thiourea and thiosemicarbazide

Bisindolylmethane thiosemicarbazides 1-18 were synthesized, characterized by

Topics: Canavalia; Dose-Response Relationship, Drug; Enzyme Inhibitors; Indoles; Models, Molecular; Molecular Structure; Semicarbazides; Structure-Activity Relationship; Urease

An efficient solid-phase synthetic route for the construction of 1,3,4-oxadiazole and 1,3,4-thiadiazole libraries based on branching diversity-oriented synthesis (DOS) has been developed in this study. The core skeleton resins, 1,3,4-oxadiazole and 1,3,4-thiadiazole, were obtained through desulfurative and dehydrative cyclizations of thiosemicarbazide resin, respectively. Various functional groups have been introduced to the core skeleton resins, such as aryl, amine, amide, urea, thiourea, and an amino acid. Most of the libraries were purified by simple trituration without extraction or column chromatography after cleavage of the products from the solid-supported resin. As a result, we obtained high yields of pure 1,3,4-oxadiazole and 1,3,4-thiadiazole derivatives (total numbers = 128). Finally, we confirmed the drug-like properties of our library by calculation of physicochemical properties, displays of the skeletal diversities of the library in 3D-space, and occupation of a broad range of areas by their functional groups.

Topics: Amides; Amines; Amino Acids; Combinatorial Chemistry Techniques; Cyclization; Molecular Structure; Oxadiazoles; Semicarbazides; Small Molecule Libraries; Solid-Phase Synthesis Techniques; Structure-Activity Relationship; Thiadiazoles; Thiourea

By a simple and convenient method of using formaldehyde as linkages, two new chitosan (CS) derivatives modified respectively with thiosemicarbazide (TSFCS) and thiocarbohydrazide (TCFCS) were synthesized. The new compounds were characterized and studied by Fourier transform infrared spectroscopy, elemental analysis, thermal gravity analysis and differential scanning calorimetry, and their surface morphologies were determined via scanning electron microscopy. These CS derivatives could form pH dependent gels. The behavior of 304 steel in 2% acetic acid containing different inhibitors or different concentrations of inhibitor had been studied by potentiodynamic polarization test. The preliminary results show that the new compound TCFCS can act as a mixed-type metal anticorrosion inhibitor in some extent; its inhibition efficiency is 92% when the concentration was 60 mg/L. The adsorption studies on a metal ion mixture aqueous solution show that two samples TSFCS and TCFCS can absorb As (V), Ni (II), Cu (II), Cd (II) and Pb (II) efficiently at pH 9 and 4.

Topics: Adsorption; Amines; Chitosan; Corrosion; Electrochemical Techniques; Hydrazines; Hydrogen-Ion Concentration; Metals, Heavy; Microscopy, Electron, Scanning; Nanoparticles; Semicarbazides; Spectroscopy, Fourier Transform Infrared; Surface Properties; Thiourea

A novel series of (E)-1-((2-(1-methyl-1H-imidazol-5-yl) quinolin-4-yl) methylene) thiosemicarbazides was discovered as potent inhibitors of IKKβ. In this Letter we document our efforts at further optimization of this series, culminating in 2 with submicromolar potency in a HWB assay and efficacy in a CIA mouse model.

Topics: Animals; Dogs; Female; Hepatocytes; High-Throughput Screening Assays; Humans; I-kappa B Kinase; Macaca mulatta; Male; Mice; Protein Kinase Inhibitors; Quinolines; Rats; Semicarbazides; Structure-Activity Relationship; Thiourea

A novel tridentate thiosemicarbazide-type ligand class with an SNS donor set, H(2)L(1), was prepared by reactions of N-[N',N'-dialkylamino(thiocarbonyl)]benzimidoyl chlorides with thiosemicarbazides. H(2)L(1) ligands readily react with (NBu(4))[TcOCl(4)] in MeOH under the formation of red oxotechnetium(V) complexes of composition [TcOCl(L(1))]. The monomeric, five-coordinate compounds are air-stable and bind (L(1))(2-) tridentate in the equatorial coordination sphere. The compounds represent the first examples of oxotechnetium(V) complexes with NS chelate-bonded thiosemicarbazones.

Topics: Ligands; Models, Molecular; Molecular Conformation; Organotechnetium Compounds; Semicarbazides; Thiourea

Two novel series of thio compounds bearing internal structural modifications of hexestrol were synthesized as potential anticancer agents. The first contains several N-substituted thiourea functions, and the second contains various N4-substituted-3-thiosemicarbazide moieties in place of one alpha-ethyl group of hexestrol dimethyl ether. The products showed no antileukemic activity in the P-388 lymphocytic leukemia system and did not exhibit any anticonvulsant or estrogenic properties.

Topics: Animals; Antineoplastic Agents; Hexestrol; Leukemia P388; Mice; Semicarbazides; Structure-Activity Relationship; Thiourea

Topics: Aminosalicylic Acid; Aminosalicylic Acids; Antitubercular Agents; Chemistry, Pharmaceutical; Isoniazid; Pharmacology; Rabbits; Research; Semicarbazides; Thiocyanates; Thiosemicarbazones; Thiourea

Topics: Amino Acids; Animals; Brain; gamma-Aminobutyric Acid; Hydrazines; Neurochemistry; Rats; Seizures; Semicarbazides; Thiourea

Topics: Azoles; Semicarbazides; Thiosemicarbazones; Thiourea

Topics: Ethylamines; Imines; Semicarbazides; Thiazoles; Thiocarbamates; Thiourea

Topics: Humans; Semicarbazides; Thiourea