Category: amides-buliding-blocks

Schierle, Simone; Flauaus, Cathrin; Heitel, Pascal; Willems, Sabine; Schmidt, Jurema; Kaiser, Astrid; Weizel, Lilia; Goebel, Tamara; Kahnt, Astrid S.; Geisslinger, Gerd; Steinhilber, Dieter; Wurglics, Mario; Rovati, G. Enrico; Schmidtko, Achim; Proschak, Ewgenij; Merk, Daniel published the artcile< Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology>, SDS of cas: 1524-40-9, the main research area is zafirlukast urea synthesis antiinflammatory pharmacokinetics PPAR cysteinyl leukotriene receptor.

Multitarget design offers access to bioactive small mols. with potentially superior efficacy and safety. Particularly multifactorial chronic inflammatory diseases demand multiple pharmacol. interventions for stable treatment. By minor structural changes, we have developed a close analog of the cysteinyl-leukotriene receptor antagonist zafirlukast that simultaneously inhibits soluble epoxide hydrolase and activates peroxisome proliferator-activated receptor γ. The triple modulator exhibits robust anti-inflammatory activity in vivo and highlights the therapeutic potential of designed multitarget agents.

Journal of Medicinal Chemistry published new progress about Cysteinyl leukotriene receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (antagonists). 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, SDS of cas: 1524-40-9.

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

Mao, Zhifan; Liu, Wenwen; Huang, Yunyuan; Sun, Tianyue; Bao, Keting; Feng, Jiali; Moskalev, Alexey; Hu, Zelan; Li, Jian published the artcile< Anti-aging effects of chlorpropamide depend on mitochondrial complex-II and the production of mitochondrial reactive oxygen species>, SDS of cas: 94-20-2, the main research area is chlorpropamide antiaging agent mitochondrial complex2 aging; ATP sensitive potassium channels; Anti-aging; Chlorpropamide; Mitochondrial complex II; Mitochondrial reactive oxygen species; Senescence; Succinate dehydrogenase; Sulfonylureas.

Sulfonylureas are widely used oral anti-diabetic drugs. However, its long-term usage effects on patients lifespan remain controversial, with no reports of influence on animal longevity. Hence, the anti-aging effects of chlorpropamide along with glimepiride, glibenclamide, and tolbutamide were studied with special emphasis on the interaction of chlorpropamide with mitochondrial ATP-sensitive K+ (mitoK-ATP) channels and mitochondrial complex II. Chlorpropamide delayed aging in Caenorhabditis elegans, human lung fibroblast MRC-5 cells and reduced doxorubicin-induced senescence in both MRC-5 cells and mice. In addition, the mitochondrial membrane potential and ATP levels were significantly increased in chlorpropamide-treated worms, which is consistent with the function of its reported targets, mitoK-ATP channels. Increased levels of mitochondrial reactive oxygen species (mtROS) were observed in chlorpropamide-treated worms. Moreover, the lifespan extension by chlorpropamide required complex II and increased mtROS levels, indicating that chlorpropamide acts on complex II directly or indirectly via mitoK-ATP to increase the production of mtROS as a pro-longevity signal. This study provides mechanistic insight into the anti-aging effects of sulfonylureas in C. elegans.

Acta Pharmaceutica Sinica B published new progress about Aging, animal. 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

Baruah, Prayasee; Das, Abhinandan; Paul, Debojit; Chakrabarty, Suman; Aguan, Kripamoy; Mitra, Sivaprasad published the artcile< Sulfonylurea Class of Antidiabetic Drugs Inhibit Acetylcholinesterase Activity: Unexplored Auxiliary Pharmacological Benefit toward Alzheimer's Disease>, SDS of cas: 94-20-2, the main research area is antidiabetic sulfonylurea drugrepurposing AChE inhibitor Alzheimer’s.

Contemporary literature documents extensive research on common causative mechanisms, pathogenic pathways and dual effective remedies for Alzheimer’s disease (AD) and Type 2 diabetes mellitus (T2DM). Tolbutamide (TBM), chlorpropamide (CPM), and glyburide (GLY) are three sulfonylurea antidiabetic drugs of different generations. All these drugs were found to exhibit moderate to strong inhibitory efficiency on the neurotransmitter degrading enzyme acetylcholinesterase (AChE) with GLY (IC50 = 0.74 ± 0.02μM) being the most potent, followed by CPM (IC50 = 5.72 ± 0.24μM) and TBM (IC50 = 28.9 ± 1.60μM). Notably, the inhibition efficiency of GLY is even comparable with the FDA approved AD drug, donepezil (DON). The larger size of GLY spans almost the full gorge of AChE ranging from catalytic active site (CAS) to the peripheral active site (PAS) with relatively strong binding affinity (6.0 x 105 M-1) and acts as a competitive inhibitor for AChE. On the other hand, while they show relatively weak binding ((2-6) x 104 M-1), both CPM and TBM act as noncompetitive binders. While these two drugs can bind to PAS, MD simulation results predict an alternative noncompetitive inhibition mechanism for CPM. These results open the possibility of repurposing the antidiabetic drugs, particularly GLY, in the treatment of AD. The consequential side effect of excess acetylcholine production, due to the administration of these drugs to AD-unaffected patients, can be rectified by using colloidal gold and silver nanofluids as potential AChE activity boosters.

ACS Pharmacology & Translational Science published new progress about Alzheimer disease. 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

Singh, Awadhesh Kumar; Singh, Ritu published the artcile< Pharmacotherapy in obesity: a systematic review and meta-analysis of randomized controlled trials of anti-obesity drugs>, Application In Synthesis of 96829-58-2, the main research area is meta analysis obesity orlistat phentermine lorcaserin topiramate naltrexone pharmacotherapy; Obesity; anti-obesity drugs; liraglutide 3.0 mg; lorcaserin; naltrexone plus bupropion; orlistat; phentermine plus topiramate.

Meta-anal. of obesity poses a significant increase in morbidity and mortality and thus five anti-obesity drugs have been approved currently by US FDA. Several phase 3 trials have shown a significant improvement in cardio-metabolic profile including significant weight reduction with these agents compared to placebo. We systematically searched the database of PubMed, Embase, The Cochrane Library and The ClinicalTrials.gov up to 30 Sept. 2019 and retrieved all the randomized controlled trials (RCTs) that were conducted with these five drugs for ≥1 yr and explicitly reported their efficacy vs. placebo. Subsequently, we have conducted the meta-anal. to primarily study the effect of these anti-obesity drugs on weight reduction We addnl. reviewed the effect of these drugs on other cardio-metabolic parameters including key adverse events. This meta-anal. finds a significant reduction in body weight with orlistat (N = 10,435; Δ -3.07 Kg, 95% CI, -3.76 to -2.37), phentermine plus topiramate (N = 2985; Δ -9.77 Kg; 95% CI, -11.73 to -7.81), lorcaserin (N = 16,856; Δ -3.08 Kg; 95% CI, -3.49 to -2.66), naltrexone plus bupropion (N = 3239; Δ -4.39 Kg; 95% CI, -5.05 to -3.72) and liraglutide (N = 4978; Δ -5.25 Kg; 95% CI, -6.17 to -4.32), compared to placebo (all p < 0.00001). Expert Review of Clinical Pharmacology published new progress about Antiobesity agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Application In Synthesis of 96829-58-2.

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

Rohokale, Rajendra S.; Kalshetti, Rupali G.; Ramana, Chepuri V. published the artcile< Iridium(III)-Catalyzed Alkynylation of 2-(Hetero)arylquinazolin-4-one Scaffolds via C-H Bond Activation>, Application of C9H12N2O3, the main research area is alkynylarylquinazolinone derivative preparation; arylquinazolinone ethynylbenziodoxolone alkynylation iridium catalyst.

The directed C-H alkynylation of 2-(hetero)arylquinazolin-4-ones has been explored with the ethynylbenziodoxolone reagent TIPS-EBX employing an Ir(III) catalyst. Complementary conditions for either monoalkynylation or dialkynylation have been developed. Also demonstrated is the broad scope of this reaction and the compatibility of various functional groups such as -F, -Cl, -Br, -CF3, -OMe, -NO2, and alkyl, etc.

Journal of Organic Chemistry published new progress about Alkynylation. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Application of C9H12N2O3.

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

Chen, Wei; Li, Yuxin; Zhou, Yunyun; Ma, Yi; Li, Zhengming published the artcile< Design, synthesis and SAR study of novel sulfonylurea derivatives containing arylpyrimidine moieties as potential anti-phytopathogenic fungal agents>, HPLC of Formula: 6961-82-6, the main research area is sulfonyl urea pyrimidinyl preparation plant pathogen antifungal activity.

Herein, three series of novel sulfonylureas (SUs) containing aromatic-substituted pyrimidines I (Ar = 4-methylphenyl, 2-furyl, 2-thienyl; R1 = H, Cl, Br, I; R2 = NO2, COOMe, Cl; R3 = H, NO2) were designed and synthesized according to pharmacophore-combination and bioisosterism strategy. The in vitro fungicidal activities against ten phytopathogenic fungi indicated that most of the title compounds I exhibited broad-spectrum and excellent fungicidal activities. Based on the preliminary fungicidal activities, a CoMFA model was constructed and the 3D-QSAR anal. indicated that either a bulky group around the 5-position of the pyrimidine ring or electropos. group around the 2-position of the benzene ring would be favor to fungicidal activities. In order to study interaction mechanism, compound I (Ar = 2-furyl; R1 = Br; R2 = Cl; R3 = H) was automatically docked into yeast acetohydroxyacid synthase (AHAS) and it further indicated that bearing bulky groups-aryl at the pyrimidine ring was critical to enhance antifungal activities. It revealed that the antifungal activity of derivatives I probably results from the inhibition of fungal AHAS. Thus, the present results strongly showed that SUs should be considered as lead compounds or model mols. to develop novel anti-phytopathogenic fungal agents.

Chinese Chemical Letters published new progress about Agrochemical fungicides. 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, HPLC of Formula: 6961-82-6.

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

Ruhela, R.; Panja, S.; Singh, A. K.; Dhami, P. S.; Gandhi, P. M. published the artcile< BenzoDODA grafted polymeric resin-Plutonium selective solid sorbent>, Recommanded Product: 2-Chloro-N,N-diisobutylacetamide, the main research area is wastewater treatment sorption plutonium polymeric resin; BenzoDODA SDVB resin; Plutonium; Selective; Separation; Sorption.

A new ligand grafted polymeric resin (BenzoDODA SDVB) was synthesized by covalently attaching plutonium selective ligand (BenzoDODA) on to styrene divinyl benzene (SDVB) polymer matrix. BenzoDODA SDVB resin was evaluated for separation and recovery of plutonium(IV) from nitric acid medium. Sorption of Pu(IV) was found to decrease with the increase in nitric acid concentration, with very small sorption above 7.0 M HNO3. Sorption kinetics was fast enough to achieve the equilibrium within 60 min of contact where the kinetic data fitted well to pseudo-second-order model. Sorption isotherm data fitted well to Langmuir model suggesting chem. interaction between the BenzoDODA moiety and plutonium(IV) ions. Sorption studies with some of representative radionuclides of high level waste showed that BenzoDODA SDVB is selective and therefore could be a promising solid sorbent for separation and recovery of plutonium. Further, the theor. calculations done on BenzoDODA SDVB resin suggested Pu(NO3)4·BenzoDODA (1:1) sorbed complex conformed to generally observed square antiprism geometry of the plutonium complexes, with contributions from oxygen atoms of four nitrate ions as well as from four oxygen atoms present in BenzoDODA (two phenolic ether oxygen atoms and two carbonyl oxygen atoms of amidic moiety).

Journal of Hazardous Materials published new progress about Sorptive wastewater treatment. 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Recommanded Product: 2-Chloro-N,N-diisobutylacetamide.

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

Yuan, Shuo; Wang, Bo; Dai, Qing-Qing; Zhang, Xiao-Nan; Zhang, Jing-Ya; Zuo, Jia-Hui; Liu, Hui; Chen, Zhe-Sheng; Li, Guo-Bo; Wang, Shaomeng; Liu, Hong-Min; Yu, Bin published the artcile< Discovery of New 4-Indolyl Quinazoline Derivatives as Highly Potent and Orally Bioavailable P-Glycoprotein Inhibitors>, Related Products of 5004-88-6, the main research area is indolyl quinazoline derivative preparation oral P glycoprotein inhibitor cancer.

The major drawbacks of P-glycoprotein (P-gp) inhibitors at the clin. stage make the development of new P-gp inhibitors challenging and desirable. In this study, we reported our structure-activity relationship studies of 4-indolyl quinazoline, which led to the discovery of a highly effective and orally active P-gp inhibitor, YS-370. YS-370 effectively reversed multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 bound directly to P-gp, did not alter expression or subcellular localization of P-gp in SW620/AD300 cells, but increased the intracellular accumulation of paclitaxel. Furthermore, YS-370 stimulated the P-gp ATPase activity and had moderate inhibition against CYP3A4. Significantly, oral administration of YS-370 in combination with paclitaxel achieved much stronger antitumor activity in a xenograft model bearing SW620/Ad300 cells than either drug alone. Taken together, our data demonstrate that YS-370 is a promising P-gp inhibitor capable of overcoming MDR and represents a unique scaffold for the development of new P-gp inhibitors.

Journal of Medicinal Chemistry published new progress about Antitumor agent resistance. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Related Products of 5004-88-6.

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

Vaskevych, Alla I.; Savinchuk, Nataliia O.; Vaskevych, Ruslan I.; Rusanov, Eduard B.; Grygorenko, Oleksandr O.; Vovk, Mykhailo V. published the artcile< The PIFA-initiated oxidative cyclization of 2-(3-butenyl)quinazolin-4(3H)-ones - an efficient approach to 1-(hydroxymethyl)-2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-ones>, Application In Synthesis of 5004-88-6, the main research area is hydroxymethyl dihydropyrroloquinazolinone preparation regioselective; butenyl quinazolinone oxidative exo trig cyclization PIFA; [bis(trifluoroacetoxy)iodo]benzene PIFA; nitrogen heterocycles; oxidative cyclization; pyrrolo[1,2-a]quinazolines.

A regioselective method for the synthesis of 1-(hydroxymethyl)-2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-ones – close structural analogs of naturally occurring vasicinone alkaloids – is described. The procedure is based on PIFA-initiated oxidative 5-exo-trig cyclization of 2-(3-butenyl)quinazolin-4(3H)-ones, in turn prepared by thermal cyclocondensation of the corresponding 2-(pent-4-enamido)benzamides. The products obtained have a good natural product likeness (NPL) score and therefore can be useful for the design of natural product-like compound libraries.

Beilstein Journal of Organic Chemistry published new progress about Benzamides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Application In Synthesis of 5004-88-6.

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

Cheng, Ching-Feng; Ku, Hui-Chen; Cheng, Jing-Jy; Chao, Shi-Wei; Li, Hsiao-Fen; Lai, Pei-Fang; Chang, Che-Chang; Don, Ming-Jaw; Chen, Hsi-Hsien; Lin, Heng published the artcile< Adipocyte browning and resistance to obesity in mice is induced by expression of ATF3.>, Computed Properties of 96829-58-2, the main research area is Diabetes; Drug discovery; Medical research; Obesity; Transcription.

Billions of people have obesity-related metabolic syndromes such as diabetes and hyperlipidemia. Promoting the browning of white adipose tissue has been suggested as a potential strategy, but a drug still needs to be identified. Here, genetic deletion of activating transcription factor 3 (ATF3-/- ) in mice under a high-fat diet (HFD) resulted in obesity and insulin resistance, which was abrogated by virus-mediated ATF3 restoration. ST32da, a synthetic ATF3 inducer isolated from Salvia miltiorrhiza, promoted ATF3 expression to downregulate adipokine genes and induce adipocyte browning by suppressing the carbohydrate-responsive element-binding protein-stearoyl-CoA desaturase-1 axis. Furthermore, ST32da increased white adipose tissue browning and reduced lipogenesis in HFD-induced obese mice. The anti-obesity efficacy of oral ST32da administration was similar to that of the clinical drug orlistat. Our study identified the ATF3 inducer ST32da as a promising therapeutic drug for treating diet-induced obesity and related metabolic disorders.

Communications biology published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Computed Properties of 96829-58-2.

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