Search results for "thiadiazole"
showing 10 items of 79 documents
Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-(thi)one derivatives.
2002
Several 2,3-diaryl-1,3-thiazolidine-4-thione derivatives and 2,3-diaryl-1,3-thiazolidin-4-ones bearing a methyl group at C-5 position have been synthesized and tested as anti-HIV agents. The results of the in vitro tests showed that some of them proved to be effective inhibitors of HIV-1 replication.
CCDC 684501: Experimental Crystal Structure Determination
2008
Related Article: M.Holm, D.Schollmeyer, S.Laufer|2008|Acta Crystallogr.,Sect.E:Struct.Rep.Online|64|o700|doi:10.1107/S1600536808003917
Preparation and Promotion of Fruit Growth in Kiwifruit of Fluorinated N-Phenyl-N‘-1,2,3-thiadiazol-5-yl Ureas
2004
Seventeen phenyl-fluorinated analogues of thidiazuron [N-phenyl-N'-(1,2,3-thiadiazol-5-yl)urea, TDZ] have been prepared and characterized. The effects of each fluorinated urea on growth and quality of kiwifruits (Actinidia deliciosa) were evaluated by comparison with untreated (control) and TDZ-treated fruits. The results obtained showed a clear dependence of the growth-promoting activity of these fluorinated ureas on the pattern and degree of fluorine substitution in the phenyl ring. The most effective for promoting fruit growth was N-(2,3,5,6-tetrafluorophenyl)-N'-(1',2',3'-thiadiazol-5'-yl)urea at 25 ppm (at harvest, treated fruits were 58% heavier than untreated ones) followed by N-(3,5…
Non-Innocent Base Properties of 3- and 4-Pyridyl-dithia- and Diselenadiazolyl Radicals : The Effect of N-Methylation
2018
International audience; Condensation of persilylated nicotinimideamide and isonicotinimideamide with sulfur monochloride affords double salts of the 3-, 4-pyridyl-substituted 1,2,3,5-dithiadiazolylium DTDA cations of the general formula [3-, 4-pyDTDA][Cl][HCl] in which the pyridyl nitrogen serves as a noninnocent base. Reduction of these salts with triphenylantimony followed by deprotonation of the intermediate-protonated radical affords the free base radicals [3-, 4-pyDTDA], the crystal structures of which, along with those of their diselenadiazolyl analogues [3-, 4-pyDSDA], have been characterized by powder or single-crystal X-ray diffraction. The crystal structures consist of “pancake” π…
GSK-3? Can Regulate the Sensitivity of MIA-PaCa-2 Pancreatic and MCF-7 Breast Cancer Cells to Chemotherapeutic Drugs, Targeted Therapeutics and Nutra…
2021
Glycogen synthase kinase-3 (GSK-3) is a regulator of signaling pathways. KRas is frequently mutated in pancreatic cancers. The growth of certain pancreatic cancers is KRas-dependent and can be suppressed by GSK-3 inhibitors, documenting a link between KRas and GSK-3. To further elucidate the roles of GSK-3β in drug-resistance, we transfected KRas-dependent MIA-PaCa-2 pancreatic cells with wild-type (WT) and kinase-dead (KD) forms of GSK-3β. Transfection of MIA-PaCa-2 cells with WT-GSK-3β increased their resistance to various chemotherapeutic drugs and certain small molecule inhibitors. Transfection of cells with KD-GSK-3β often increased therapeutic sensitivity. An exception was observed wi…
Formation of Pyrazol-1,3,4-Thiadiazoles through 1,3-Dipolar Cycloadditions of 3-Thioxo-[1,2,4]-Triazepin-5-one with Nitrilimines: An Experimental and…
2009
In this work the results of experimental and computational study of the title compounds and some ancillary compounds are reported. Two bicyclic pyrazol-1,3,4-thiadiazole derivatives were synthesized by reaction between 6-dimethylaminomethylene-3-thioxo-[1,2,4]- triazepin-5-one 1 and several nitrilimines 2a-f to give corresponding spirocycloadducts 3a-f, which undergo a rapid rearrangement leading to the new bicyclic compounds, 4a-f and 5a-f. These obtained bicyclic products were characterized by 1H and 13C NMR spectroscopy and finally by X-ray crystallography. Theoretical calculations have been carried out using DFT methods to rationalize the formation of the two new bicyclic compounds. Two…
SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL SMALL MOLECULES AS PROMISING ALTERNATIVE AGENTS TO COUNTERACT DRUG RESISTANCE IN CANCER AND MICROBIAL IN…
2022
Il cancro rimane un grave problema di salute pubblica, rappresentando la seconda principale causa di morte in tutto il mondo. Tra le diverse tipologie di tumori, l'adenocarcinoma duttale pancreatico (PDAC) è una delle forme più letali nell'uomo, a causa della diagnosi tardiva e delle limitate possibilità di trattamento. Pertanto, lo studio di nuove strategie terapeutiche per i pazienti affetti da PDAC è altamente necessario. Allo stesso modo, il mesotelioma rappresenta una malattia rara ma aggressiva, difficile da diagnosticare per il lungo periodo di latenza prima dei segni clinici. Gli approcci terapeutici standard includono la chirurgia, la chemioterapia e la radioterapia. Tuttavia, la s…
Biological Evaluation of the Antiproliferative and Anti-migratory Activity of a Series of 3-(6-Phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indole …
2019
Heterocyclic rings are recognized as key components of many natural, semi-synthetic and synthetic molecules with a broad spectrum of biological activities. Among these molecules, the indole and imidazo[2,1-b][1,3,4]thiadiazole systems have recently been described as useful scaffolds for the design of anticancer agents. Herein the antitumor activity of a series of 3-(6-phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indoles, designed as hybrid structures, was assessed. Seven out of 10 compounds (1a-g) were submitted to National Cancer Institute (NCI). Remarkably, compound 1g showed antiproliferative activity against the full panel of sixty human cancer lines, with half-maximal inhibitory conc…
Synthesis and antimicrobial screening of tetra Schiff bases of 1,2,4,5-tetra (5-amino-1,3,4-thiadiazole-2-yl)benzene
2014
Abstract In the present study, novel tetra Schiff bases were synthesized by condensation of 1,2,4,5-tetra (5-amino-1,3,4-thiadiazole-2-yl)benzene with different aromatic aldehydes. The chemical structures were confirmed by means of IR, 1 H NMR, 13 C NMR, and elemental analysis. All compounds were screened for antibacterial ( Staphylococcus aureus ATCC-9144, Staphylococcus epidermidis ATCC-155, Micrococcus luteus ATCC-4698, Bacillus cereus ATCC-11778, Escherichia coli ATCC-25922, and Pseudomonas aeruginosa ATCC-2853) and antifungal ( Aspergillus niger ATCC-9029 and Aspergillus fumigatus ATCC-46645) activities by paper disc diffusion technique. The minimum inhibitory concentrations (MICs) of …
Synthesis and characterization of a Cu(II) complex of 2-benzylmercapto-5- methyl-1,3,4-thiadiazole (C10H10N2S 2)
2008
A Cu(II) complex of 2-benzylmercapto-5-methyl-1,3,4-thiadiazole was synthesized and characterized. The crystal structure of the copper complex and the free ligand were determined by single-crystal X-ray diffraction at room temperature: {[Cu(C10H10N2S2) 2(Cl)2], P1 triclinic, a = 8.1450(2) Å, b = 8.1690(2) Å, c = 10.8180(3) Å, α = 97.4040(12)°, β = 101.6270(11)°, γ = 116.1431(14)°; C10H10N2S2 ligand, Pbca orthorhombic, a = 8.7938(7) Å, b = 9.6491(7) Å, c = 25.3552(18) Å}. The metal complex framework consists of discrete units that provide crystalline stability through a network of van der Waals contacts. The Cu(II) is coordinated by two chloride ions and two 2-benzylmercapto-5-methyl-1,3,4- …