Month: October 2022

D’Angelo, Noel D.; Kim, Tae-Seong; Andrews, Kristin; Booker, Shon K.; Caenepeel, Sean; Chen, Kui; Freeman, Dan; Jiang, Jian; McCarter, John D.; San Miguel, Tisha; Mullady, Erin L.; Schrag, Michael; Subramanian, Raju; Tang, Jin; Wahl, Robert C.; Wang, Ling; Whittington, Douglas A.; Wu, Tian; Xi, Ning; Xu, Yang; Yakowec, Peter; Zalameda, Leeanne P.; Zhang, Nancy; Hughes, Paul; Norman, Mark H. published the artcile< Discovery and Optimization of a Series of Benzothiazole Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitors>, Electric Literature of 1524-40-9, the main research area is benzothiazole derivative preparation SAR mTOR PI3K inhibitor antitumor bioavailability.

Phosphoinositide 3-kinase α (PI3Kα) is a lipid kinase that plays a key regulatory role in several cellular processes. The mutation or amplification of this kinase in humans has been implicated in the growth of multiple tumor types. Consequently, PI3Kα has become a target of intense research for drug discovery. Our studies began with the identification of benzothiazole compound 1 from a high throughput screen. Extensive SAR studies led to the discovery of sulfonamide 45 as an early lead, based on its in vitro cellular potency. Subsequent modifications of the central pyrimidine ring dramatically improved enzyme and cellular potency and led to the identification of chloropyridine 70. Further arylsulfonamide SAR studies optimized in vitro clearance and led to the identification of 82 as a potent dual inhibitor of PI3K and mTOR. This mol. exhibited potent enzyme and cell activity, low clearance, and high oral bioavailability. In addition, compound 82 demonstrated tumor growth inhibition in U-87 MG, A549, and HCT116 tumor xenograft models.

Journal of Medicinal Chemistry published new progress about Antitumor agents. 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Electric Literature of 1524-40-9.

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

Zhao, Xue-Mei; Huang, En-Ling; Zhu, Yu-Shen; Li, Jing; Song, Bing; Zhu, Xinju; Hao, Xin-Qi published the artcile< Oxidative sulfonamidomethylation of imidazopyridines utilizing methanol as the main C1 source>, Application In Synthesis of 6961-82-6, the main research area is phenyl imidazopyridine methanol sulfamide oxidative sulfonamidomethylation; imidazopyridine methanol amine oxidative aminomethylation.

An efficient one-pot, three-component synthesis of C3 sulfonamidomethylated imidazopyridines was disclosed under metal-free conditions, which utilized the com. available and renewable reagent methanol as the main methylene source. A wide range of substituted imidazopyridines and sulfamides/amines were well tolerated to afford the corresponding products in up to 92% yield. In the isotopic labeling experiment, it was found that a minor part of the methylene also originated from DTBP. Moreover, the radical scavenger reactions were conducted, which suggested that a free-radical mechanism was probably not involved. The current methodol. featured several advantages, including broad substrate scope, good functional group tolerance and high reaction efficiency.

Organic & Biomolecular Chemistry published new progress about Amines Role: 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, Application In Synthesis of 6961-82-6.

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

Singh, Imocha Rajkumar; Mitra, Sivaprasad published the artcile< Interaction of chlorpropamide with serum albumin: Effect on advanced glycated end (AGE) product fluorescence>, HPLC of Formula: 94-20-2, the main research area is chlorpropamide blood albumin interaction advanced glycated end product fluorescence; AGE product; Chlorpropamide; Diabetes; Fluorescence quenching; Serum albumin.

Carrier proteins like bovine or human serum albumin (BSA and HSA, resp.) are prone to glycation as compared to the other available proteins. Reducing sugars such as L-arabinose (ara), D-(-) galactose (gal) and D-(-) fructose (fru) were used to create model glycated serum albumins and binding ability of these with known antidiabetic drug chlorpropamide (CPM) was monitored. Fluorescence quenching experiment revealed that interaction of CPM with native as well as glycated albumins undergoes through a ground state complex formation. CPM binds strongly to glycated HSA with arabinose (gHSAara) as compared to other glycated systems and to the native proteins. CPM interacts through Van der Waals and hydrogen bonding interaction to glycated BSA by D-(-) fructose (gBSAfru) and also with native HSA; whereas, it’s interaction with BSA and others glycated systems like gBSAara, gBSAgal and gHSAara occurs primarily through hydrophobic interaction. CPM showed an enhancement in the production of the advanced glycated end products (AGE) in all the glycated proteins. The difference in the binding capability of CPM to differently glycated albumins could be a major model to understand the drug carrying capacity of the glycated serum albumins.

Spectrochimica Acta, Part A: Molecular and Biomolecular Spectroscopy published new progress about Advanced glycosylation end products Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, HPLC of Formula: 94-20-2.

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

Zhang, Yan; Zhou, Zhenghong; Li, Zhibin; Hu, Kangfei; Zha, Zhenggen; Wang, Zhiyong published the artcile< Iodine-mediated electrochemical C(sp3)-H cyclization: the synthesis of quinazolinone-fused N-heterocycles>, Related Products of 5004-88-6, the main research area is quinazolinone fused heterocycle preparation; methyl heteroaromatic aminobenzamide electrochem cyclization iodine.

An efficient iodine-mediated electrochem. C(sp3)-H cyclization was developed under mild conditions. A variety of functionalized quinazolinone-fused N-heterocycles can be obtained with good to excellent yields by virtue of this method. The reaction features a broad substrate scope and scalability, and is metal-free and chem. oxidant-free.

Chemical Communications (Cambridge, United Kingdom) published new progress about Benzamides Role: RCT (Reactant), RACT (Reactant or Reagent) (amino). 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

Tak, Young Jin; Lee, Sang Yeoup published the artcile< Long-Term Efficacy and Safety of Anti-Obesity Treatment: Where Do We Stand?>, 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 Anti-obesity drugs; Liraglutide; Naltrexone/bupropion; Orlistat; Phentermine/topiramate; Weight loss medications.

PURPOSE OF REVIEW: As a chronic and relapsing disease, obesity impairs metabolism and causes cardiovascular diseases. Although behavioral modification is important for the treatment of obesity, it is difficult to achieve an ideal weight or sustain the process of long-term weight loss. Therefore, the obesity control guidelines strongly recommend lifestyle interventions along with medical treatment for patients who are overweight. There is sufficient evidence supporting that pharmacotherapy in combination with behavior-based interventions can result in significant weight loss and improved cardiometabolism. RECENT FINDINGS: Recent meta-analyses of new anti-obesity drugs and their weight-loss efficacy have shown that the overall placebo-subtracted weight reduction (%) for at least 12 months ranged from 2.9 to 6.8% for the following drugs: phentermine/topiramate (6.8%), liraglutide (5.4%), naltrexone/bupropion (4.0%), orlistat (2.9%), and lorcaserin (3.1%). However, very recently, on February 13, 2020, the US Food and Drug Administration (FDA) ordered the withdrawal of lorcaserin from markets, as a clinical trial to assess drug safety showed an increased risk of cancer. Currently, the anti-obesity medications that have been approved by the FDA for chronic weight management are orlistat, phentermine/topiramate, naltrexone/bupropion, and liraglutide. However, they are costly and may have adverse effects in some individuals. Therefore, drug therapy should be initiated in obese individuals after weighing its benefits and risks. One of the strategies for long-term obesity control is that anti-obesity medications should be tailored for specific patients depending on their chronic conditions, comorbidities, and preferences.

Current obesity reports 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

Ahmed, Mohamed; Baqtiyar, Sheema; Khanum, Ruqiya; Fatima, Kulsum; Fatima, Anees published the artcile< Drug utilization pattern of anti diabetic drugs in type II diabetic patients in a teaching and general hospital>, SDS of cas: 94-20-2, the main research area is antidiabetic drug utilization pattern diabetes type 2.

BACKGROUND: Diabetes mellitus is defined as abnormal increase in levels of sugar (glucose) in the blood. Diabetes is a chronic (long-lasting) disease that affects how your body turns food into energy. In people with diabetes, blood sugar levels remain high. This may be because insulin is not being produced at all or is not made at sufficient levels, or is not as effective as it should be. The most common forms of diabetes are type 1diabetes (5%), which is an autoimmune disorder, and type 2 diabetes (95%), which is associated with obesity. Gestational diabetes is a form of diabetes that occurs in pregnancy, and other forms of diabetes are very rare and are caused by a single gene mutation. OBJECTIVE: The present study was undertaken to study the drug utilization pattern of anti-diabetic drugs in diabetic patients. METHOD: A six-month prospective observational study was carried out at Shadan teaching and general hospital, Peerancheru (Hyderabad). The data was collected from the case sheets of in patients and OPD cards of outpatients and critically analyzed using predetermined criteria. RESULTS: Out of 250 patients, 110(44%) patients were males and 140(56%) patients were females. It is observed that diabetes mellitus II is more common in patients of age groups (51-60) years. Pharmacotherapy revealed that 210 (81.6%) patients were treated with monotherapy followed by 34 (14%) patients with 2 drug therapy and 6 (4.4%) patients were prescribed with 3 drug therapy. Metformin was the drug of choice in monotherapy while metformin along with glimepiride was the preferred drug combination used in both 2 drug and 3 drug therapies. The overall drug usages in this study revealed that a total number of 301 drugs were prescribed. Out of which, metformin was most prescribed [128 (42.52%)]. CONCLUSION: Periodic evaluation of drug utilization patterns need to be done to provide suitable medications profile in prescription of drugs to increase the therapeutic benefit and reduce the adverse effects. The study of prescribing patterns require regular monitoring and evaluation and if necessary, suggestion of modification in prescribing pattern of medical practitioners to make medical care rational and cost effective. The current anti diabetic drugs includes insulin preparation and oral hypoglycemic agents (OHA), the preference is given mostly to metformin which is first choice of drug but the other drugs such as human insulin is also prescribed for many patients, also some combinations of (OHA) drugs are also preferred.

Indo American Journal of Pharmaceutical Research published new progress about Antidiabetic agents. 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

Mishra, Ashish A.; Bhanage, Bhalchandra M. published the artcile< Ru-Tethered (R,R)-TsDPEN with DMAB as an efficient catalytic system for high enantioselective one-pot synthesis of chiral β-aminol via asymmetric transfer hydrogenation>, Related Products of 1192620-83-9, the main research area is alpha substituted beta aminol enantioselective preparation; aniline alpha bromo ketone asym transfer hydrogenation ruthenium catalyst.

This work reflected Ru-tethered-TsDPEN as an active chiral catalyst for one pot selective synthesis of optically active α-substituted alcs. ArCH(OH)CH2NHAr1 [Ar = Ph, 2-FC6H4, 2,3-(MeO)2C6H3, etc.; Ar1 = Ph, 4-MeC6H4, 4-ClC6H4, 4-Cl-2-I-C6H3, etc.; stereo = S] and its derivatives from α-bromo ketones ArCOCH2Br in presence of dimethylamine borane (DMAB) as hydrogen source. Various Ru-chiral catalysts were screened and methodol. proceeded via a (R,R) Ru-tethered TsDPEN catalyst through asym. transfer hydrogenation (ATH) of in-situ formed ketones to corresponding chiral β-aminol product. Thus, Ru-tethered TsDPEN-DMAB catalytic system works efficiently with higher yield and high enantiomeric excess over others for ATH process. Based on a study of ortho, meta and para substituted α-bromo acetophenone derivatives, effective enantioselectivity was observed for ortho substituted β-aminol. The mechanism was optimized depending on product anal. with help of its kinetic AT-IR study. This work also focused on synthesis of various β-amino alc. derivatives where effect of an EWG and EDG on enantio-selectivity was studied.

New Journal of Chemistry published new progress about Amino alcohols 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, Related Products of 1192620-83-9.

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

Saleh, Amira; ElFayoumi, Hassan M.; Youns, Mahmoud; Barakat, Waleed published the artcile< Rutin and orlistat produce antitumor effects via antioxidant and apoptotic actions>, Product Details of C29H53NO5, the main research area is rutin orlistat antitumor antioxidant apoptosis; Ehrlich ascites carcinoma; MCF-7; Mice; Orlistat; PANC-1; Rutin.

Cancer is a broad term used to describe a large number of diseases characterized by uncontrolled cell proliferation that leads to tumor production Cancer is associated with mutations in genes controlling proliferation and apoptosis, oxidative stress, fatty acid synthase (FAS) expression, and other mechanisms. Currently, most antineoplastic drugs have severe adverse effects and new effective and safe drugs are needed. This study aims to investigate the possible anticancer activity of rutin and orlistat which are both safely used clin. in humans against two breast cancer models (in vivo EAC and in vitro MCF7) and the pancreatic cancer cell line (PANC-1). Our results have shown that both rutin and orlistat exerted an in vivo anticancer activity as evidenced by the decrease in tumor volume, CEA level, cholesterol content, FAS, and the exerted antioxidant action (reduced MDA level and increased GSH content) and through histopathol. examination In addition, both were cytotoxic to MCF-7 and Panc-1 cell lines by promoting apoptosis. In conclusion, the anticancer activity of rutin and orlistat makes them promising candidates for cancer treatment alone or in combination with other anticancer drugs specially that they are used clin. with an acceptable safety profile.

Naunyn-Schmiedeberg’s Archives of Pharmacology published new progress about Antioxidants Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Product Details of C29H53NO5.

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

Chu, Junjun; Xing, Changsheng; Du, Yang; Duan, Tianhao; Liu, Siyao; Zhang, Pengfei; Cheng, Chumeng; Henley, Jill; Liu, Xin; Qian, Chen; Yin, Bingnan; Wang, Helen Yicheng; Wang, Rong-Fu published the artcile< Pharmacological inhibition of fatty acid synthesis blocks SARS-CoV-2 replication>, Reference of 96829-58-2, the main research area is pharmacol inhibition fatty acid synthesis replication SARSCoV2 COVID19.

Caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), COVID-19 is a virus-induced inflammatory disease of the airways and lungs that leads to severe multi-organ damage and death. Here we show that cellular lipid synthesis is required for SARS-CoV-2 replication and offers an opportunity for pharmacol. intervention. Screening a short-hairpin RNA sublibrary that targets metabolic genes, we identified genes that either inhibit or promote SARS-CoV-2 viral infection, including two key candidate genes, ACACA and FASN, which operate in the same lipid synthesis pathway. We further screened and identified several potent inhibitors of fatty acid synthase (encoded by FASN), including the US Food and Drug Administration-approved anti-obesity drug orlistat, and found that it inhibits in vitro replication of SARS-CoV-2 variants, including more contagious new variants, such as Delta. In a mouse model of SARS-CoV-2 infection (K18-hACE2 transgenic mice), injections of orlistat resulted in lower SARS-CoV-2 viral levels in the lung, reduced lung pathol. and increased mouse survival. Our findings identify fatty acid synthase inhibitors as drug candidates for the prevention and treatment of COVID-19 by inhibiting SARS-CoV-2 replication. Clin. trials are needed to evaluate the efficacy of repurposing fatty acid synthase inhibitors for severe COVID-19 in humans.

Nature Metabolism published new progress about Animal gene Role: BSU (Biological Study, Unclassified), PRP (Properties), BIOL (Biological Study) (FASN). 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Reference of 96829-58-2.

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

Kaniskan, Nevin; Kokten, Sule; Celik, Ilhami published the artcile< A new protocol for the synthesis of primary, secondary and tertiary anthranilamides utilizing N-(2-aminoarylacyl)benzotriazoles>, Application In Synthesis of 5004-88-6, the main research area is anthranilamide production benzotriazole intermediate.

A convenient route for efficient conversion of unprotected anthranilic acids into the corresponding N-(2-aminoarylacyl)benzotriazoles is described. N-(2-Aminoarylacyl)benzotriazoles have been successfully used to synthesize primary, secondary, and tertiary anthranilamides in high yields (71-96%).

ARKIVOC (Gainesville, FL, United States) published new progress about Aromatic amides Role: SPN (Synthetic Preparation), 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