A novel series of benzenesulfonamide derivatives containing 4-aminobenzenesul-fonamide and α-amides branched valproic acid or 2,2-dimethylcyclopropanecarboxylic acid moieties were synthesized and screened for their anticonvulsant activities in mice maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ) test. The activity experimental study showed that 2,2-dipropyl-N1-(4-sulfamoylphenyl)malonamide (18b) had the lowest median effective dose (ED50) of 16.36 mg/kg in MES test, and 2,2-dimethyl-N-(4-sulfamoylphenyl)cyclopropane-1,1-dicarboxamide (12c) had the lowest ED50 of 22.50 mg/kg in scPTZ test, which resulted in the protective indexe (PI) of 24.8 and 20.4, respectively. These promising data suggest the new compounds have good potential as new class of anticonvulsant agents with high effectiveness and low toxicity for the treatment of epilepsy.
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Sulfonamides are the first effective chemotherapeutic agents used for several years to cure or prevent systemic bacterial infections. In addition, this agents showed anti-carbonic anhydrase and cause cell cycle perturbation in the G1 phase, disruption of microtubule assembly, suppression of the transcription activator Nf-Y, angiogenesis and matrix metalloproteinase (MMP). In recent years, novel synthesized sulfonamides have been introduced as antitumor, antiviral and anti-inflammatory agents. In this paper, the cytotoxic effects of 8 synthesized sulfonamides were investigated by MTT assay on HeLa, MDA-MD-468 and MCF-7 cancer cell lines. Human cancer cells were cultured and passaged in RPMI-1640 medium. Cells incubated in 96-well plates in a concentration of 1 × 105 cells/mL for 24 h, and then logarithmic concentrations (0.1 µm, 1 µm, 10 µm, 100 µm, 1mM) of each drug were prepared, added to the plates and incubated for 72 h. Cell survival was then determined using ELISA plate reader in 540 nm
JNST (ISSN: 2455-0191) - JACS Directory- Abstract: The title compound methyl (2E)-2-{[N-(2-formylphenyl)-4-methylbenzene sulfonamido] methyl}-3- phenylprop-2-enoate (MFMSPE) is a derivative of sulfonamide. FT-IR spectra of MFMSPE in the solid phase were recorded and analyzed. The optimized geometry and vibrational wave numbers were computed using DFT/B3LYP method with aid of 6-311++G (d,p) basis set. Stability of the molecule arising from hyper conjugative interactions, charge delocalization has been analyzed using natural bond orbital (NBO) analysis. The calculated HOMO and LUMO energies confirm that charge transfer occurs within the molecule. Molecular electrostatic potentials (MEP) was carried out at and interpreted. To recognize the biological activity of MFMSPE, molecular docking was done to recognize the hydrogen bond lengths and binding energy with antibacterial protein (1KE4).

Keywords: DFT Calculation; NBO; Molecular Docking; - Journal of Nanoscience and Technology.
Quinoline derivatives have diverse biological activities including anticancer activity. On the other hand, many sulfonamide derivatives exhibited good cytotoxic activity. Hybrids of both moieties may present novel anticancer agents. Chloroquinoline incorporating a biologically active benzene-sulfonamide moieties 5-21 and diarylsulfone derivatives 22 and 23 were prepared using (E)-1-(4-((E)-7-chloro-1-methylquinolin-4(1H)-ylideneamino)phenyl)-3-(dimethyl-amino)prop-2-en-1-one 4 as strategic starting material. The structure of the newly synthesized compounds were confirmed by elemental analyses and spectral data. Compound 4 was confirmed by X-ray crystallographic analysis. The prepared compounds were evaluated for their anticancer activity against Lung, HeLa, Colorectal and breast cancer cell lines. Compounds 2, 4, 7, 11, 14 and 17 showed better or comparable activity to 2′, 7′-dichlorofluorescein (DCF) as reference drug. Molecular docking of the active compounds on the active site of PI3K enzyme was
We used a targeted PCR of integrons from polluted environmental samples followed by amplicon sequencing using next generation sequencing technologies to greatly extend our knowledge of mobile antibiotic resistance genes found as gene cassettes. Combining the accuracy of short reads from Illumina sequencing with the higher resolution of long reads from PacBio sequencing generated a clear view of the gene cassettes and their immediate context, also providing clues about their evolutionary history. We therefore suggest that a similar approach could be applied to search for ARGs as well as other functional genes in different contexts.. Putative novel ARGs for aminoglycosides, beta-lactams, trimethoprim, rifampicin, chloramphenicol, and sulfonamides were identified. Several novel OXA variants provided reduced susceptibility to carbapenems, providing an additional battery of integron-borne genes that could contribute to resistance against last-line antibiotics. Many of the known and putative ARGs that ...
N-(1H-Imidazole-5-ylmethyl)-N-[4-[4-(benzylcarbamoyl)piperazino]phenyl]benzenesulfonamide | C28H30N6O3S | CID 44282638 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
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TYTU : Synthesis, QSAR studies, and metabolic stability of novel 2-alkylthio-4-chloro-N-(5-oxo-4,5-dihydro-1,2,4-triazin-3-yl)benzenesulfonamide derivatives as potential anticancer and apoptosis-inducing agents ...
PRIMARY OBJECTIVES:. I. To assess the feasibility and safety of individualizing pazopanib (pazopanib hydrochloride) monotherapy based upon attained pazopanib plasma concentrations so as to achieve desired target pazopanib plasma concentration in the highest possible fraction of treated patients.. SECONDARY OBJECTIVES:. I. To assess whether patient cytochrome P450 (CYP) or other polymorphisms may correlate with attained pazopanib levels in response to standard pazopanib dosing.. II. To assess whether patient trough pazopanib levels attained 24 hours after initiation of 800 mg daily fasting may predict steady state trough pazopanib levels after 14 days of pazopanib administration.. III. To assess whether patient trough pazopanib levels may correlate with observed pazopanib toxicities.. OUTLINE: This is a dose-escalation study.. Patients receive pazopanib hydrochloride orally (PO) once daily (QD) on days 1-28. Courses repeat every 28 days in the absence of disease progression or unacceptable ...
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The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More parti
A profound analysis of the industry based on the N-tert-butyl-benzothiazole Sulfonamide (TBBS) Market all over the world is named as Global N-tert-butyl-benzothiazole Sulfonamide (TBBS) Market Report. The research report assesses the current as well as the upcoming performance of the N-tert-butyl-benzothiazole Sulfonamide (TBBS) market, in addition to with newest trends in the market. The major player of the N-tert-butyl-benzothiazole Sulfonamide (TBBS) market (Lanxess, Eastman, Agrofert, KUMHO PETROCHEMICAL, Arkema, Kemai Chemical, Sunsine, Shandong Yanggu Huatai Chemical, Jiangsu Sinorgchem Technology, Puyang Willing Chemicals, Sumitomo Chemical, Sanshin, King Industries, Stairchem)are also included in the market report. The report forecasts the future of the N-tert-butyl-benzothiazole Sulfonamide (TBBS) market on the basis of this evaluation.. The research analysis for N-tert-butyl-benzothiazole Sulfonamide (TBBS) market comprises each and every feature of the market all over the world, ...
[Vitamins and metabolism of sulfonamides. I. Behavior of the sulfonamide levels in the body fluids and tissues of guinea pigs after loading with B complex vitam
ACID-CATALYZED REACTION OF PHENOLS WITH N -(4,4-DIETHOXYBUTYL)SULFONAMIDES - A NEW METHOD FOR THE SYNTHESIS OF 2-ARYL-1-SULFONYLPYRROLIDINES
ment, separation, and detection of the analytes were identifiedand optimized. The pH of the sample proved to be the mostinfluential variable during sample extraction. A critical impact onthe retention of the analytes on the cartridge material wasobserved, especially for sulfonamides caused by their aminogroups. Our enrichment tests between pH 2 and 6 revealed, asexpected, highest recoveries at pH 4 for the sulfonamides, whilethe recovery of the macrolides and trimethoprim showed nostrong pH dependence. This behavior can be explained by thecharge state of the sulfonamides at the particular pH values (Table1).26-31 With a compound specific pKa of 5-8 for the sulfonaminogroups (pKa 1) and a pKa of 2-2.5 for the arylamin (pKa 2), thesulfonamides are positively charged at pH 2 and negatively at a shows the breakdown curves for N4AcSMX and its four most pH above 5. The interaction with the cartridge material is strongest intense fragments as a function of the collision energy. As for analytes in ...
Sulfonamide antibiotics have been used to combat a wide spectrum of bacterial infections ever since the discovery of Prontosil in 1932.
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Compounds 9 and 11 were also noted as attractive, novel compounds in their own right. These were used for very limited library construction. The compounds derived from 9 were profiled first. While better than the parent bromide, subsequent structural analysis showed that they were not making good interactions with the sites intended (WPF shelf). The sulfonamides derived from 11 on the other hand showed significantly improved activity. The SAR was relatively insensitive to the substitution of the aryl group, due to the optimized placement on the shelf and the reversed sulfonamide ...
1222-40-8 - UWACTLZRFVZIPC-UHFFFAOYSA-N - 2H-1-Benzothiopyran-7-sulfonamide, 2-ethyl-3,4-dihydro-6-methyl-,1,1-dioxide - Similar structures search, synonyms, formulas, resource links, and other chemical information.
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Sickle cell disease is a highly prevalent disease in the United States, affecting 1 in 500 African American infants. It is common in individuals of African, Caribbean, Mediterranean, Arab, and other Middle Eastern descent. It is a genetic disorder with an autosomal recessive inheritance pattern. Sickle cell disease is often called "the first molecular disease" because the biochemical alteration in sickle hemoglobin described by Linus Pauling in 1948 was one of the first lesions identified at the molecular level for a human disease. Sickle hemoglobin forms rod-like polymers in deoxygenated red cells in areas of the circulation, with low oxygen tension, acidosis, or hyperosmolarity. Sickle hemoglobin polymerization causes a host of secondary molecular and cellular changes, many of which impair blood flow and contribute to tissue damage. The microcirculation can be acutely or chronically impaired in virtually any organ in the body, resulting in the characteristic crisis pattern of intermittent pain ...
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Title:Dosimetry and Toxicity Studies of the Novel Sulfonamide Derivative of Sulforhodamine 101([18F]SRF101) at a Preclinical Level. VOLUME: 12 ISSUE: 1. Author(s):Ingrid Kreimerman, Erick Mora-Ramirez, Laura Reyes, Manuel Bardiès, Eduardo Savio* and Henry Engler. Affiliation:Uruguayan Centre of Molecular Imaging (CUDIM), Radiopharmacy Department, Montevideo, Inserm, UMR1037 CRCT, F-31000 Toulouse, Uruguayan Centre of Molecular Imaging (CUDIM), Radiopharmacy Department, Montevideo, Inserm, UMR1037 CRCT, F-31000 Toulouse, Uruguayan Centre of Molecular Imaging (CUDIM), Radiopharmacy Department, Montevideo, Uruguayan Centre of Molecular Imaging (CUDIM), Radiopharmacy Department, Montevideo. Keywords:Preclinical evaluation, toxicity, dosimetry, [18F]SRF101, PET radiotracers, tissue-weighting factors.. Abstract:Background: The SR101 N-(3-[18F]Fluoropropyl) sulfonamide ([18F]SRF101) is a Sulforhodamine 101 derivative that was previously synthesised by our group. The fluorescent dye SR101 has been ...
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The purpose of the study is to investigate the possible benefits of giving the anti-HIV drug maraviroc to people who are taking darunavir/ritonavir alone for their HIV treatment. Many people successfully take only darunavir/ritonavir treatment for their HIV. However, there are some concerns that this treatment may not reach some areas of the body, such as the brain and spinal cord (central nervous system or CNS), as effectively as it does the bloodstream.. There is already a large clinical study looking at any differences between conventional HIV treatment with 3 drugs and single drug treatment with a protease inhibitor, also called PI monotherapy, such as darunavir/ritonavir. This includes differences in the effects on the CNS. However, this study will only be finished in 2013.. The investigators know that maraviroc can reach the CNS very effectively. The investigators in this study will investigate the effect of adding maraviroc to darunavir/ritonavir monotherapy by looking at levels of ...
Bosentan treatment for pulmonary arterial hypertension related to connective tissue disease: a subgroup analysis of the pivotal clinical trials and their open‐ ... Bosentan treatment for pulmonary arterial hypertension related to connective ... ,中国医师协会免疫吸附学术委员会
A green and efficient transformation of thioamide compounds to corresponding amides using heterogeneous silica supported tungstosilicic acid under solvent free conditions
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Rats administered doses up to 43 mg/kg/day in males and 52 mg/kg/day in females had no increases in tumor incidence, with the exception of a modest increase in the frequency of mammary gland fibroadenomas in female rats receiving doses ≥5.4 mg/kg (P,0.015). The highest doses of tamsulosin hydrochloride evaluated in the rat carcinogenicity study produced systemic exposures (AUC) in rats 3 times the exposures in men receiving the maximum therapeutic dose of 0.8 mg/day.. Mice were administered doses up to 127 mg/kg/day in males and 158 mg/kg/day in females. There were no significant tumor findings in male mice. Female mice treated for 2 years with the two highest doses of 45 and 158 mg/kg/day had statistically significant increases in the incidence of mammary gland fibroadenomas (P,0.0001) and adenocarcinomas (P,0.0075). The highest dose levels of tamsulosin hydrochloride evaluated in the mice carcinogenicity study produced systemic exposures (AUC) in mice 8 times the exposures in men receiving ...
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PubMedID: 24737576 | Acute renal failure associated with the new BRAF inhibitor vemurafenib: A case series of 8 patients. | Cancer | 7/15/2014
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It is important to note that sulfone-containing products are non-antibiotic sulfonamides and therefore also lack the N1 heterocyclic ring. Recent investigations into the COX-2 inhibitor, celecoxib, which also lacks the aromatic amine and N1-substituent, did not show any cross-reaction in patients with a sulfonamide antibiotic allergy.11,12 Another example of a sulfone-containing agent is the newer COX-2 inhibitor, etoricoxib (Figure 4),13,14 which is a sulfone and also lacks the aromatic amine and N1-substituent.. It seems most authors agree that non-antibiotics are less likely to cause severe reactions, and that the chemical differences between sulfa-antibiotics and non-antibiotics make true cross-reactivity extremely unlikely. An extensive literature survey found only one case report of anaphylaxis caused by furosemide;15 the authors were not able to prove that the allergen was in fact conclusively chemically related to the sulfa moiety.. Perhaps the most reassuring evidence comes from Strom ...
Several studies suggest that cyclooxygenase (COX)-2 plays a pivotal role in the progression of ischemic brain damage. In the present study, we investigated the effects of selective inhibition of COX-2 with nimesulide (12 mg/kg) and selective inhibition of COX-1 with valeryl salicylate (VAS, 12-120 mg/kg) on prostaglandin E2 (PGE2) levels, myeloperoxidase (MPO) activity, Evans Blue (EB) extravasation and infarct volume in a standardized model of transient focal cerebral ischemia in the rat. Postischemic treatment with nimesulide markedly reduced the increase in PGE2 levels in the ischemic cerebral cortex 24 h after stroke and diminished infarct size by 48 % with respect to vehicle-treated animals after 3 days of reperfusion. Furthermore, nimesulide significantly attenuated the blood-brain barrier (BBB) damage and leukocyte infiltration (as measured by EB leakage and MPO activity, respectively) seen at 48 h after the initial ischemic episode. These studies provide the first experimental evidence ...
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