Month: October 2022

Song, Kwang-Seop; Kim, Min Ju; Seo, Hee Jeong; Lee, Sung-Han; Jung, Myung Eun; Kim, Soo-Un; Kim, Jeongmin; Lee, Jinhwa published the artcile< Synthesis and structure-activity relationship of novel diarylpyrazole imide analogues as CB1 cannabinoid receptor ligands>, Category: amides-buliding-blocks, the main research area is diarylpyrazole imide derivative preparation CB1 cannabinoid receptor antagonist.

A myriad of research groups have been engaged in searching for novel CB1 receptor antagonists, since SR141716A (rimonabant, I), a CB1 receptor antagonist, was discovered for an obesity treatment. In this research, extended series, based on the 1,5-diarylpyrazole template of rimonabant, was synthesized and tested for CB1 receptor binding affinity. In the present study, N-piperidinylcarboxamide group of rimonabant was replaced with the corresponding sulfonamide, imide, N-Me imide and methylenediamide, resp. The SAR studies to optimize the CB1 binding affinity led to the potent imide derivatives The in vivo efficacy test of a derivative II gave a promising result for this novel scaffold. In order to explore physicochem. properties (hydrophobic, steric and electronic) of the representative imide derivatives responsible for their CB1 receptor binding affinity, quant. structure activity relationship (QSAR) studies were performed. Hansch QSAR models, which were moderate in the explanation for SAR, were generated with hydrophobic, steric and electronic properties of substituents. Especially, the Taft Es-based parabolic model was obtained with the best correlation result (r 2 = 0.846).

Bioorganic & Medicinal Chemistry published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Category: amides-buliding-blocks.

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

Chen, Ming; Yang, Chao; Wang, Yanpei; Li, Dazhi; Xia, Wujiong published the artcile< UV Light Induced Direct Synthesis of Phenanthrene Derivatives from a Linear 3-Aryl-N-(arylsulfonyl) Propiolamides>, Formula: C6H6FNO2S, the main research area is phenanthrene preparation UV light induced tandem reaction arylarylsulfonyl propiolamide; photochem radical Smiles rearrangement carbon sulfur bonding Mallory reaction; gram scale reaction flow reactor phenanthrene preparation.

A novel photochem. approach for the synthesis of phenanthrene derivatives from linear 3-aryl-N-(arylsulfonyl) propiolamides via a tandem radical Smiles rearrangement/C-S bonding/Mallory reaction is disclosed. The control experiment results and isolation of the key intermediates give further insight into the reaction mechanism. Gram scale reaction using a flow reactor demonstrated the synthetic potential applications of our protocol.

Organic Letters published new progress about Alkynes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Formula: C6H6FNO2S.

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

Pilitsi, Eleni; Farr, Olivia M.; Polyzos, Stergios A.; Perakakis, Nikolaos; Nolen-Doerr, Eric; Papathanasiou, Aimilia-Eirini; Mantzoros, Christos S. published the artcile< Pharmacotherapy of obesity: Available medications and drugs under investigation>, COA of Formula: C29H53NO5, the main research area is adult obesity pharmacol management FDA approved medication drug review; Liraglutide; Lorcaserin; Naltrexone/bupropion; Obesity; Orlistat; Personalized therapy phentermine/topiramate.

A review. Obesity is a chronic disease with a continuously rising prevalence that currently affects more than half a billion people worldwide. Energy balance and appetite are highly regulated via central and peripheral mechanisms, and weight loss triggers a homeostatic response leading to weight regain. Lifestyle and behavioral modifications are the cornerstones of obesity management; however, they often fail to achieve or sustain long-term weight loss. Pharmacotherapy added onto lifestyle modifications results in an addnl., albeit limited, weight reduction Regardless, this weight reduction of 5-10% conveys multiple cardiovascular and metabolic benefits. In this review, evidence on the food and drug administration (FDA)-approved medications, i.e., orlistat, lorcaserin, phentermine/topiramate, liraglutide and naltrexone/bupropion, is summarized. Furthermore, anti-obesity agents in the pipeline for potential future therapeutic use are presented.

Metabolism, Clinical and Experimental published new progress about Pipelines. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, COA of Formula: C29H53NO5.

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

Asano, Toru; Yoshikawa, Tomohiro; Usui, Taikou; Yamamoto, Hiroshi; Yamamoto, Yoshinori; Uehara, Yoshimasa; Nakamura, Hiroyuki published the artcile< Benzamides and benzamidines as specific inhibitors of epidermal growth factor receptor and v-Src protein tyrosine kinases>, Product Details of C9H12N2O3, the main research area is EGF receptor tyrosine kinase inhibitor design cytotoxic.

The benzamides 1 and the benzamidines 2 as well as the cyclic benzamidines 3 were designed and synthesized as the mimics of 4-anilinoquinazolines for an inhibitor of EGFR tyrosine kinase. The specific inhibitions of EGFR tyrosine kinase were observed in the benzamides 1c and 1d, and the benzamidine 2a, whereas the specific inhibitions of v-Src kinase were observed in the benzamide 1j and the benzamidine 2d at a 10 μg/mL concentration of compounds The cyclic benzamidines 3a and 3b showed potent kinase inhibition of EGFR at a 1.0 μg/mL concentration According to the docking simulation using the x-ray structure of EGFR kinase domain in complex with erlotinib, the LigScore2 scoring function value of erlotinib was calculated as 5.61, whereas that of the benzamide 1c was 5.05. In a similar manner, the LigScore2 value of the cyclic benzamidine 3a was calculated as 5.10.

Bioorganic & Medicinal Chemistry published new progress about Cytotoxic agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Product Details of C9H12N2O3.

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

Zhou, Hai-Shan; Hu, Lv-Bin; Zhang, Han; Shan, Wen-Xin; Wang, Yan; Li, Xue; Liu, Tian; Zhao, Jing; You, Qi-Dong; Jiang, Zheng-Yu published the artcile< Design, Synthesis, and Structure-Activity Relationships of Indoline-Based Kelch-like ECH-Associated Protein 1-Nuclear Factor (Erythroid-Derived 2)-Like 2 (Keap1-Nrf2) Protein-Protein Interaction Inhibitors>, Quality Control of 6961-82-6, the main research area is indoline design synthesis cardioprotective Keap1 Nrf2 protein interaction inhibition.

The Keap1 (Kelch-like ECH-associated protein 1)-Nrf2 (nuclear factor erythroid 2-related factor 2)-ARE (antioxidant response element) pathway is the major defending mechanism against oxidative stresses, and directly disrupting the Keap1-Nrf2 protein-protein interaction (PPI) has been an attractive strategy to target oxidative stress-related diseases, including cardiovascular diseases. Here, we describe the design, synthesis, and structure-activity relationships (SARs) of indoline-based compounds as potent Keap1-Nrf2 PPI inhibitors. Comprehensive SAR anal. and thermodn.-guided optimization identified I as the most potent inhibitor in this series, with an IC50 of 22 nM in a competitive fluorescence polarization assay. Further evaluation indicated the proper drug-like properties of I. I dose-dependently upregulated genes and protein level of Nrf2 as well as its downstream markers and showed protective effects against lipopolysaccharide-induced injury in both H9c2 cardiac cells and mouse models. Collectively, we reported here a novel indoline-based Keap1-Nrf2 PPI inhibitor as a potential cardioprotective agent.

Journal of Medicinal Chemistry published new progress about Cardioprotective agents. 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Quality Control of 6961-82-6.

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

Talamas, Francisco X.; Abbot, Sarah C.; Anand, Shalini; Brameld, Ken A.; Carter, David S.; Chen, Jun; Davis, Dana; de Vicente, Javier; Fung, Amy D.; Gong, Leyi; Harris, Seth F.; Inbar, Petra; Labadie, Sharada S.; Lee, Eun K.; Lemoine, Remy; Le Pogam, Sophie; Leveque, Vincent; Li, Jim; McIntosh, Joel; Najera, Isabel; Park, Jaehyeon; Railkar, Aruna; Rajyaguru, Sonal; Sangi, Michael; Schoenfeld, Ryan C.; Staben, Leanna R.; Tan, Yunchou; Taygerly, Joshua P.; Villasenor, Armando G.; Weller, Paul E. published the artcile< Discovery of N [4-[6-tert-Butyl-5-methoxy-8-(6-methoxy-2-oxo-1H-pyridin-3-yl)-3-quinolyl]phenyl]-methanesulfonamide (RG7109), a Potent Inhibitor of the Hepatitis C Virus NS5B Polymerase>, Application In Synthesis of 112253-70-0, the main research area is oxopyridinyl butylquinolinylphenyl methanesulfonamide preparation hepatitis C virus polymerase inhibitor.

In the past few years, there have been many advances in the efforts to cure patients with hepatitis C virus (HCV). The ultimate goal of these efforts is to develop a combination therapy consisting of only direct-antiviral agents (DAAs). In this paper, we discuss our efforts that led to the identification of a bicyclic template with potent activity against the NS5B polymerase, a critical enzyme on the life cycle of HCV. In continuation of our exploration to improve the stilbene series, the 3,5,6,8-tetrasubstituted quinoline core was identified as replacement of the stilbene moiety. 6-Methoxy-2-(1H)-pyridone was identified among several heterocyclic headgroups to have the best potency. Solubility of the template was improved by replacing a planar aryl linker with a saturated pyrrolidine. Profiling of the most promising compounds led to the identification of quinoline I (RG7109), which was selected for advancement to clin. development.

Journal of Medicinal Chemistry published new progress about Antiviral agents (hepatitis C). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Application In Synthesis of 112253-70-0.

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

Narasimhamurthy, Kereyagalahally H.; Chandrappa, Siddappa; Sharath Kumar, Kothanahally S.; Harsha, Kachigere B.; Ananda, Hanumappa; Rangappa, Kanchugarakoppal S. published the artcile< Easy access for the synthesis of 2-aryl 2,3-dihydroquinazolin-4(1H)-ones using gem-dibromomethylarenes as synthetic aldehyde equivalent>, Recommanded Product: 2-Amino-4,5-dimethoxybenzamide, the main research area is quinazolinone dihydro aryl preparation.

One step synthesis of 2,3-dihydroquinazolin-4(1H)-ones I (R = H, Cl, OCH3; R1 = H, Br, Cl, OCH3; Ar = 3-ClC6H4, 4-pyridyl, 4-CF3C6H4, etc.) from gem-dibromomethylarenes ArCH(Br)2 using 2-aminobenzamide is described. Gem-dibromomethylarenes are used as aldehyde equivalent for the efficient synthesis of 2,3-dihydroquinazolin-4(1H)-ones, this synthesis takes shorter reaction time with quick isolation and excellent product yield.

RSC Advances published new progress about Amino amides Role: RCT (Reactant), RACT (Reactant or Reagent). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Recommanded Product: 2-Amino-4,5-dimethoxybenzamide.

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

Fang, Zhijia; Wills, Martin published the artcile< Asymmetric Transfer Hydrogenation of Functionalized Acetylenic Ketones>, HPLC of Formula: 1192620-83-9, the main research area is acetylenic ketone diketone ruthenium catalyzed stereoselective transfer hydrogenation; propargylic alc yashabushidiol B stereoselective preparation.

A systematic study of the asym. transfer hydrogenations of functionalized acetylenic ketones and diketones has been completed, together with a total synthesis of (S,S)-(-)-yashabushidiol B. In several cases, excellent enantioselectivities and yields were achieved.

Journal of Organic Chemistry published new progress about Alcohols, propargyl Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (chiral). 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, HPLC of Formula: 1192620-83-9.

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

Gediya, Shweta K.; Vyas, Vijyesh K.; Clarkson, Guy J.; Wills, Martin published the artcile< Asymmetric Transfer Hydrogenation of α-Keto Amides; Highly Enantioselective Formation of Malic Acid Diamides and α-Hydroxyamides>, COA of Formula: C30H31ClN2O2RuS, the main research area is hydroxydiamide regioselective enantioselective preparation; oxodiamide ruthenium chiral diamine catalyst asym transfer hydrogenation; hydroxyamide regioselective enantioselective preparation; oxoamide ruthenium chiral diamine catalyst asym transfer hydrogenation.

The asym. transfer hydrogenation (ATH) of α-keto-1,4-diamides using a tethered Ru/TsDPEN catalyst was achieved in high ee. Studies on derivatives identified the structural elements which led to the highest enantioselectivities in the products. The α-keto-amide reduction products were converted to a range of synthetically valuable derivatives

Organic Letters published new progress about Acetamides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 1192620-83-9 belongs to class amides-buliding-blocks, and the molecular formula is C30H31ClN2O2RuS, COA of Formula: C30H31ClN2O2RuS.

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

Vats, B. G.; Kannan, S.; Pius, I. C.; Noronha, D. M.; Maity, D. K.; Drew, M. G. B. published the artcile< Synthetic, structural, extraction and theoretical studies of uranyl nitrate dithio-diglycolamide compounds>, Safety of 2-Chloro-N,N-diisobutylacetamide, the main research area is crystal structure thioglycolamide thiotolylamide uranyl complex preparation actinide extraction; optimized mol structure glycolamide thioglycolamide uranyl monodentate bidentate extraction.

Dithio-diglycolamide ligands [(CH2SCH2CONR2)2] (R = iPr, Bu, iBu, C8H17) and [C7H6(SCH2CONR2)2] (R = iBu) were prepared and characterized. The complex chem. of these ligands with uranyl nitrate was studied using IR, NMR and ESI-MS techniques and elemental anal. The structures for two of the compounds, [UO2(NO3)2(CH2SCH2CONBu2)2] (2) and [UO2(NO3)2C7H6(SCH2CON{iBu}2)2] (4), were determined by the x-ray diffraction method and revealed a bidentate chelating mode of bonding for the ligands in the solid state. The structures further show that the uranyl group is surrounded by six O atoms in a hexagonal bi-pyramidal geometry. Theor. studies were carried out to explain the relative stability of this chelating mode of ligand bonding. Extraction studies of U(VI), Pu(IV) and Am(III) ions from HNO3 by one of the ligands, [(CH2SCH2CON{C8H17}2)2] (L4), in dodecane show appreciable extractions The extracted metal ions could be back extracted quant. using 0.5M HNO3 or a mixture of 0.5 M HNO3 and 0.5M H2C2O4.

Polyhedron published new progress about Actinide ions Role: PEP (Physical, Engineering or Chemical Process), PROC (Process). 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