhou, Yi; Yang, Xinying; Fang, Hao published an article.Product Details of 97-09-6 The title of the article was 1-Phenyl-1H-indole derivatives as a new class of Bcl-2/Mcl-1 dual inhibitors: Design, synthesis, and preliminary biological evaluation. And the article contained the following:

Bcl-2 proteins, such as B-cell lymphoma (Bcl-2) protein, myeloid cell leukemia sequence 1 (Mcl-1) protein, has been implicated in the progression and survival of multiple tumor types and become a validated and attractive target for cancer therapy. In this work, a series of 1-phenyl-1H-indole derivatives has been designed and synthesized. The preliminary biol. studies (binding assay for Bcl-2 proteins and MTT assay) suggested that some active compounds showed potent inhibitory activities on Bcl-2/Mcl-1 without binding on Bcl-XL. Furthermore, Compound I and II showed better anti-proliferative activity than WL-276. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Product Details of 97-09-6

The Article related to phenylindole synthesis antitumor bcl2 mcl1, 1-phenyl-1h-indole derivatives, anti-tumor, apoptosis, bcl-2/mcl-1 dual inhibition, Pharmacology: Structure-Activity and other aspects.Product Details of 97-09-6

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

On January 1, 2017, Wan, Yichao; Liu, Tingting; Li, Xiaoxian; Chen, Chen; Fang, Hao published an article.Category: amides-buliding-blocks The title of the article was Improved binding affinities of pyrrolidine derivatives as Mcl-1 inhibitors by modifying amino acid side chains. And the article contained the following:

As an important member of anti-apoptotic Bcl-2 protein, myeloid cell leukemia sequence 1 (Mcl-1) protein is an attractive target for cancer therapy. In this study, a new series of pyrrolidine derivatives as Mcl-1 inhibitors were developed by mainly modifying the amino acid side chain of compound 1. Among them, compound 18 (Ki = 0.077 μM) exhibited better potent inhibitory activities towards Mcl-1 protein compared to pos. control Gossypol (Ki = 0.18 μM). In addition, compound 40 possessed good antiproliferative activities against PC-3 cells (Ki = 8.45 μM), which was the same as pos. control Gossypol (Ki = 7.54 μM). The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Category: amides-buliding-blocks

The Article related to pyrrolidine derivative preparation sar mcl1 inhibitor bcl2 apoptosis cancer, bcl-2, cancer, mcl-1, pyrrolidine, target, Pharmacology: Structure-Activity and other aspects.Category: amides-buliding-blocks

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