Month: October 2022

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

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

Roy, Bivas Chandra; Samim, Sk. Abdus; Panja, Dibyajyoti; Kundu, Sabuj published the artcile< Tandem synthesis of quinazolinone scaffolds from 2-aminobenzonitriles using aliphatic alcohol-water system>, COA of Formula: C9H12N2O3, the main research area is aminobenzonitrile aliphatic alc water tandem hydration dehydrogenative coupling; quinazolinone preparation green chem.

Ru(II) complex catalyzed tandem synthesis of quinazolinone derivatives is reported here. In this sustainable protocol, 2-aminobenzonitriles were directly transformed to quinazolinones using alc.-water system. A variety of quinazolinones was successfully synthesized in good to excellent yields by utilizing challenging methanol and aliphatic alcs. The practical applicability of the protocol was extended by preparative scale synthesis of various heterocycles as well as natural products. To understand the mechanism of this protocol, several control experiments and DFT studies were carried out. Based on the DFT calculations, a metal-ligand cooperative mechanism was proposed for this system.

Catalysis Science & Technology published new progress about Aliphatic alcohols Role: NUU (Other Use, Unclassified), PRP (Properties), RCT (Reactant), USES (Uses), 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

Baranauskiene, Lina; Skiudaite, Lina; Michailoviene, Vilma; Petrauskas, Vytautas; Matulis, Daumantas published the artcile< Thiazide and other Cl-benzenesulfonamide-bearing clinical drug affinities for human carbonic anhydrases>, Safety of o-Chlorobenzenesulfonamide, the main research area is human carbonic anhydrase chlorine benzenesulfonamide thiazide drug affinity.

Twelve carbonic anhydrase (CA) isoforms catalyze carbon dioxide hydration to bicarbonate and acid protons and are responsible for many biol. functions in human body. Despite their vital functions, they are also responsible for, or implicated in, numerous ailments and diseases such as glaucoma, high altitude sickness, and cancer. Because CA isoforms are highly homologous, clin. drugs designed to inhibit enzymic activity of a particular isoform, can also bind to others with similar affinity causing toxic side effects. In this study, the affinities of twelve CA isoforms have been determined for nineteen clin. used drugs used to treat hypertension related diseases, i.e. thiazides, indapamide, and metolazone. Their affinities were determined using a fluorescent thermal shift assay. Stopped flow assay and isothermal titration calorimetry were also employed on a subset of compounds and proteins to confirm inhibition of CA enzymic activity and verify the quant. agreement between different assays. The findings of this study showed that pharmaceuticals could bind to human CA isoforms with variable affinities and inhibit their catalytic activity, even though the drug was intended to interact with a different (non-CA) protein target. Relatively minor structural changes of the compounds may cause significant changes in affinity and selectivity for a particular CA isoform.

PLoS One published new progress about Antidiuretics. 6961-82-6 belongs to class amides-buliding-blocks, and the molecular formula is C6H6ClNO2S, Safety of o-Chlorobenzenesulfonamide.

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

Li, Feng; Lu, Lei; Liu, Pengcheng published the artcile< Acceptorless Dehydrogenative Coupling of o-Aminobenzamides with the Activation of Methanol as a C1 Source for the Construction of Quinazolinones>, Electric Literature of 112253-70-0, the main research area is dehydrogenative coupling aminobenzamide methanol iridium catalyst; quinazolinone preparation dehydrogenative coupling aminobenzamide methanol iridium catalyst.

A strategy for the synthesis of quinazolinones I (R = H, 7-Me, 6-MeO, 8-F, etc.) via acceptorless coupling of o-aminobenzamides with methanol has been accomplished in the presence of the metal-ligand bifunctional catalyst [Cp*Ir(2,2′-bpyO)(H2O)]. Notably, this research exhibited the potential of transition-metal-catalyzed activation of methanol as a C1 source for the construction of heterocycles.

Organic Letters published new progress about Benzamides Role: RCT (Reactant), RACT (Reactant or Reagent) (o-aminobenzamides). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, Electric Literature of 112253-70-0.

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

Appel, Rolf; Montenarh, Mathias published the artcile< Reactions of N,N-dialkyl- and N,N-diarylsulfamides with chlorosulfonyl isocyanate>, Product Details of C4H10N2O3S, the main research area is sulfamide reaction chlorosulfonyl isocyanate; urea sulfamoyl.

Reaction of RR1NSO2NH2 with ClSO2NCO gave RR1NSO2NHCONHSO2Cl [R = R1 = Me, Et, or Ph; NRR1 = piperidino or morpholino], which were hydrolyzed to give RR1NSO2NHCONH2.

Chemische Berichte published new progress about 25999-04-6. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Product Details of C4H10N2O3S.

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

Zhang, Yan-Shun; Gui, Hou-Ze; Wei, Yin; Shi, Min published the artcile< Synthesis of Dihydro-2-oxopyrrole (DPO) Building Blocks Catalyzed by Potassium Carbonate>, HPLC of Formula: 1524-40-9, the main research area is dihydro oxopyrrole preparation cascade dimerization cyclization sulfonaminoacrylate; potassium carbonate catalyzed cascade dimerization cyclization sulfonaminoacrylate.

A dimerization and cyclization cascade reaction of 2-sulfonaminoacrylates catalyzed by K2CO3 provides dihydro-2-oxopyrrole (DPO) derivatives This straightforward and atom-economic transformation features a simple exptl. operation with easily available starting materials, a broad substrate scope as well as good functional group tolerance. The desired DPO building blocks are obtained in moderate to good yields.

European Journal of Organic Chemistry published new progress about Atom economy. 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, HPLC of Formula: 1524-40-9.

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

Cohen, Jordana B.; Gadde, Kishore M. published the artcile< Weight Loss Medications in the Treatment of Obesity and Hypertension>, Related Products of 96829-58-2, the main research area is review antiobesity agent weight loss obesity hypertension; Blood pressure; Hypertension; Obesity; Weight loss; Weight loss medication; Weight loss pharmacotherapy.

A review. Purpose of Review: Weight loss is strongly associated with improvement in blood pressure; however, the mechanism of weight loss can impact the magnitude and sustainability of blood pressure reduction Recent Findings: Five drugs-orlistat, lorcaserin, liraglutide, phentermine/topiramate, and naltrexone/bupropion-are currently approved for weight loss therapy in the USA. Naltrexone/bupropion results in an increase in in-office and ambulatory blood pressure compared to placebo. Other therapies are associated with modest lowering of blood pressure, and are generally well-tolerated; nonetheless, evidence is limited regarding their effect on blood pressure, particularly longitudinally, in individuals with hypertension. Summary: Although weight loss medications can be an effective adjunct to lifestyle modifications in individuals with obesity, there is limited evidence regarding their benefit with regard to blood pressure. Future studies evaluating the effectiveness of weight loss medications should include careful assessment of their short- and long-term impact on blood pressure in individuals with hypertension.

Current Hypertension Reports published new progress about Antiobesity agents. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Related Products of 96829-58-2.

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

Vasconcelos, Ingrid; da Silva, Pedro Henrique Reis; Dias, Derick Rodrigues Davila; de Freitas Marques, Maria Betania; da Nova Mussel, Wagner; Pedrosa, Tercio Assuncao; Ribeiro e Silva, Maria Elisa Scarpelli; de Souza Freitas, Roberto Fernando; de Sousa, Ricardo Geraldo; Fernandes, Christian published the artcile< Synthesis and characterization of a molecularly imprinted polymer (MIP) for solid-phase extraction of the antidiabetic gliclazide from human plasma>, Computed Properties of 94-20-2, the main research area is gliclazide molecularly imprinted polymer solid phase extraction; Diabetes mellitus; Molecularly imprinted solid-phase extraction; Sample preparation; Sulfonylureas.

Gliclazide is a sulfonylurea frequently prescribed for the management of type 2 diabetes mellitus in elderly patients and for patients with chronic renal or hepatic diseases. Even though it is considered a safer alternative, the drug can provoke side effects in some patients, especially hypoglycemia, due to the high interindividual variability. Therefore, the quantification of gliclazide in biol. samples is usually recommended in order to assure efficacy and safety of the pharmacotherapy. However, due to the complexity of biol. matrixes, therapeutic monitoring can be very challenging, especially in the sample preparation step. Synthesis conditions were optimized (monomer, crosslinker and porogen) and the polymer was characterized for its morphol., physicochem. and stability properties. The influence of drug concentration, solvent composition and pH on the coefficient of distribution (Kd) and imprinting factor (IF) were studied, as well as repeatability between batches and selectivity. The best reaction yield, extraction capacity, and selectivity was obtained using 2-hydroxyethyl methacrylate (2-HEMA), ethyleneglycol dimethacrylate (EGDMA) and acetonitrile. The developed method by MISPE-HPLC-UV showed to be appropriate to determine gliclazide in human plasma samples.

Materials Science & Engineering, C: Materials for Biological Applications published new progress about Blood plasma. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Computed Properties of 94-20-2.

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

Sagandira, Cloudius R.; Watts, Paul published the artcile< Rapid Multigram-Scale End-to-End Continuous-Flow Synthesis of Sulfonylurea Antidiabetes Drugs: Gliclazide, Chlorpropamide, and Tolbutamide>, Related Products of 94-20-2, the main research area is chlorpropamide gliclazide tolbutamide continuous flow preparation antidiabetic agent.

A multigram-scale robust, efficient, and safe end-to-end continuous-flow process for the diabetes sulfonylurea drugs gliclazide, chlorpropamide, and tolbutamide is reported. The drugs were prepared by the treatment of an amine with a haloformate affording carbamate, which was subsequently treated with a sulfonamide to afford sulfonylurea. Gliclazide was obtained in 87% yield within 2.5 min total residence time with 26 g/h throughput; 0.2 kg of the drug was produced in 8 h of running the system continuously. Chlorpropamide and tolbutamide were both obtained in 94% yield within 1 min residence time with 184-188 g/h throughput; 1.4-1.5 kg of the drugs was produced in 8 h of running the system continuously. N-Substituted carbamates were used as safe alternatives to the hazardous isocyanates in constructing the sulfonyl urea moiety.

Synthesis published new progress about Antidiabetic agents. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Related Products of 94-20-2.

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