Category: amides-buliding-blocks

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

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

El-Shal, Laila Moustafa; El-Star, Alyaa A. Abd; Azmy, Abeer M.; Elnegris, Heba M. published the artcile< The possible protective role of N-acetyl cysteine on duodenal mucosa of high fat diet and orlistat treated adult male albino rats and the active role of tumor necrosis factor α (TNFα) and Interleukin 6 (IL6) (histological and biochemical study)>, Safety of (S)-(S)-1-((2S,3S)-3-Hexyl-4-oxooxetan-2-yl)tridecan-2-yl 2-formamido-4-methylpentanoate, the main research area is HFD; IL6; N-acetyl cysteine; Orlistat; TNFα; duodenal mucosa.

BackgroundObesity is a major universal health issue linked to a majority of illness. AimTo evaluate the histol. and biochem. changes occurred in the duodenal mucosa of high fat diet HFD and orlistat fed rats and to assess the possible protective role of N-acetyl cysteine NAC supplementation. Material and methodSixty male albino rats weighing 180-200 g were classified randomly into control group I and three exptl. groups (HFD group II, HFD + orlistat group III, and HFD + orlistat + NAC group IV). All exptl. groups received HFD alone/and treatment for 6 wk. Group III received orlistat (32 mg/kg/day) before meals and group IV received the same regimen as group III in addition to NAC (230 mg/kg/day) after meals. After completion of the experiment, duodenal sections were processed for histol. examination, oxidative stress parameters, and semiqualitative real time PCR for proinflammatory mediators TNFα and IL6 evaluation. Also, plasma lipid parameters were assessed and morphometric duodenal results were analyzed statistically. ResultsBy histol. examination of HFD and (HFD + orlistat) groups, we found severe to moderate duodenal structural disturbances, increased goblet cells, collagen fibers, and BAX and iNOS immunostaining. By Biochem. examination, both groups showed increased proinflammatory markers level (TNFα and IL6) with decreased all antioxidant parameters and increased MDA. Moreover, NAC treatment in group IV significantly reduced all structural changes, levels of proinflammatory mediators and increased all antioxidant parameter levels and decreased MDA. ConclusionAll findings elucidated that NAC could be accounted to be a useful drug for protection of duodenal mucosa of HFD and orlistat treated animals.

Ultrastructural Pathology published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, Safety of (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

Sivaramakrishna, Mallampalli; Raut, Dhaval R.; Nayak, Shashikant; Nayak, Sandip K.; Mohapatra, Prasanta K. published the artcile< Unusual selective extraction of Pu4+ by some novel diamide ligands in a room temperature ionic liquid>, Product Details of C10H20ClNO, the main research area is plutonium selective extraction diamide ligand ionic liquid uranyl ion.

Extraction of Pu4+ was carried out from nitric acid feeds employing ionic liquid solutions of four novel diamide ligands containing an aromatic bridging group. The ligands with iso-Bu, Bu, n-octyl and 2-ethylhexyl groups were termed as LI, LII, LIII, and LIV, resp. and showed significantly higher extraction of the tetravalent plutonium ion as compared to the hexavalent uranyl ion. Using 0.05 M ligands, the extraction of Pu4+ was in the range of 80-95% when 3 M HNO3 was used as the feed and followed the order: LIII > LII > LI > LIV while the UO22+ ion extraction was less than 4-5% and no particular trend could be established. The extraction of UO22+ could be partly due to the anionic nitrate complex of uranyl ion which was extracted in the absence of the ligands, while the ligand assisted extraction contributing for the remaining. Out of the other metal ions studied, Cs+ showed some extraction which was not ligand assisted while almost no extraction of metal ions such as Sr2+, Am3+ and Eu3+ was noticed. Unusually high selectivity was seen for Pu4+ ion extraction out of all the metal ions studied making the solvent systems very important for a plutonium specific separation method development. The extraction was found to be increasing with the aqueous phase nitric acid concentration conforming to a ‘solvation mechanism’ of extraction where the extracted species conforming to Pu(NO3)4·LIL for all the four diamide extractants.

Separation and Purification Technology published new progress about Extraction. 5326-82-9 belongs to class amides-buliding-blocks, and the molecular formula is C10H20ClNO, Product Details of C10H20ClNO.

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

Karatas, Mehmet; Chaikuad, Apirat; Berger, Bianca; Kubbutat, Michael H. G.; Totzke, Frank; Knapp, Stefan; Kunick, Conrad published the artcile< 7-(2-Anilinopyrimidin-4-yl)-1-benzazepin-2-ones designed by a ""cut and glue"" strategy are dual Aurora A/VEGF-R kinase inhibitors>, Related Products of 25999-04-6, the main research area is anilinopyrimidinyl benzazepinone AuroraA VEGFR kinase inhibitor; Aurora kinase; X-ray structure analysis; anilinopyrimidine; benzazepinone; molecular docking; protein kinase inhibitor; sulfamide.

Although overexpression and hyperactivity of protein kinases are causative for a wide range of human cancers, protein kinase inhibitors currently approved as cancer drugs address only a limited number of these enzymes. To identify new chemotypes addressing alternative protein kinases, the basic structure of a known PLK1/VEGF-R2 inhibitor class was formally dissected and reassembled. The resulting 7-(2-anilinopyrimidin-4-yl)-1-benzazepin-2-ones were synthesized and proved to be dual inhibitors of Aurora A kinase and VEGF receptor kinases. Crystal structures of two representatives of the new chemotype in complex with Aurora A showed the ligand orientation in the ATP binding pocket and provided the basis for rational structural modifications. Congeners with attached sulfamide substituents retained Aurora A inhibitory activity. In vitro screening of two members of the new kinase inhibitor family against the cancer cell line panel of the National Cancer Institute (NCI) showed antiproliferative activity in the single-digit micromolar concentration range in the majority of the cell lines.

Molecules published new progress about Antiproliferative agents. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Related Products of 25999-04-6.

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

Bakhache, William; Neyret, Aymeric; McKellar, Joe; Clop, Camille; Bernard, Eric; Weger-Lucarelli, James; Briant, Laurence published the artcile< Fatty acid synthase and stearoyl-CoA desaturase-1 are conserved druggable cofactors of Old World Alphavirus genome replication>, SDS of cas: 96829-58-2, the main research area is Chikungunya virus; Fatty acid synthase; Genome replication; Lipid metabolism; Mayaro virus; Stearoyl-CoA desaturase-1.

Chikungunya virus (CHIKV) is a rapidly emerging mosquito-borne RNA virus that causes epidemics of debilitating disease in tropical and sub-tropical regions with autochtonous transmission in regions with temperate climate. Currently, there is no licensed vaccine or specific antiviral drug available against CHIKV infection. In this study, we examine the role, in the CHIKV viral cycle, of fatty acid synthase (FASN) and stearoyl-CoA desaturase (SCD1), two key lipogenic enzymes required for fatty acid production and early desaturation We show that both enzymes and their upstream regulator PI3K are required for optimal CHIKV infection. We demonstrate that pharmacol. manipulation of FASN or SCD1 enzymic activity by non-toxic concentrations of cerulenin or CAY10566 decreases CHIKV genome replication. Interestingly, a similar inhibitory effect was also obtained with Orlistat, an FDA-approved anti-obesity drug that targets FASN activity. These drugs were also effective against Mayaro virus (MAYV), an under-studied arthritogenic Old world Alphavirus endemic in South American countries with potential risk of emergence, urbanization and dispersion to other regions. Altogether, our results identify FASN and SCD1 as conserved druggable cofactors of Alphavirus genome replication and support the broad-spectrum activity of drugs targeting the host fatty acids metabolism

Antiviral Research published new progress about 96829-58-2. 96829-58-2 belongs to class amides-buliding-blocks, and the molecular formula is C29H53NO5, SDS of cas: 96829-58-2.

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

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

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

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