Month: October 2022

Gao, Zhenhua; Guo, Huichuang; Guo, Yongbiao; Zhu, Xiaxia published the artcile< General and Efficient Synthesis of Quinazolinones under CF3COOH Catalysis and Solvent-Free Conditions>, Computed Properties of 112253-70-0, the main research area is quinazolinone green preparation; benzamide ortho ester condensation trifluoroacetic acid catalyst.

Herein, the general and facile synthesis of quinazolinones I [R = H, 7-OH, 4-F, etc.; X = N, NH; R1 = H, Ph, 4-MeC6H4, etc.] by condensation of ortho ester as C1 synthon wirh 2-aminobenzamides and CF3COOH as the catalyst under solvent-free conditions was reported. This represented one of the most mild, practical and user-friendly methodologies with easy-separation procedure.

ChemistrySelect published new progress about Anilines Role: RCT (Reactant), RACT (Reactant or Reagent). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Computed Properties of 112253-70-0.

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

van Loevezijn, Arnold; Venhorst, Jennifer; Iwema Bakker, Wouter I.; de Korte, Cor G.; de Looff, Wouter; Verhoog, Stefan; van Wees, Jan-Willem; van Hoeve, Martijn; van de Woestijne, Rob P.; van der Neut, Martina A. W.; Borst, Alice J. M.; van Dongen, Maria J. P.; de Bruin, Natasja M. W. J.; Keizer, Hiskias G.; Kruse, Chris G. published the artcile< N'-(Arylsulfonyl)pyrazoline-1-carboxamidines as Novel, Neutral 5-Hydroxytryptamine 6 Receptor (5-HT6R) Antagonists with Unique Structural Features>, Recommanded Product: 3-Fluorobenzenesulfonamide, the main research area is arylsulfonylpyrazolinecarboxamidine hydroxytryptamine 6 receptor antagonist.

The 5-HT6 receptor (5-HT6R) has been in the spotlight for several years regarding CNS-related diseases. We set out to discover novel, neutral 5-HT6R antagonists to improve off-target selectivity compared to basic amine-containing scaffolds dominating the field. High-throughput screening identified the N’-(sulfonyl)pyrazoline-1-carboxamidine scaffold as a promising neutral core for starting hit-to-lead. Medicinal chem., mol. modeling, small mol. NMR and X-ray crystallog. were subsequently applied to optimize the leads into antagonists displaying high 5-HT6R affinity with optimal off-target selectivity. Unique structural features include a pseudoarom. system and an internal hydrogen bond freezing the bioactive conformation. While physicochem. properties and CNS availability were generally favorable, significant efforts had to be made to improve metabolic stability. The optimized structure 42 (I) is an extremely selective, hERG-free, high-affinity 5-HT6R antagonist showing good human in vitro metabolic stability. Rat pharmacokinetic data were sufficiently good to enable further in vivo profiling.

Journal of Medicinal Chemistry published new progress about 5-HT antagonists (5-HT6). 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Recommanded Product: 3-Fluorobenzenesulfonamide.

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

Sharma, Shikha; Ghosh, Sunil K.; Sharma, Joti N. published the artcile< Sorption of ruthenium by dipropylmethyl-2-(N,N-diisobutyl) acetamidoammonium iodide impregnated Amberlite XAD-4 resin from nitric acid medium>, Safety of 2-Chloro-N,N-diisobutylacetamide, the main research area is ruthenium dipropylmethyldiisobutyl acetamidoammonium iodide Amberlite impregnation nitric acid sorption.

Dipropylmethyl-2-(N,N-diisobutyl)acetamidoammonium iodide has been impregnated on Amberlite XAD-4 resin and investigated for sorption of Ru from nitric acid medium. Equilibrium sorption data for Ru uptake were represented well by the Langmuir isotherm equation (R2 = 0.98) compared to Freundlich isotherm equation (R2 = 0.86). The maximum monolayer coverage (Q0) value of 6.25 mg/g as obtained from Langmuir isotherm was close to the exptl. value (5.63 mg/g). The heterogeneity parameter (1/n) = 0.37 obtained from the slope of Freundlich isotherm indicates slight heterogeneity in sorption process. Aqueous solutions of 5% ammonia or 10% sodium hydroxide were found suitable for desorption. The method can be applied for separation of Ru from acidic waste solutions

Separation Science and Technology (Philadelphia, PA, United States) published new progress about Desorption. 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Safety of 2-Chloro-N,N-diisobutylacetamide.

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

Yu, Zhou; Fan, Wufa; Wang, Luting; He, Haisheng; Lv, Yongjiu; Qi, Jianping; Lu, Yi; Wu, Wei published the artcile< Slowing down lipolysis significantly enhances the oral absorption of intact solid lipid nanoparticles>, SDS of cas: 96829-58-2, the main research area is solid lipid nanoparticle lipolysis oral absorption.

Only a limited amount of orally administered lipid nanoparticles are absorbed as intact particles due to lipolysis by lipases in the gastrointestinal tract. It is hypothesized that by counteracting lipolysis, more particles will survive gastrointestinal digestion and be absorbed as intact particles. In this study, incorporation of a lipase inhibitor orlistat (OLST), as well as polyethylene glycol (PEG) coating, is employed to slow down the lipolysis using solid lipid nanoparticles (SLNs) as model particles. To explore the in vivo behaviors of the particles, near-IR fluorescent probes with absolute aggregation-caused quenching (ACQ) properties are used to label and track the unmodified, PEG-coated and OLST-loaded SLNs. The in vitro lipolysis study indicates very fast first-order degradation of unmodified SLNs and significantly decreased degradation of OLST-SLNs. Live imaging reveals the same trend of slowed-down lipolysis in vivo which correlates well with the in vitro lipolysis. The scanning of ex vivo gastrointestinal segments confirms the considerably prolonged residence time of OLST-SLNs, mirroring the significantly decreased lipolysis rate. The observation of fluorescence in the blood, though very weak, and in the liver speaks of the oral absorption of intact SLNs. Similarly, slowing down lipolysis also contributes to the significantly enhanced cumulative lymphatic transport of OLST-SLNs (7.56% vs. 1.27% for the unmodified SLNs).

Biomaterials Science published new progress about Biomacromolecular compounds Role: TEM (Technical or Engineered Material Use), USES (Uses). 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, SDS of cas: 96829-58-2.

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

Mishra, Ashish A.; Bhanage, Bhalchandra M. published the artcile< Electronic And Steric Effect Favored Selective Synthesis Of Asymmetric (-) N-Aryl Mandelamides>, SDS of cas: 1192620-83-9, the main research area is asym aryl mandelamide preparation enantioselective; aryl benzoyl formamide asym transfer hydrogenation ruthenium catalyst.

This work reports selective synthesis of asym. (-) α-Hydroxyl Amides like N-aryl mandelamides (S)-4-RC6H4NHC(O)CH(OH)R1 [R = H, Me; R1 = Ph, 2-fluorophenyl, 2,4,6-tris(propan-2-yl)phenyl, etc.] via asym. transfer hydrogenation (ATH) of α-keto Amides like N-aryl benzoyl formamides 4-RC6H4NH(C(O))2R1 using Ru-Tethered TsDPEN catalyst I. The electronic and steric effect at ortho position leading to high enantioselectivity for ATH of carbonyl, sandwiched between two sp2 carbon is studied. A wide range of mono and di ortho substituted α-hydroxyl amide is synthesized using this protocol with good enantioselectivity.

ChemistrySelect published new progress about Amides, hydroxy Role: SPN (Synthetic Preparation), PREP (Preparation). 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, SDS of cas: 1192620-83-9.

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

Zhao, Peng; Wang, Xiangzhu; Zhuang, Linghang; Huang, Song; Zhou, Yu; Yan, Yuna; Shen, Ru; Zhang, Fan; Li, Jie; Hu, Qiyue; Liu, Suxing; Zhang, Rumin; Dong, Ping; Wan, Hong; Bai, Chang; He, Feng; Tao, Weikang published the artcile< Discovery of novel spiro compound as RAF kinase inhibitor with in vitro potency against KRAS mutant cancer>, Synthetic Route of 112253-70-0, the main research area is RAF kinase inhibitor KRAS mutant cancer; Kinase inhibitor; Mutation; Paradoxical activation; RAF; RAS; Spiro compound.

The development of RAF inhibitors targeting cancers with wild type RAF kinase and/or RAS mutation has been challenging due to the paradoxical activation of the RAS-RAF-MEK-ERK cascade following RAF inhibitor treatment. Herein is the discovery and optimization of a series of RAF inhibitors with a novel spiro structure. The most potent spiro mol. 9 showed excellent in vitro potency against b/c RAF enzymes and RAS mutant H358 cancer cells with minimal paradoxical RAF signaling activation. Compound 9 also exhibited good drug-like properties as demonstrated by in vitro cytochrome P 450 (CYP), liver microsome stability (LMS) data and moderate oral pharmacokinetics (PK) profiles in rat and mouse.

Bioorganic & Medicinal Chemistry Letters published new progress about Animal gene Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (KRAS). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Synthetic Route of 112253-70-0.

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

Raut, Dhaval R.; Sharma, Shikha; Ghosh, Sunil K.; Mohapatra, Prasanta K. published the artcile< Glycolamide-functionalized ionic liquid: Synthesis and actinide ion extraction studies>, Related Products of 5326-82-9, the main research area is glycolamide ionic liquid fission product actinide ion extraction enthalpy.

A glycolamide-functionalized ionic liquid (G-FIL) was synthesized for the first time and was evaluated for the extraction of actinide ions such as Am3+, Pu4+ and UO22+ and fission product element ions such as Eu3+, Sr2+ and Cs+. The extraction of the trivalent metal ions was found to be exceptionally high at low acid concentrations, which rapidly decreased with increasing acidity. In view of the high viscosity of the G-FIL, the studies were carried out using its diluted solution in a com. ionic liquid, viz. 1-butyl-3-methylimidazolium bis(trifluoromethylsulfonyl)imide ([C4mim][Tf2N]).

Separation Science and Technology (Philadelphia, PA, United States) published new progress about Actinide ions. 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Related Products of 5326-82-9.

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

Zhang, Fan; Wu, Dang; Wang, Gao-Lei; Hou, Shuang; Ping, Ou-Yang; Huang, Jin; Xu, Xiao-Yong published the artcile< Synthesis and biological evaluation of novel 1,2,3-benzotriazin-4-one derivatives as leukotriene A4 hydrolase aminopeptidase inhibitors>, COA of Formula: C7H7BrN2O, the main research area is thiazolidinyl benzotriazinone preparation leukotriene hydrolase inhibition mol docking SAR.

A series of novel 1,2,3-benzotriazin-4-one derivatives I [R = H, 6-O2N, 7-Cl, etc.; X = (CH2)n; n = 0, 1, 2, 3, 4] were designed, synthesized and their inhibitory activities against leukotriene A4 hydrolase aminopeptidase in-vitro were evaluated. Many compounds showed moderate to good activities at the concentration of 10 μmol/L. Among them, compound I [R = 7-Cl; X = (CH2)4 (II)] exhibited the highest inhibitory activity up to 80.6% with an IC50 of 1.30 ± 0.20 μmol/L. The compound II was also tested for the proliferation inhibitory activities in THP1 human AML cell line and its binding model with LTA4H enzyme by mol. docking was studied. It indicated that 1,2,3-benzotriazin-4-one was a promising scaffold for further study. The relationship between structure and inhibitory activity was also preliminarily discussed.

Chinese Chemical Letters published new progress about Alkylation. 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, COA of Formula: C7H7BrN2O.

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

Manu, Peter; Lăcătuşu, Cristina-Mihaela; Rogozea, Liliana M; Cernea, Simona published the artcile< Pharmacological Management of Obesity: A Century of Expert Opinions in Cecil Textbook of Medicine.>, Synthetic Route of 96829-58-2, the main research area is .

BACKGROUND: Innovations in drug therapy for obesity have had a limited impact on the body mass index, prevalence of medical complications, quality of life, and work potential of a substantial majority of affected persons. STUDY QUESTION: What are the milestones of the changes in the expert approach to the pharmacological management of obesity in the past century? STUDY DESIGN: To determine the changes in the experts’ approach to the management of obesity, as presented in a widely used textbook in the United States. DATA SOURCES: The primary sources were chapters describing the management of obesity in the 26 editions of Cecil Textbook of Medicine published from 1927 through 2020. Secondary sources were publications retrieved from Medline that clarified technical issues related to the development, regulatory approval, and use of the drugs mentioned in the Cecil Textbook of Medicine. RESULTS: Pharmacological interventions aimed at increasing caloric expenditures through thermogenesis were recommended from 1927 through 1943. Thyroid extracts were prescribed even in the absence of demonstrated hypothyroidism or decreased basal metabolic rate throughout this period. Dinitrophenol was mentioned in 1937, but was banned soon thereafter. Appetite suppression with amphetamine was considered useful from 1943 through 1988, after which the drug was replaced with other centrally acting molecules, such as fenfluramine in 1988, sibutramine in 2000, and rimonabant in 2008, which were in turn withdrawn because of major adverse effects. In the past decade, obesity has been treated with the appetite suppressants phentermine-topiramate, bupropion-naltrexone, lorcaserin, and liraglutide, and with orlistat, a drug promoting fat malabsorption. The change in weight produced by these drugs is generally modest and transient. CONCLUSIONS: The pharmacological management of obesity has remained frustratingly inefficient. The reasons for the relative lack of success may reside in the ever-growing access to dense, palatable, and relatively inexpensive food, coupled with the decrease in energy expenditure created by a sedentary lifestyle.

American journal of therapeutics published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Synthetic Route of 96829-58-2.

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

Momoh, T. B.; Hassan, A. O.; Abaniwo, R. M.; Ojade, F. E.; Olorunnado, G. B. published the artcile< Effect of aqueous leaf extract of Uvariaopsis tripetala on hyperglycaemia, weight loss, polydipsia and polyphagia in alloxan- induced diabetic Wistar rats>, Synthetic Route of 94-20-2, the main research area is Uvariopsis leaf antidiabetic hyperglycemia weight loss polydipsia polyphagi diabetes.

Diabetes, a disorder characterized by hyperglycemia is the leading cause of death in developed, developing and underdeveloped nations around the world today. According to World Health Organization (WHO), its incidence is increasing and assuming epidemic proportions. In this chronic study the antidiabetic effect of orally administered aqueous crude leaf extract of the Uvariopsis tripetala was investigated in Alloxan (150mg/kg) induced diabetic albino rats. The results obtained indicated that after administration of the aqueous extract at different dosages (100, 200, 400 mg/kg body weight) for twenty eight (28) days, there was a time and dosedependent significant (P< 0.05) reduction in FBS on days 7, 14, 21 and 28 compared to diabetic control. The body weight of rats in the treatment groups showed no statistically significant (P>0.05) difference on days 7 and 14 compared to diabetic control. However, a dose-dependent significant (P<0.05) increase was produced by the extract when compared to the diabetic control on days 21 and 28. The extract also showed time and dose-dependent significant (P< 0.05) reduction in food and water consumption in weeks 1, 2, 3 and 4 compared to diabetic control. It was concluded that the aqueous extract of U. tripetala exhibited anti-diabetic properties. Hence this plant may serve as a good candidate for alternative and/or complimentary medicine in the management of diabetes. International Journal of Current Research in Chemistry and Pharmaceutical Sciences published new progress about Antidiabetic agents. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Synthetic Route of 94-20-2.

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