Tag: M.W=150-200

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

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

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

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

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

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

Li, Sifan; Wang, Yu; Wu, Zibo; Shi, Weiliang; Lei, Yibo; Davies, Paul W.; Shu, Wei published the artcile< A Radical-Initiated Fragmentary Rearrangement Cascade of Ene-Ynamides to [1,2]-Annulated Indoles via Site-Selective Cyclization>, Synthetic Route of 1524-40-9, the main research area is annulated indole regioselective preparation; ene ynamide fragmentary rearrangement cascade radical initiated.

Herein, a radical triggered fragmentary cyclization cascade reaction of ene-ynamides was presented, providing a rapid access into [1,2]-annulated indoles I [R = H, Me, SMe, etc.; R1 = Ph, 4-MeC6H4, 3-pyridyl, etc.; R2 = H, Me, n-Bu; n = 1,2,3] by an intermol. radical addition, intramol. cyclization, desulfonylative aryl migration, and site-selective C(sp2)-N cyclization sequence. DFT calculations support oxidation of N-centered radical species to cations prior to the C-N bond formation, followed by an unusual aza-Nazarov cyclization.

Organic Letters published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 1524-40-9 belongs to class amides-buliding-blocks, and the molecular formula is C6H6FNO2S, Synthetic Route of 1524-40-9.

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

Grib, Ismahene; Berredjem, Malika; Rachedi, Khadidja Otmane; Djouad, Seif-Eddine; Bouacida, Sofiane; Bahadi, Rania; Ouk, Tan-Sothea; Kadri, Mekki; Ben Hadda, Taibi; Belhani, Billel published the artcile< Novel N-sulfonylphthalimides: Efficient synthesis, X-ray characterization, spectral investigations, POM analyses, DFT computations and antibacterial activity>, Safety of Morpholine-4-sulfonamide, the main research area is sulfonylphthalimide preparation antibacterial DFT; phthalic anhydride sulfonamide condensation ultrasonication.

Some novel N-sulfonylphthalimides I [R = NPh2, N-piperidinyl, morpholino, etc.] were synthesized in good yields by condensation of anhydride phthalic with various sulfonamides in one step. These compounds were screened for their antibacterial activity against E. coli, S. aureus, Morganella morganii and Klebsiella pneumoniae. So it will benificial to test these mols. against other biotargets different of bacterial strains such as viruses, fungus and parasites. The mol. structure of I [R = 3,4-dihydro-1H-isoquinolin-2-yl] was obtained by X-ray diffraction on mono crystal. The crystal packing could be described as alternating layers in zigzag parallel to (100) plane along the c axis, which were connected together with C-H···O hydrogen bonds.

Journal of Molecular Structure published new progress about Amines Role: PAC (Pharmacological Activity), PRP (Properties), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses) (sulfonyl-). 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Safety of Morpholine-4-sulfonamide.

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

Qiao, Jin-Bao; Zhang, Ya-Qian; Yao, Qi-Wei; Zhao, Zhen-Zhen; Peng, Xuejing; Shu, Xing-Zhong published the artcile< Enantioselective Reductive Divinylation of Unactivated Alkenes by Nickel-Catalyzed Cyclization-Coupling Reaction>, Computed Properties of 1524-40-9, the main research area is methylene five membered heterocycle carbocycle chemoselective regioselective enantioselective preparation; bromo diene vinyl electrophile divinylation cyclization coupling nickel catalyst.

An enantioselective cross-electrophile divinylation reaction of nonaromatic substrates, 2-bromo-1,6-dienes was reported. The approach thus offered a route to new chiral cyclic architectures, which were key structural motifs found in various biol. active compounds The reaction proceeded under mild conditions, and use of chiral t-Bu-pmrox and 3,5-difluoro-pyrox ligands resulted in formation of divinylated products with high chemo-, regio-, and enantioselectivity. The method was applicable for incorporation of chiral hetero- and carbocycles into complex mols.

Journal of the American Chemical Society published new progress about Alkadienes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 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