Month: October 2022

Dutta, Deep; Jaisani, Ritu; Khandelwal, Deepak; Ghosh, Soumitra; Malhotra, Rajiv; Kalra, Sanjay published the artcile< Role of metformin, sodium-glucose cotransporter-2 (SGLT2) Inhibitors, glucagon-like peptide-1 (GLP-1) receptor agonists, and orlistat based multidrug therapy in glycemic control, weight loss, and euglycemia in diabesity: a real-world experience>, Name: (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is diabetes metformin SGLT2 GLP1 weight loss multi drug therapy; Diabesity; GLP1 receptor agonists; SGLT2 inhibitors; diabetes reversal; metformin; orlistat; weight loss.

Results: In total, 5,336 patient records were screened; 2,442 with prediabetes/diabetes were considered; 1,509 patients who fulfilled all criteria were analyzed. Use of metformin, SGLT2i, sulfonylureas, DPP4i, pioglitazone, orlistat, and GLP1a was 85.35%, 74.95%, 68.32%, 60%, 39.16%, 9.08%, and 4.17%, resp. However, 365, 970, and 104 patients were on one of 4 concerned medications (Group-1; 24.18%), dual MDT (Group-2; 64.28%), and triple/quadruple MDT (Group-3; 6.89%). Metformin with SGLT2i was most commonly used dual MDT (94.12%). Anal. according to weight-loss quartiles from 558 patients showed 6.9 kg weight-loss in the highest quartile. People losing maximum weight were significantly younger; had higher use of metformin, SGLT2i, GLP1, orlistat, and lower pioglitazone use; greatest HbA1c reduction (-1.3 vs. -0.3; quartile-1 vs. quartile -4; P < 0.001); and significantly higher occurrence of HbA1c<5.7% (16.8% vs. 6.29%; quartile-1 vs. 4; P < 0.001). Patients in Group-3 had the highest baseline BMI and maximum weight loss with highest number of patients with HbA1c<5.7% (19.44% vs. 10.34%; Group-3 vs. Group-1; P < 0.001). Conclusion: Greater weight loss with HbA1c reduction along with a greater number of patients attaining HbA1c <5.7% highlights that MDT is the way forward to tackle diabesity in India. Indian Journal of Endocrinology and Metabolism published new progress about Body mass index. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Name: (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

Li, Ze-Lin; Wu, Peng-Yu; Cai, Chun published the artcile< Nickel-catalyzed regioselective C-H halogenation of electron-deficient arenes>, Name: o-Chlorobenzenesulfonamide, the main research area is amide halosuccinimide regioselective halogenation nickel catalyst.

A straightforward Ni(II)-catalyzed general strategy was developed for the ortho-halogenation of electron-deficient arenes such as benzamide, benzenesulfonamide, Me benzoate, etc. with easily available halogenating reagents N-halosuccinimides (NXS; X = Br, Cl and I). The transformation was highly regioselective and a wide substrate scope and functional group tolerance were observed This discovery could be of great significance for the selective halogenation of amides, benzoic esters and other substances with guiding groups. Mechanistic investigations were also described.

New Journal of Chemistry published new progress about Aromatic esters 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, Name: o-Chlorobenzenesulfonamide.

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

Hopkins, Megan D.; Ozmer, Garett L.; Witt, Ryan C.; Brandeburg, Zachary C.; Rogers, David A.; Keating, Claire E.; Petcoff, Presley L.; Sheaff, Robert J.; Lamar, Angus A. published the artcile< PhI(OAc)2 and iodine-mediated synthesis of N-alkyl sulfonamides derived from polycyclic aromatic hydrocarbon scaffolds and determination of their antibacterial and cytotoxic activities>, Computed Properties of 1524-40-9, the main research area is alkyl sulfonamide preparation antibacterial antitumor physicochem human.

The development of new approaches toward chemo- and regioselective functionalization of polycyclic aromatic hydrocarbon (PAH) scaffolds will provide opportunities for the synthesis of novel biol. active small mols. that exploit the high degree of lipophilicity imparted by the PAH unit. Herein, new synthetic method for C-X bond substitution that is speculated to operate via a N-centered radical (NCR) mechanism according to exptl. observations was reported. A series of PAH sulfonamides have been synthesized and their biol. activity has been evaluated against Gram-neg. and Gram-pos. bacterial strains (using a BacTiter-Glo assay) along with a series of mammalian cell lines (using CellTiter-Blue and CellTiter-Glo assays). The viability assays have resulted in the discovery of a number of bactericidal compounds that exhibit potency similar to other well-known antibacterials such as kanamycin and tetracycline, along with the discovery of a luciferase inhibitor. Addnl., the physicochem. and drug-likeness properties of the compounds were determined exptl. and using in silico approaches and the results are presented and discussed within.

Organic & Biomolecular Chemistry published new progress about Antibacterial agents. 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Computed Properties of 1524-40-9.

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

de Almeida, Luciana Y.; Mariano, Flavia S.; Bastos, Debora C.; Cavassani, Karen A.; Raphelson, Janna; Mariano, Vania S.; Agostini, Michelle; Moreira, Fernanda S.; Coletta, Ricardo D.; Mattos-Graner, Renata O.; Graner, Edgard published the artcile< The antimetastatic activity of orlistat is accompanied by an antitumoral immune response in mouse melanoma>, 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 antimetastatic activity antitumoral immune response melanoma; Experimental melanoma; Fatty acid synthase; Immune response; Metastasis; Orlistat.

Our group has previously shown that pharmacol. inhibition of FASN with orlistat decreases proliferation, promotes apoptosis, and reduces the metastatic spread of B16-F10 cells in exptl. models of melanoma. While most of the orlistat antitumor properties seem to be closely related to direct effects on malignant cells, its impact on the host immune system is still unknown. The effects of orlistat on the phenotype and activation status of infiltrating leukocytes in primary tumors and metastatic lymph nodes were assessed using a model of spontaneous melanoma metastasis (B16-F10 cells/C57BL/6 mice). Cells from the primary tumors and lymph nodes were mech. dissociated and immune cells phenotyped by flow cytometry. The expression of IL-12p35, IL-12p40, and inducible nitric oxide synthase (iNOS) was analyzed by qRT-PCR and production of nitrite (NO2-) evaluated in serum samples with the Griess method. Orlistat-treated mice exhibited a 25% reduction in the number of mediastinal lymph node metastases (mean 3.96 ± 0.78, 95% CI 3.63-4.28) compared to the controls (mean 5.7 ± 1.72; 95% CI 5.01-6.43). Taken together, these findings suggest that orlistat supports an antitumor response against exptl. melanomas by increasing CD80/CD81-pos. and IL-12-pos. DC populations, granzyme b/NKG2D-pos. NK populations, and perforin/granzyme b-pos. CD8 T lymphocytes as well as reducing Tregs counts within exptl. melanomas.

Cancer Chemotherapy and Pharmacology published new progress about Antitumor agents. 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

Moukha-chafiq, Omar; Reynolds, Robert C. published the artcile< Parallel Solution-Phase Synthesis and General Biological Activity of a Uridine Antibiotic Analog Library>, Electric Literature of 1524-40-9, the main research area is uridine antibiotic analog preparation agonist antagonist activator enzyme receptor; nucleoside peptide preparation biol activity screening.

A small library of ninety four uridine antibiotic analogs was synthesized, under the Pilot Scale Library (PSL) Program of the NIH Roadmap initiative, from amine 2 and carboxylic acids 33 and 77 in solution-phase fashion. Diverse aldehyde, sulfonyl chloride, and carboxylic acid reactant sets were condensed to 2, leading after acid-mediated hydrolysis, to the targeted compounds 3-32 in good yields and high purity. Similarly, treatment of 33 with diverse amines and sulfonamides gave 34-75. The coupling of the amino terminus of D-phenylalanine Me ester to the free 5′-carboxylic acid moiety of 33 followed by sodium hydroxide treatment led to carboxylic acid analog 77. Hydrolysis of this material gave analog 78. The intermediate 77 served as the precursor for the preparation of novel dipeptidyl uridine analogs 79-99 through peptide coupling reactions to diverse amine reactants. None of the described compounds show significant anticancer or antimalarial activity. A number of samples exhibited a variety of promising inhibitory, agonist, antagonist, or activator properties with enzymes and receptors in primary screens supplied and reported through the NIH MLPCN program.

ACS Combinatorial Science published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 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

Shirai, Kohji; Tanaka, Michitaka; Fujita, Toru; Fujii, Yuka; Shimomasuda, Masatsugu; Sakai, Soichi; Samukawa, Yoshishige published the artcile< Safety of Excessive Visceral Fat Reduction with 52-Week Administration of Lipase Inhibitor Orlistat in Japanese Individuals: A Long Term Clinical Study>, 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 inhibitor visceral fat antiobesity agent; Body weight; Efficacy; Japanese; Lipase inhibitor; Long-term administration; Obesity; Orlistat; Safety; Visceral fat; Waist circumference.

Introduction: Orlistat is an inhibitor of pancreatic lipase and is used as an anti-obesity drug in many countries. However, there are no data available regarding the effects of orlistat on visceral fat (VF) accumulation in Japanese individuals. Therefore, this study aimed to analyze the efficacy and safety of 52 wk of orlistat administration in Japanese individuals. Methods: Orlistat 60 mg was administered orally three times daily for 52 wk to Japanese participants with excessive VF accumulation and without dyslipidemia, diabetes mellitus, and hypertension (metabolic diseases). Participants were also counseled to improve their diet and to maintain exercise habits. We defined excessive VF accumulation as a waist circumference (WC) of ≥ 85 cm for males and ≥ 90 cm for females, which corresponds to a VF area of 100 cm2. Adverse reactions, clin. laboratory tests, VF, WC, body weight (BW), etc., were monitored throughout the study period. Results: VF, WC, and BW were significantly reduced at week 52 from baseline; the mean ± standard error rate of change was – 21.52% ± 1.89%, – 4.89% ± 0.45%, and – 5.36% ± 0.56%, resp., and continued to reduce throughout the 52 wk; these significantly reduced at whole term compared with baseline. Most adverse reactions were defecation-related symptoms such as oily spotting and flatus with discharge (flatus with small amounts of stool or oil) due to the pharmacol. effects of the lipase inhibitor. These symptoms were mostly mild, reversible, and recognizable by the participants; none were serious or severe. No participants discontinued by medical judgment about adverse reactions, and the drug could be administered continuously. Conclusion: VF, WC, and BW were reduced from week 4 to week 52, indicating the effect of long-term orlistat administration. Moreover, it was well tolerated with an acceptable safety profile. Long-term administration of orlistat may be efficacious in reducing VF accumulation with safety when used in combination with diet and exercise. Trial Registration: This study is registered with the Japan Pharmaceutical Information Center (identifier: JapicCTI-184004). Funding: Funding for this study was provided by Taisho Pharmaceutical Co., Ltd.

Advances in Therapy published new progress about Antiobesity agents. 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

Zhuang, Xiaohui; Ling, Lan; Wang, Yingying; Li, Bingqian; Sun, Bin; Su, Weike; Jin, Can published the artcile< Photoinduced Cascade C-N/C=O Bond Formation from Bromodifluoroalkyl Reagents, Amines, and H2O via a Triple-Cleavage Process>, SDS of cas: 6280-57-5, the main research area is unsym oxalamide derivative green preparation; bromodifluoroalkyl reagent amine water cascade bond formation photocatalyst.

A green, sustainable, and straightforward method for synthesis of unsym. oxalamides RC(O)NR1R2 [R = C(O)NHPh, C(O)NH-4-BrC6H4, C(O)Ph, etc.; R1 = Me, Et, nPr, etc.; R2 = Me, Et, nPr, etc.; R1R2 = pyrrolidin-1-yl, morpholin-4-yl, cyclohex-1-yl] via photoinduced C-N/C=O bonds formation of bromodifluoroacetamide, amine and H2O through proceeding triple cleavage process was developed. In addition, this approach also gave an access to build the known bioactive compounds, and a feasible reaction mechanism was proposed. Moreover, the advantages of this transformation, including mild reaction conditions, broad substrate scope and operational simplicity, made this protocol attractive for further applications.

Organic Letters published new progress about Acetamides Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (bromodifluoro-). 6280-57-5 belongs to class amides-buliding-blocks, and the molecular formula is C17H35NO, SDS of cas: 6280-57-5.

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

Kerdphon, Sutthichat; Jongcharoenkamol, Jira; Chatwichien, Jaruwan; Singh, Thishana; Channei, Duangdao; Choommongkol, Vachira; Rithchumpon, Puracheth; Meepowpan, Puttinan published the artcile< Microwave-Assisted Green Synthesis of 2,3-Dihydroquinazolinones under Base- and Catalyst-Free conditions>, COA of Formula: C7H7BrN2O, the main research area is dihydroquinazolinone acetonitrile cinnamaldehyde aldehyde butyraldehyde irradiation hydrolysis.

A facile and green one-pot synthesis of 2,3-dihydroquinazolinones, using microwave irradiation, has been developed. Dihydroquinazolinones were synthesized from 2-aminobenzamide derivatives and various aldehydes in aqueous solution under base and catalyst free reaction conditions. The desired products, from aliphatic and aromatic aldehydes substrates, were obtained in 5 min with up to 99 % isolated yields.

ChemistrySelect published new progress about Aldehydes Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 112253-70-0 belongs to class amides-buliding-blocks, and the molecular formula is C7H7BrN2O, COA of Formula: C7H7BrN2O.

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

Nakamura, Akio; Yamada, Tetsuhiro; Asaki, Tetsuo published the artcile< Synthesis and evaluation of N-acylsulfonamide and N-acylsulfonylurea prodrugs of a prostacyclin receptor agonist>, Electric Literature of 25999-04-6, the main research area is diphenyl pyrazine sulfonamide prodrug preparation hydrolysis.

N-Acylsulfonamide and N-acylsulfonylurea derivatives of the carboxylic acid prostacyclin receptor agonist 1 (I) were synthesized and their potential as prodrug forms of the carboxylic acid was evaluated in vitro and in vivo. These compounds were converted to the active compound 1 by hepatic microsomes from rats, dogs, monkeys, and humans, and some of the compounds were shown to yield sustained plasma concentrations of 1 when they were orally administered to monkeys. These types of analogs, including NS-304 (2a), are potentially useful prodrugs of 1.

Bioorganic & Medicinal Chemistry published new progress about Homo sapiens. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Electric Literature of 25999-04-6.

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

Yadav, Mange Ram; Chauhan, Bishram Singh; Naik, Prashant; Gandhi, Hardik; Giridhar, Rajani published the artcile< 6,7-Dimethoxyquinazolines as Potential Cytotoxic Agents: Synthesis and in vitro Activity>, Electric Literature of 5004-88-6, the main research area is quinazolinone dimethoxy preparation anticancer cytotoxicity; quinazoline dimethoxy diamino preparation antitumor.

Series of substituted 6,7-dimethoxyquinazolinones I (R1 = H, n-Bu; n = 0, 1; R2 = 4-ClC6H4, 4-MeOC6H4, etc.) and diaminoquinazolines II (R3 = 2-MeC6H4, 3-HO2CC6H4, 4-H2NSO2C6H4, etc.) were synthesized. The compounds I (R1 = n-Bu) were synthesized with the aim of increasing the lipophilicity. The cytotoxicity of the selected products was evaluated against National Cancer Institute (NCI) 60 cell panel using the NCI disease oriented antitumor screen protocol. Based on the results of this screening, it was generalized that compounds having aryl groups directly attached to the quinazoline ring are less active than those which have one atom linker between the two ring systems. Substitution with a lipophilic group like n-Bu decreased cytotoxic activity among the compounds, whereas 4-aminoquinazolines showed better activity than 4-quinazolinones. Lipophilic groups in the aromatic ring increased the cytotoxicity. The selected compounds I (R1 = H; n = 1; R2 = 4-MeOC6H4) and II (R3 = 3-ClC6H4) were found to be potential lead compounds, which could be further optimized as potential anti-neoplastic agents.

Letters in Drug Design & Discovery published new progress about Antitumor agents. 5004-88-6 belongs to class amides-buliding-blocks, and the molecular formula is C9H12N2O3, Electric Literature of 5004-88-6.

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