Category: 25999-04-6

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

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

Yamaguchi, Hachiro; Tsujihara, Kenji published the artcile< Sulfonyl diamide derivatives. II. Amide exchange reaction of sulfonyl diamide>, Application In Synthesis of 25999-04-6, the main research area is exchange amine sulfonyl diamide.

In the amide exchange reaction of sulfonyl diamide with amines, the reaction with primary amines under anhydrous conditions gave monosubstituted products at first and then N,N’-disubstituted products. However, the reaction with primary amines under aqueous conditions and with secondary amines in the absence of water gave only mono substituted products. The first intermediates were N-monosubstituted sulfonyl diamides in the case of primary amines, and N,N’-disubstituted sulfonyl diamides in the case of secondary amines. 1,3-Disubstituted imidodisulfonyl diamide was isolated as an intermediate from the reaction under anhydrous conditions, and 1-monosubstituted imidodisulfonyl diamide was isolated as an intermediate from the reaction under aqueous conditions. The former reacted with anhydrous primary amine to give N,N’-disubstituted sulfonyl diamide. The latter reacted with aqueous primary amine to give N-monosubstituted sulfonyl diamide.

Nippon Kagaku Kaishi published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Application In Synthesis of 25999-04-6.

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

Appel, Rolf; Montenarh, Mathias published the artcile< Preparation of silylated amidosulfuric acid derivatives and their reaction with sulfur(IV) halides>, Synthetic Route of 25999-04-6, the main research area is aminosulfamide silylation; sulfamide silylation; sulfur halide sulfamide; diimide sulfur disulfamoyl; sulfinylamine thiobis.

The silylation of aminosulfamides, R2NSO2NH2 with HN(SiMe3)2 gave R2NSO2NHSiMe3 (R = Me, Et; R2N = piperidino, morpholino). Me2NSO2NHSiMe3 was lithiated and silylated with Me3SiCl to give Me3NSO2N(SiMe3)2 (I), also prepared from Me2NSO2NH2 and Me3SiCl. ROSO2NH2 [R = H (II), Me) was silylated with Me3SiCl to give ROSO2NR1SiMe3 (R = Me3Si, R1 = H; R = Me, R1 = Me3Si). II and Me3SiCl also gave Me3SiOSO2N(SiMe3)2 (III), also prepared from (Me3Si)3N and SO3. I and II with SOCl2 gave RSO2NSO [R = Me2N (IV), Me3SiO]. S(NSO)2 was prepared from [(Me3Si)2N]2SO2 and SOCl2, from Me3SiNSO and SO2Cl2, and from Me3SiN:S:NSiMe3 and SOCl2. IV was heated to give Me2NSO2N:S:NSO2NMe2, also prepared from I and SF4. I and SF4 also gave Me2NSO2N:SF2 (V), also prepared from IV and SF4. V and N(SiMe3)3 gave Me2NSO2N:S:NSiMe3.

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

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

Yamaguchi, Hachiro; Nakano, Keiji published the artcile< Hydrolysis of N-substituted derivatives of sulfamide>, Application of C4H10N2O3S, the main research area is sulfamic acid sulfamide hydrolysis; sulfamide alkyl benzyl hydrolysis; alkylsulfamide hydrolysis kinetics; benzylsulfamide hydrolysis kinetics; hydrolysis sulfamide derivative kinetics.

N-Alkyl- or -benzylsulfamides were hydrolyzed to the corresponding N-substituted sulfamates (RNHSO3NH4) in ∼ 44-87% yield with H2O and to H2NSO3Na in ∼ 64-95% yield with aqueous NaOH. N,N-Disubstituted sulfamides containing a heterocyclic ring were hydrolyzed mainly to sulfamates with H2O or NaOH. sym-N,N’-Dialkyl- or -benzylsulfamides were converted into N-substituted sulfamates in 50-97% yield with NaOH and into N,N’-disubstituted sulfamates in 63-93% yield with H2O, but (Et2N)2SO2 was hydrolyzed only with difficulty by H2O or NaOH. The reaction mechanisms were explained through electron density and steric complexity.

Hiroshima Daigaku Kogakubu Kenkyu Hokoku published new progress about Hydrolysis kinetics. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Application of C4H10N2O3S.

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

Alexandre, Francois-Rene; Brandt, Guillaume; Caillet, Catherine; Chaves, Dominique; Convard, Thierry; Derock, Michel; Gloux, Damien; Griffon, Yann; Lallos, Lisa; Leroy, Frederic; Liuzzi, Michel; Loi, Anna-Giulia; Moulat, Laure; Musiu, Chiara; Parsy, Christophe; Rahali, Houcine; Roques, Virginie; Seifer, Maria; Standring, David; Surleraux, Dominique published the artcile< Synthesis and antiviral evaluation of a novel series of homoserine-based inhibitors of the hepatitis C virus NS3/4A serine protease>, Computed Properties of 25999-04-6, the main research area is homoserine based macrocycle preparation HCV NS34A inhibitor SAR; HCV NS3/4A protease inhibitors; Hepatitis C; Macrocycle; Synthesis and biological evaluation.

We disclose here the synthesis of a series of macrocyclic HCV protease inhibitors, where the homoserine linked together the quinoline P2′ motif and the macrocyclic moiety. These compounds exhibit potent inhibitory activity against HCV NS3/4A protease and replicon cell based assay. Their enzymic and antiviral activities are modulated by substitutions on the quinoline P2′ at position 8 by Me and halogens and by small heterocycles at position 2. The in vitro structure activity relationship (SAR) studies and in vivo pharmacokinetic (PK) evaluations of selected compounds are described herein.

Bioorganic & Medicinal Chemistry Letters published new progress about Hepatitis C. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Computed Properties of 25999-04-6.

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

Roberts, Bryan; Liptrot, David; Alcaraz, Lilian published the artcile< Novel Aryl and Heteroaryl Acyl Sulfamide Synthesis via Microwave-Assisted Palladium-Catalyzed Carbonylation>, Recommanded Product: Morpholine-4-sulfonamide, the main research area is aryl heteroaryl halide sulfamide nucleophile palladium carbonylation microwave irradiation; heteroaryl aryl acyl sulfamide preparation; carbonylation catalyst palladium.

A novel, simple synthesis of aryl and heteroaryl acyl sulfamides has been developed via palladium-catalyzed carbonylation of aryl or heteroaryl halides in the presence of sulfamide nucleophiles. A range of reactions illustrating the wide scope of this reaction was carried out under microwave irradiation in a vessel equipped with a gas inlet adapter and proceeded in good to excellent yields.

Organic Letters published new progress about Aryl halides Role: RCT (Reactant), RACT (Reactant or Reagent). 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Recommanded Product: Morpholine-4-sulfonamide.

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

Hung, Alvin W.; Silvestre, H. Leonardo; Wen, Shijun; George, Guillaume P. C.; Boland, Jennifer; Blundell, Tom L.; Ciulli, Alessio; Abell, Chris published the artcile< Optimization of Inhibitors of Mycobacterium tuberculosis Pantothenate Synthetase Based on Group Efficiency Analysis>, Recommanded Product: Morpholine-4-sulfonamide, the main research area is Mycobacterium pantothenate synthetase inhibitor preparation design structure activity tuberculostatic; indole derivative preparation Mycobacterium pantothenate synthetase inhibitor structure activity; Mycobacterium tuberculosis; drug design; fragment-based screening; group efficiency; pantothenate synthetase.

Ligand efficiency has proven to be a valuable concept for optimization of leads in the early stages of drug design. Taking this one step further, group efficiency (GE) evaluates the binding efficiency of each appendage of a mol., further fine-tuning the drug design process. Here, GE anal. is used to systematically improve the potency of inhibitors of Mycobacterium tuberculosis pantothenate synthetase, an important target in tuberculosis therapy. Binding efficiencies were found to be distributed unevenly within a lead mol. derived using a fragment-based approach. Substitution of the less efficient parts of the mol. allowed systematic development of more potent compounds This method of dissecting and analyzing different groups within a mol. offers a rational and general way of carrying out lead optimization, with potential broad application within drug discovery.

ChemMedChem published new progress about Binding energy. 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Recommanded Product: Morpholine-4-sulfonamide.

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

Maybhate, Shailaja P.; Rajamohanan, Pattuparambil P.; Rajappa, Srinivasachari published the artcile< Regiospecific synthesis of N-sulfonyl derivatives of 3,5-diamino-1H-1,2,4-triazole and 2,5-diamino-1,3,4-thiadiazole>, Product Details of C4H10N2O3S, the main research area is aminoguanidine cyclocondensation alkylsulfonylcarbodithioimidate; hydrazinecarbothioamide cyclocondensation alkylsulfonylcarbodithioimidate; sulfonylaminotriazole; sulfonylaminothiadiazole; triazole sulfonylamino; thiadiazole sulfonylamino.

Condensation of (MeS)2C:NSO2R (R = 4-R1C6H4, 2-thienyl, piperidino, morpholino R1 = H, Me, MeO, Cl, AcNH) with aminoguanidine bicarbonate and hydrazinecarbothioamide leads to the regiospecific synthesis of N-sulfonyl derivatives of 3,5-diamino-1H-1,2,4-triazole I and 2,5-diamino-1,3,4-thiadiazole II, resp.

Synthesis published new progress about Cyclocondensation reaction. 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

Winters, Michael P.; Crysler, Carl; Subasinghe, Nalin; Ryan, Declan; Leong, Lynette; Zhao, Shuyuan; Donatelli, Robert; Yurkow, Edward; Mazzulla, Marie; Boczon, Lisa; Manthey, Carl L.; Molloy, Christopher; Raymond, Holly; Murray, Lynne; McAlonan, Laura; Tomczuk, Bruce published the artcile< Carboxylic acid bioisosteres acylsulfonamides, acylsulfamides, and sulfonylureas as novel antagonists of the CXCR2 receptor>, Application of C4H10N2O3S, the main research area is arylindolebutanamide alkylsulfonyl arylsulfonyl aminosulfonyl preparation CXCR2 antagonist.

A series of novel acylsulfonamide, acylsulfamide, and sulfonylurea bioisosteres of carboxylic acids were prepared as CXCR2 antagonists. Structure-activity relationships are reported for these series. The potent orally bioavailable inhibitor I had excellent PK properties and was active in a lung injury model in hyperoxia-exposed newborn rats.

Bioorganic & Medicinal Chemistry Letters published new progress about CXC chemokine receptor CXCR2 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 25999-04-6 belongs to class amides-buliding-blocks, and the molecular formula is C4H10N2O3S, Application of C4H10N2O3S.

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