Category: 10305-42-7

Kidwai, Mazaahir; Batra, Rajini published the artcile< A new route to thiaziridine 1,1-dioxides>, Reference of 10305-42-7, the main research area is thiaziridine dioxide alkyl; sulfamoyl chloride cyclocondensation diazomethane; alkylthiaziridine dioxide.

Title compounds I (R = CMe3, Me, Pr, CHMe2, CH2CHMe2) were prepared by reacting ClSO2NHR with RCHN2 in ether and NEt3.

Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry published new progress about Cyclocondensation reaction. 10305-42-7 belongs to class ethers-buliding-blocks, and the molecular formula is C3H8ClNO2S, Reference of 10305-42-7.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Matier, W. L.; Comer, W. T.; Deitchman, D. published the artcile< Sulfamoyl azides. Hydrolysis rates and hypotensive activity>, Category: ethers-buliding-blocks, the main research area is sulfamoyl azide hypotensive; blood pressure sulfamoyl azide.

Monosubstituted sulfamoyl azides, e.g. N-(1-adamantyl)sulfamoyl azide (I) [33713-04-1] and N-(p-chlorophenyl)sulfamoyl azide (II) [13479-10-2], were significantly hypotensive in dogs at a min. ED of 0.005-0.01 mg/kg i.v., which was 1-3% of the dose required for disubstituted compounds I and II rapidly lowered blood pressure in dogs after oral administration of 1 mg/kg; the hypotensive response was apparently due to a decrease in both total peripheral resistance and aortic blood flow. The difference in hypotensive activity of mono- and disubstituted compounds appeared to be due to rapid release of azide [14343-69-2] from the former in neutral aqueous media. The mechanism and kinetics of hydrolysis were discussed. Related sulfamide derivatives were inactive. I was synthesized by reacting 1-adamantylamine with SO2Cl2 to form the sulfamoyl chloride, followed by reaction with NaN3 in dry MeCN.

Journal of Medicinal Chemistry published new progress about Antihypertensives. 10305-42-7 belongs to class ethers-buliding-blocks, and the molecular formula is C3H8ClNO2S, Category: ethers-buliding-blocks.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Tait, Annalisa; Luppi, Amedeo; Avallone, Rossella; Baraldi, Mario published the artcile< 2,1,3-Benzothiadiazine derivatives: synthesis and screening versus PDE4 enzyme>, Application In Synthesis of 10305-42-7, the main research area is benzothiadiazine derivative preparation PDE4 inhibitor structure screening; antioxidant structure phosphodiesterase 4 inhibitor benzothiadiazine derivative.

A series of N-1,3 disubstituted 2,1,3-benzothiadiazine derivatives (BTDs) were synthesized and evaluated for their inhibitory activity vs. enzymic isoform PDE4 extracted from U937 cell line. Some of the tested compounds showed a high PDE4 inhibitory activity at 100 μM and the IC50 value of the most interesting terms were evaluated. The structure-activity relationships of these compounds showed that the 3,5-di-tert-butyl-4-hydroxybenzyl moiety at N-1 position is important to obtain activity at micromolar level as previously reported. For the same compounds the antioxidant activity were evaluated highlighting 14 as the most significative one. The introduction of other bulky substituents in N-1 position is detrimental.

Farmaco published new progress about Antioxidants. 10305-42-7 belongs to class ethers-buliding-blocks, and the molecular formula is C3H8ClNO2S, Application In Synthesis of 10305-42-7.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Yong, Cassandra; Devine, Shane M.; Gao, Xuexin; Yan, Angelina; Callaghan, Richard; Capuano, Ben; Scammells, Peter J. published the artcile< A Novel Class of N-Sulfonyl and N-Sulfamoyl Noscapine Derivatives that Promote Mitotic Arrest in Cancer Cells>, Electric Literature of 10305-42-7, the main research area is sulfonyl sulfamoyl noscapine derivative preparation cancer structure; anticancer agents; antimitotic agents; microtubule targeting agents; natural products; noscapine derivatives.

Noscapine displays weak anticancer efficacy and numerous research efforts have attempted to generate more potent noscapine analogs. These modifications included the replacement of the N-Me group in the 6′-position with a range of substituents, where N-ethylcarbamoyl substitution was observed to possess enhanced anticancer activity. Herein, we describe advances in this area, namely the synthesis and pharmacol. evaluation of a series of N-sulfonyl and N-sulfamoyl noscapine derivatives A number of these sulfonyl-containing noscapinoids demonstrated improved activities compared to noscapine. ((R)-5-((S)-4,5-Dimethoxy-1,3-dihydroisobenzofuran-1-yl)-4-methoxy-6-((1-methyl-1H-imidazol-4-yl)sulfonyl)-5,6,7,8-tetrahydro[1,3]dioxolo[4,5-g]isoquinoline) (14 q) displayed sub-micromolar activities of 560, 980, 271 and 443 nM against MCF-7, PANC-1, MDA-MB-435 and SK-MEL-5 cells, resp. This antiproliferative effect was also maintained against drug-resistant NCI/AdrRES cells despite high expression of the multidrug efflux pump, P-glycoprotein.

ChemMedChem published new progress about Antimitotic agents. 10305-42-7 belongs to class ethers-buliding-blocks, and the molecular formula is C3H8ClNO2S, Electric Literature of 10305-42-7.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Jeon, Heechol; Jo, Nam Hyun; Yoo, Kyung Ho; Choi, Joung-Hoon; Cho, Heeyeong; Cho, Jung-Hyuck; Oh, Chang-Hyun published the artcile< Synthesis and antibacterial evaluation of 1β-methyl-2-[5-(1-methoxyimino-2-substituted sulfonamide ethyl)pyrrolidin-3-ylthio]carbapenems and their related compounds>, Computed Properties of 10305-42-7, the main research area is carbapenem sulfonamide pyrrolidinyl preparation antibacterial structure activity relationship.

The synthesis of a new series of 1β-methylcarbapenems, I (R = SO2Me, SO2Et, SO2NHEt, SO2NMe2, SO2NH-n-Pr, COMe, H, CONH2) having methoxyimine and substituted sulfonamide moieties is described. Their in vitro antibacterial activities against both Gram-pos. and Gram-neg. bacteria were tested and the effect of substituents on the pyrrolidine ring was investigated. A particular compound I (R = SO2NHMe) having (methylamino)sulfonamide moiety showed the most potent antibacterial activity.

European Journal of Medicinal Chemistry published new progress about Antibacterial agents. 10305-42-7 belongs to class ethers-buliding-blocks, and the molecular formula is C3H8ClNO2S, Computed Properties of 10305-42-7.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Jeon, Heechol; Jo, Nam Hyun; Yoo, Kyung Ho; Choi, Joung-Hoon; Cho, Heeyeong; Cho, Jung-Hyuck; Oh, Chang-Hyun published the artcile< Synthesis and antibacterial evaluation of 1β-methyl-2-[5-(1-methoxyimino-2-substituted sulfonamide ethyl)pyrrolidin-3-ylthio]carbapenems and their related compounds>, Computed Properties of 10305-42-7, the main research area is carbapenem sulfonamide pyrrolidinyl preparation antibacterial structure activity relationship.

The synthesis of a new series of 1β-methylcarbapenems, I (R = SO2Me, SO2Et, SO2NHEt, SO2NMe2, SO2NH-n-Pr, COMe, H, CONH2) having methoxyimine and substituted sulfonamide moieties is described. Their in vitro antibacterial activities against both Gram-pos. and Gram-neg. bacteria were tested and the effect of substituents on the pyrrolidine ring was investigated. A particular compound I (R = SO2NHMe) having (methylamino)sulfonamide moiety showed the most potent antibacterial activity.

European Journal of Medicinal Chemistry published new progress about Antibacterial agents. 10305-42-7 belongs to class ethers-buliding-blocks, and the molecular formula is C3H8ClNO2S, Computed Properties of 10305-42-7.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Gyulavari, Pal; Szokol, Balint; Szabadkai, Istvan; Brauswetter, Diana; Banhegyi, Peter; Varga, Attila; Marko, Peter; Boros, Sandor; Illyes, Eszter; Szantai-Kis, Csaba; Kreko, Marcell; Czudor, Zsofia; Orfi, Laszlo published the artcile< Discovery and optimization of novel benzothiophene-3-carboxamides as highly potent inhibitors of Aurora kinases A and B>, Safety of n-Propylsulphamoyl chloride, the main research area is benzothiophene carboxamide derivative preparation Aurora kinase inhibitor cancer; Aurora kinase; Benzothiophene-3-carboxamide; Cancer; Kinase inhibitor; Targeted therapy.

Aurora kinases as regulators of cell division have become promising therapeutic targets recently. Here we report novel, low mol. weight benzothiophene-3-carboxamide derivatives designed and optimized for inhibiting Aurora kinases. The most effective compound 36 inhibits Aurora kinases in vitro in the nanomolar range and diminishes HCT 116 cell viability blocking cytokinesis and inducing apoptosis. According to western blot anal., the lead mol. inhibits Aurora kinases equipotently to VX-680 (Tozasertib) and similarly synergizes with other targeted drugs.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents (drug potential as). 10305-42-7 belongs to class ethers-buliding-blocks, and the molecular formula is C3H8ClNO2S, Safety of n-Propylsulphamoyl chloride.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Cano, Carolina; Paez, Juan Antonio; Goya, Pilar; Serrano, Antonia; Pavon, Javier; Rodriguez de Fonseca, Fernando; Suardiaz, Margarita; Martin, Maria Isabel published the artcile< Synthesis and pharmacological evaluation of sulfamide-based analogues of anandamide>, Recommanded Product: n-Propylsulphamoyl chloride, the main research area is anandamide sulfamide derivative preparation CB1 receptor affinity structure activity.

Arachidonyl and linoleyl sulfamide derivatives have been synthesized and their potential cannabimimetic properties evaluated in in vitro functional and binding assays. Replacement of the ethanolamide moiety of anandamide by -CH2NHSO2NH-R (R = saturated or unsaturated long chain alkyl, adamantyl derivative) considerably reduces the CB1 receptor activity and only some of the compounds showed modest cannabinoid properties in binding assays. The new compounds were also tested as inhibitors of the FAAH enzyme but were inactive.

European Journal of Medicinal Chemistry published new progress about Cannabinoid receptor 1 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 10305-42-7 belongs to class ethers-buliding-blocks, and the molecular formula is C3H8ClNO2S, Recommanded Product: n-Propylsulphamoyl chloride.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Hansen, N. C. published the artcile< Monoalkylsulfamyl chlorides>, Electric Literature of 10305-42-7, the main research area is .

Normal C2-5 amine hydrochlorides were treated with excess SO2Cl2 18 hrs. on a water bath at 75°. In some cases more SO2Cl2 was added. The resulting oil was treated with dry ether, the precipitated amine hydrochloride filtered off, and the filtrate distilled in vacuo to give monoalkylsulfamyl chlorides, RNHSO2Cl (I). [RNH2.HCl (R given), amount added, and recovered (g.), volume (ml.) SO2Cl2 used, % yield of corresponding I (based on RNH2.HCl used) and b.p. (redistilled samples) given]: Et, 52, 23, 105 (a further 100 ml. was added after 4 hrs. reflux), 42, b0.05 52; Pr, 52, 26, 350, 13, b0.2 78°; Bu, 77, 27, 450, 39, b0.11 80°; and Am, 19, 12, 150, 8, b0.15 95°. When HCl salts of methyl-, hexyl-, cyclohexyl-, and octylamine were used, the yields of the corresponding I were too low to permit their isolation. That at least MeNHSO2Cl was formed could be concluded from the fact that MeNHSO2NHPr, m. 57-8° (ether-petr. ether), could be obtained when the impure product was treated with PrNH2. EtNHSO2NHBu, m. 73-5° (hexane), was similarly obtained from EtNHSO2Cl.

Acta Chemica Scandinavica published new progress about NMR (nuclear magnetic resonance). 10305-42-7 belongs to class ethers-buliding-blocks, and the molecular formula is C3H8ClNO2S, Electric Literature of 10305-42-7.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Sparey, Tim; Beher, Dirk; Best, Jonathan; Biba, Mirlinda; Castro, Jose L.; Clarke, Earl; Hannam, Joanne; Harrison, Timothy; Lewis, Huw; Madin, Andrew; Shearman, Mark; Sohal, Bindi; Tsou, Nancy; Welch, Christopher; Wrigley, Jonathan published the artcile< Cyclic sulfamide γ-secretase inhibitors>, Product Details of C3H8ClNO2S, the main research area is cyclic sulfamide derivative preparation gamma secretase inhibitor.

A novel series of N-alkyl-substituted cyclic sulfamides were developed from a screening hit. Chemistries were developed which allowed surveys of N-alkyl groups and amines resulting in the identification of N-trifluoroethyl-substituted cyclic sulfamides with good in vitro and in vivo γ-secretase activity. One compound with subnanomolar activity elicited a reduction in brain Aβ40 after oral dosing in APP-YAC mice.

Bioorganic & Medicinal Chemistry Letters published new progress about Alzheimer disease. 10305-42-7 belongs to class ethers-buliding-blocks, and the molecular formula is C3H8ClNO2S, Product Details of C3H8ClNO2S.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem