Synthesis of a new series of sulfonamides containing isatin moiety

Im Rahmen der Ökoqualitätsverordnung (ÖQV) erhalten Schweizer Landwirte Direktzahlungen, wenn eine definierte Mindestanzahl seltener Arten auf ihrem Grünland stehen, wofür Transaktionskosten nur etwa in der Höhe wie bei konventionellen Agrarumweltprogrammen entstehen. Dieser Beitrag beschäftigt sich mit der Effektivität dieses outputorientierten Programms. Eine Konfiguralfrequenzanalyse zeigt, dass Landwirte, die an der ÖQV teilnehmen, mit nur geringer Wahrscheinlichkeit ihre Teilnahme an Agrarumweltprogrammen reduzieren. Es wird die Schlussfolgerung gezogen, dass outputorientierte Agrarumweltprogramme ein effizientes Mittel zur Erlangung ökologischer Qualität sind

A new family of 1,2,5-thiadiazolidine 1,1-dioxides: Synthesis, structure and antibacterial activity

International audienceA convenient synthesis of novel N-N’-substituted 1,2,5-thiadiazolidine 1,1-dioxides starting from amino acids isreported in five step (reduction, carbamoylation-sulfamoylation, intermolecular cyclization via the Mitsunobureaction and acylation). The newly synthesized compounds were characterized by IR, NMR and mass spectralanalysis. Some of the newly synthesized compounds (4c and 4d) were examined for their antibacterial activityagainst several strains of Gram-positive and Gram-negative bacteria

Effect of novel phosphoramidate on growth and respiratory metabolism of Paramecium aurelia

The continuous increase in the number of new chemicals as well as the discharges of solid and liquid wastes triggered the need for simple and inexpensive bioassays for routine testing. In recent years, there has been increasing development of methods (particularly rapid tests) for testing environmental samples. This paper describes the quick toxic evaluation of a novel synthetic compound: Phosphoramidate derivative B at different concentrations (2, 4 and 8 μM) for 72 h on Paramecium aurelia. We showed that B concentrations affect the growth of Paramecium in concentration- dependent manner; also it decreases the growth rate and increases response percentage in concentration- dependent manner. The value of LC50 obtained for these protozoa was estimated at 4.9693 μM after 24 hours of exposure. The respiratory metabolism of protozoan is perturbed at three concentrations, noting that the oxygen consumption was significantly increased at high concentrations after 18 hours of exposure. The results indicate that the Paramecium toxicity assay could be used as a complementary system to rapidly elucidate the cytotoxic potential of insecticides. The major advantages associated with these tests are: inexpensive, simple, rapid and seem to be attractive alternatives to conventional bioassay

New pseudonucleosides containing chiral oxazolidin-2-ones and cyclosulfamides as aglycones: Synthesis and antiviral evaluation

9 - conference paper: Proceedings of the 17th International Roundtable of Nucleosides, Nucleotides, and Nucleic Acids MAR 07-SEP 07, 2006 Bern (SWITZERLAND)A series of chiral cyclosulfamides and oxazolidinon-2-ones have been synthesized starting from aminoacids. Regioselective substitution of these pseudopyrimidic heterocyles was carried out under Mitsunobu conditions. Best substitution results were obtained by preliminary deprotection of cyclosulfamides and their condensation with beta-D-ribofuranose. Chiral oxazolidin-2-ones were coupled directly with D-ribofuranose. All compounds were tested against HSV-2, VV and SV viruses. Two compounds 6b and 6e showed significant activities against HSV-type 1

Synthesis and antitumor evaluation of novel sulfonylcycloureas derived from nitrogen mustard

International audienceA new series of sulfonylcycloureas derivatives have been synthesized and evaluated in vitro for their antitumor activity against four cancer cell lines (A431, Jurkat, U266, and K562). These compounds were prepared by the condensation of several sulfonamides (2a–m) with ethyl bis(2-chloroethyl)carbamate (1a). The relative cytotoxicity of these new derivatives in comparison to chlorambucil is reported

Morphological, molecular, and biochemical study of cyanobacteria from a eutrophic Algerian reservoir (Cheffia)

The cyanobacteria management in water bodies requires a deep knowledge of the community composition. Considering the reliable and thorough information provided by the polyphasic approach in cyanobacteria taxonomy, here we assess the cyanobacterial community structure of the Cheffia reservoir from Algeria. Cyanobacteria were identified on the basis of morphological traits and next-generation sequencing (NGS); toxins-related genes were localized in addition to the identification of toxins; temperature and nutrient level of water samples were also determined. The polyphasic approach was essential for cyanobacteria investigation; 28 genera were identified through 16S rRNA metabarcoding with the dominance of taxa from Microcystis (34.2%), Aphanizomenon (20.1%), and Planktothrix (20.0%), and morphological analysis revealed the association in this water body of five species within the genus Microcystis: M. aeruginosa, M. novacekii, M. panniformis, M. ichthyoblabe, and M. flos-aquae. The presence of mcyE genotypes was detected; moreover, HPLC–PDA and LC–ESI–MS/MS revealed the production of microcystin-LR. Results obtained in our study are very important since this ecosystem is used for water supply and irrigation; as a consequence, a good water management plan is essential

Synthesis and Evaluation of Some New 4<i>H</i>-Pyran Derivatives as Antioxidant, Antibacterial and Anti-HCT-116 Cells of CRC, with Molecular Docking, Antiproliferative, Apoptotic and ADME Investigations

Colorectal cancer oncogenesis is linked to dysbiosis, oxidative stress and overexpression of CDK2. The 4H-pyran scaffold is considered an antitumoral, antibacterial and antioxidant lead as well as a CDK2 inhibitor. Herein, certain 4H-pyran derivatives were evaluated as antibacterial, antioxidant and cytotoxic agents against HCT-116 cells. Derivatives 4g and 4j inhibited all the tested Gram-positive isolates, except for B. cereus (ATCC 14579), with lower IC50 values (µM) than ampicillin. In addition, 4g and 4j demonstrated the strongest DPPH scavenging and reducing potencies, with 4j being more efficient than BHT. In cell viability assays, 4d and 4k suppressed the proliferation of HCT-116 cells, with the lowest IC50 values being 75.1 and 85.88 µM, respectively. The results of molecular docking simulations of 4d and 4k, inhibitory kinase assays against CDK2, along with determination of CDK2 protein concentration and the expression level of CDK2 gene in the lysates of HCT-116 treated cells, suggested that these analogues blocked the proliferation of HCT-116 cells by inhibiting kinase activity and downregulating expression levels of CDK2 protein and gene. Moreover, 4d and 4k were found to induce apoptosis in HCT-116 cells via activation of the caspase-3 gene. Lastly, compounds 4g, 4j, 4d and 4k were predicted to comply with Lipinski’s rule of five, and they are expected to possess excellent physiochemical and pharmacokinetic properties suitable for in vivo bioavailability, as predicted by the SwissADME web tool