Author: Jessica.F

Agbaje, Olorunsola F.; Coleman, Ruth L.; Hattersley, Andrew T.; Jones, Angus G.; Pearson, Ewan R.; Shields, Beverley M.; Holman, Rury R. published the artcile< Predicting post one-year durability of glucose-lowering monotherapies in patients with newly-diagnosed type 2 diabetes mellitus - A MASTERMIND precision medicine approach (UKPDS 87)>, Application In Synthesis of 94-20-2, the main research area is durability glucose monotherapy diabetes mellitus; Durability; Glucose-lowering agents; Modelling; Monotherapy failure; Precision medicine.

Predicting likely durability of glucose-lowering therapies for people with type 2 diabetes (T2D) could help inform individualised therapeutic choices. We used data from UKPDS patients with newly-diagnosed T2D randomised to first-line glucose-lowering monotherapy with chlorpropamide-glibenclamide-basal insulin or metformin. In 2339 participants who achieved one-year HbA1c values <7.5% (<59 mmol/mol)-we assessed relationships between one-year characteristics and time to monotherapy-failure (HbA1c ≥ 7.5% or requiring second-line therapy). Model validation was performed using bootstrap sampling.Follow-up was median (IQR) 11.0 (8.0-14.0) years. Monotherapy-failure occurred in 72%-82%-75% and 79% for those randomised to chlorpropamide-glibenclamide-basal insulin or metformin resp.-after median 4.5 (3.0-6.6)-3.7 (2.6-5.6)-4.2 (2.7-6.5) and 3.8 (2.6- 5.2) years. Time-to-monotherapy-failure was predicted primarily by HbA1c and BMI values-with other risk factors varying by type of monotherapy-with predictions to within ±2.5 years for 55%-60%-56% and 57% of the chlorpropamide-glibenclamide-basal insulin and metformin monotherapy cohorts resp. Post one-year glycemic durability can be predicted robustly in individuals with newly-diagnosed T2D who achieve HbA1c values < 7.5% one year after commencing traditional monotherapies. Such information could be used to help guide glycemic management for individual patients. Diabetes Research and Clinical Practice published new progress about Durability of materials. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Application In Synthesis of 94-20-2.

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

Kim, Dae Hun; Maharjan, Pooja; Kim, Jae Yeol; Jang, Dong-Jin; Koo, Tae-Sung; Min, Kyoung Ah; Cho, Kwan Hyung published the artcile< Enhanced solubility, in-vitro dissolution and lipase inhibition of a self-nanoemulsifying drug delivery system containing orlistat>, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is orlistat lipase solubility dissolution gastrointestinal lumen SNEDDS.

The aim of this work was to prepare and assess a self-nanoemulsifying drug delivery system (SNEDDS) containing water-insoluble orlistat that was used for the inhibition of lipase activity in gastrointestinal lumen. The pseudo-ternary phase diagram, composed of orlistat and medium chain triglycerides (MCT) as oil phase and Cremophor EL as surfactant, was made for the confirmation of giving SNEDDS preconc. The phys. state, particle size dispersed in water, dissolution and lipase inhibition of SNEDDS preconcs. were investigated. The appointed SNEDDS preconcs. in the pseudo-ternary phase diagram showed no endothermic peak of orlistat and a liquid state. The particle sizes of SNEDDS dispersed with water were uniform and in the range of <200 nm. In the dissolution test, the liquid SNEDDS preconc. and solid state mixture exhibited 90.89 ± 2.03% vs. 22.42 ± 3.71% at 60 min., resp., whereas the raw orlistat showed no significant dissolution rate. The SNEDDS preconc. showed a lipase inhibition of 92.42 ± 1.58% until 60 min., with no significant inhibition activity of orlistat. Therefore, the SNEDDS preconc. presented in this work solubilized orlistat and increased its dissolution rate, and resulted in sufficient inhibitory action on lipase. Journal of Nanoscience and Nanotechnology published new progress about Castor oil, ethoxylated Role: MOA (Modifier or Additive Use), PAC (Pharmacological Activity), THU (Therapeutic Use), USES (Uses), BIOL (Biological Study). 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

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

Venkateswarlu, Somepalli; Satyanarayana, Meka; Lakshmikanthan, Vijaybaskar; Siddaiah, Vidavalur published the artcile< Fused Quinazolinoquinazolinones: Synthesis, Isomerization, Spectroscopic Identification, and Anticancer Activity>, Quality Control of 5004-88-6, the main research area is EGFR tyrosine kinase anticancer fused quinazolino quinazolinone; fused quinazolino quinazolinone preparation anticancer.

13H-quinazolino[3,4-a]quinazolin-13-ones have been synthesized from 2-aminobenzamides in four steps. An acid-catalyzed or base-catalyzed isomerization of 13H-quinazolino[3,4-a]quinazolin-13-ones to 8H-quinazolino[4,3-b]quinazolin-8-ones in excellent yields (90-95%) has been reported. The differences in the IR and NMR (1H & 13C) data of these isomeric fused quinazolinoquinazolinones afford a useful method for distinguishing between the two series. These analogs showed moderate anticancer activity (EGFR-TK inhibition).

Journal of Heterocyclic Chemistry published new progress about Epidermal growth factor receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Quality Control of 5004-88-6.

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

Singh, Imocha Rajkumar; Mitra, Sivaprasad published the artcile< Modulated Protein Binding Ability of Anti-Diabetic Drugs in Presence of Monodispersed Gold Nanoparticles and its Inhibitory Potential towards Advanced Glycated End (AGE) Product Formation>, SDS of cas: 94-20-2, the main research area is gold nanoparticle delivery advanced glycated end antidiabetic agent; AGE product; Drug binding; Fluorescence; Nanomedicine; Serum albumin.

Binding strength of the anti-diabetic drugs chlorpropamide (CPM) and tolbutamide (TBM) with model protein bovine serum albumin (BSA) shows strong modulation in presence of colloidal gold nanoparticles (AuNP). Intrinsic tryptophan fluorescence of both the native BSA and BSA-AuNP conjugate quenched in presence of the drugs. Stern-Volmer quenching constant (KSV) of CPM binding to BSA-AuNP conjugate at different temperatures is almost twice (6.76∼14.76 x 103 M-1) than the corresponding values in native BSA (3.21∼5.72 x 103 M-1). However, the calculated KSV values with TBM show certain degree of reduction in presence of AuNP (6.46x 103 M-1), while comparing with native BSA (8.83 x 103 M-1). The binding mode of CPM towards BSA-AuNP conjugate is mainly through hydrophobic forces; whereas, TBM binding is identified to be Van der Waal’s and hydrogen bonding type of interaction. Fluorescence lifetime anal. confirms static type of quenching for the intrinsic tryptophan fluorescence of BSA as well as BSA-AuNP conjugate with addition of CPM and TBM at different concentrations The α-helical content in the secondary structure of BSA is decreased to 48.32% and 45. 28% in presence of AuNP, when the concentration of CPM is 0.08 mM and 0.16 mM in comparison with that of native protein (50.13%). On the other hand, the intensity of sugar induced advanced glycated end (AGE) product fluorescence is decreased by 55% and 80% at 0.13 nM and 0.68 nM AuNP, resp. Change in the binding strength of the drugs with transport protein and reduced AGE product formation in presence of AuNP could lead to a major development in the field of nanomedicine and associated drug delivery techniques. Graphical AbstractModulated drug binding ability and AGE product formation of serum proteins in presence of AuNP [graphic not available: see fulltext].

Journal of Fluorescence published new progress about Adsorption. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, SDS of cas: 94-20-2.

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

Belhani, Billel; Berredjem, Malika; Le Borgne, Marc; Bouaziz, Zouhair; Lebreton, Jacques; Aouf, Nour-Eddine published the artcile< A one-pot three-component synthesis of novel α-sulfamidophosphonates under ultrasound irradiation and catalyst-free conditions>, Safety of Morpholine-4-sulfonamide, the main research area is alpha sulfamidophosphonate preparation green chem; benzaldehyde sulfamide trialkylphosphite sonication three component reaction.

An efficient and convenient one-pot synthesis of novel α-sulfamidophosphonates was described via a three-component reaction. This reaction was carried out through a three component condensation reaction of sulfamide, an aromatic aldehyde and trialkylphosphite under conventional/ultrasonic techniques, catalyst-free and solvent-free conditions. This methodol. was established with many advantages, including mild reaction conditions, short reaction times, good yields, simple work-up procedures and environmental friendliness.

RSC Advances published new progress about Condensation reaction. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Safety of Morpholine-4-sulfonamide.

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

Wang, Ze; Zhao, Junli; Ma, Xiang; Sun, Yun; Hao, Guimin; Yang, Aijun; Ren, Wenchao; Jin, Lei; Lu, Qun; Wu, Gengxiang; Ling, Xiufeng; Hao, Cuifang; Zhang, Bo; Liu, Xinyu; Yang, Dongzi; Zhu, Yimin; Li, Jing; Bao, Hongchu; Wang, Ancong; Liu, Jianqiao; Chen, Zi-Jiang; Tan, Jichun; Shi, Yuhua published the artcile< Effect of Orlistat on Live Birth Rate in Overweight or Obese Women Undergoing IVF-ET: A Randomized Clinical Trial.>, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is IVF; live birth; obesity management; orlistat; weight loss.

CONTEXT: Obesity management prior to infertility treatment remains a challenge. To date, results from randomized clinical trials involving weight loss by lifestyle interventions have shown no evidence of improved live birth rate. OBJECTIVE: This work aimed to determine whether pharmacologic weight-loss intervention before in vitro fertilization and embryo transfer (IVF-ET) can improve live birth rate among overweight or obese women. METHODS: We conducted a randomized, double-blinded, placebo-controlled trial across 19 reproductive medical centers in China, from July 2017 to January 2019. A total of 877 infertile women scheduled for IVF who had a body mass index of 25 or greater were randomly assigned to receive orlistat (n = 439) or placebo (n = 438) treatment for 4 to 12 weeks. The main outcome measurement was the live birth rate after fresh ET. RESULTS: The live birth rate was not significantly different between the 2 groups (112 of 439 [25.5%] with orlistat and 112 of 438 [25.6%] with placebo; P = .984). No significant differences existed between the groups as to the rates of conception, clinical pregnancy, or pregnancy loss. A statistically significant increase in singleton birth weight was observed after orlistat treatment (3487.50 g vs 3285.17 g in the placebo group; P = .039). The mean change in body weight during the intervention was -2.49 kg in the orlistat group, as compared to -1.22 kg in the placebo group, with a significant difference (P = .005). CONCLUSION: Orlistat treatment, prior to IVF-ET, did not improve the live birth rate among overweight or obese women, although it was beneficial for weight reduction.

The Journal of clinical endocrinology and metabolism published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Recommanded Product: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate.

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

Zhang, Weikang; Meng, Chong; Liu, Yan; Tang, Yawen; Li, Feng published the artcile< Auto-Tandem Catalysis with Ruthenium: From o-Aminobenzamides and Allylic Alcohols to Quinazolinones via Redox Isomerization/Acceptorless Dehydrogenation>, COA of Formula: C9H12N2O3, the main research area is quinazolinone preparation; aminobenzamide alc tandem redox isomerization dehydrogenation ruthenium catalyst microwave.

A strategy for the synthesis of quinazolinones I [R = H, 7-Me, 6,8-di-Cl, etc.; R1 = Et, i-Pr, n-Bu, etc.; R2 = H, n-Bu, Bn] was proposed via Ru-catalyzed redox isomerization/acceptorless dehydrogenation of o-aminobenzamides with allylic alcs. and was obtained in moderate to high yields. This strategy was attractive due to high atom efficiency, minimal consumption of chems. and energy.

Advanced Synthesis & Catalysis published new progress about Allylic alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, COA of Formula: C9H12N2O3.

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

Ma, Tao; Hua, Jiawei; Bian, Mixue; Qin, Hong; Lin, Xinxin; Yang, Xiaobing; Liu, Chengkou; Yang, Zhao; Fang, Zheng; Guo, Kai published the artcile< Visible light-promoted aerobic oxidative cleavage and cyclization of olefins to access 3-hydroxy-isoindolinones>, Related Products of 6961-82-6, the main research area is alkenylbenzamide iron catalyst photochem regioselective aerobic oxidative cleavage heterocyclization; hydroxy isoindolinone preparation green chem.

A convenient and environmentally friendly synthetic route from 2-vinylbenzimides to 3-hydroxy-isoindolinones through visible light-promoted transformations via iron/disulfide catalysis and mol. oxygen oxidation was developed. A range of 3-hydroxy-isoindolinones were obtained in moderate to good yields, which exhibited excellent functional group compatibility and broad substrate scope. Further mechanistic investigations proved that dioxetane might be a key intermediate being involved in the reaction.

Organic Chemistry Frontiers published new progress about Amines Role: PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Related Products of 6961-82-6.

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

Narasimhamurthy, K. H.; Girish, Y. R.; Thimmaraju, N.; Rangappa, K. S. published the artcile< Utility of ZrO2-Al2O3 in the synthesis of 2,3-dihydroquinazolin-4(1H)-ones>, Safety of 2-Amino-4-bromobenzamide, the main research area is zirconium dioxide aluminum oxide acid nanocatalyst preparation surface structure; aminobenzamide aldehyde zirconium dioxide aluminum oxide nanocatalyst cyclocondensation; quinazolinone dihydro preparation zirconium dioxide alumina nanocatalyst.

In this paper, the authors report the synthesis of a nano acid catalyst ZrO2-Al2O3 by using urea as a fuel and the evaluation of its catalytic efficiency in the synthesis of a series of novel substituted dihydroquinazolinones. The catalyst was found to be a highly effective solid acid catalyst and it exhibited significant catalytic activity in converting substituted 2-aminobenzamides into the corresponding 2,3-dihydroquinazolin-4(1H)-ones under mild conditions. The optimized synthetic method is facile, rapid and efficient and may emerge as one of the best methodologies for accessing pharmaceutically useful dihydroquinazolines.

Chemical Data Collections published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Safety of 2-Amino-4-bromobenzamide.

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

Xia, Y.; Yang, Z.-Y.; Hour, M.-J.; Kuo, S.-C.; Xia, P.; Bastow, K. F.; Nakanishi, Y.; Nampoothiri, P.; Hackl, T.; Hamel, E.; Lee, K.-H. published the artcile< Antitumor Agents. Part 204:1 Synthesis and Biological Evaluation of Substituted 2-Aryl Quinazolinones>, Synthetic Route of 5004-88-6, the main research area is quinazolinone aryl preparation antitumor HIV agent; tubulin polymerization inhibitor arylquinazolinone preparation.

A series of 2-aryl-quinazolinones I (R6 = R7 = H, R2′ = F, R3′ = H, R4′ = H; R6 = R7 = H, R2′ = H, R3′ = F, R4′ = H; R6 = R7 = H, R2′ = H, R3′ = H, R4′ = F; R6 = R7 = OMe, R2′ = F, R3′ = H, R4′ = H; R6 = R7 = OMe, R2′ = H, R3′ = F, R4′ = H; R6 = R7 = OMe, R2′ = H, R3′ = H, R4′ = F; R6 = R7 = H, OMe, R2′ = H, R3’R4′ = CH:CHCH:CH; R6 = R7 = H, R2′ = H, R3′ = OMe, R4′ = H; R6 = OMe, R7 = H, R2′ = H, R3′ = OMe, R4′ = H; R6 = R7 = OMe, R2′ = H, R3′ = OMe, R4′ = H) was synthesized and evaluated for biol. activity. Among them, I (R6 = OMe, R7 = H, R2′ = H, R3′ = OMe) displayed significant growth inhibitory action against a panel of tumor cell lines and was also a potent inhibitor of tubulin polymerization Quinazolinones I (R6 = R7 = H, R2′ = F, R3′ = H, R4′ = H; R6 = R7 = H, R2′ = H, R3′ = F, R4′ = H; R6 = R7 = H, R2′ = H, R3′ = H, R4′ = F) displayed selective activity against P-gp-expressing epidermoid carcinoma of the nasopharynx. Anti-HIV activity of some of the prepared quinazolinones in acutely infected H9 lymphocytes was also assayed.

Bioorganic & Medicinal Chemistry Letters published new progress about Anti-HIV agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Synthetic Route of 5004-88-6.

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