Buffalopox virus, a zoonotic Indian vaccinia-like virus, is responsible for contagious disease affecting mainly buffaloes, cattle and humans. H3L gene, encoding for an immunodominant major envelope protein of intracellular mature virion of orthopoxviruses, is highly conserved and found to elicit...

The major envelope protein, p35, of vaccinia virus (VV; strain LIVP) was purified by extraction from virions with the non-ionic detergent Nonidet P-40. The protein was cleaved with CNBr. Four homogeneous peptides were isolated and their N-terminal amino-acid (aa) sequences determined. A computer...

In this study, five phage display antibodies (pdAbs) against ectromelia virus (ECTV) were selected from vaccinia virus (VACV)-immune phage-display library of human single chain variable fragments (scFv). ELISA demonstrated that selected pdAbs could recognize ECTV, VACV, and cowpox virus (CPXV). ...

The antiproliferative metal chelate bis(2,3,4-trihydroxybenzaldoxyimato)copper(II) (CuTRI2) was shown to distinctly enhance the cytotoxicity of the spleen effector cells of CBA/CA mice to YAC-1 tumor cells in vitro as measured using a 4-h 51Cr release test. The compound was either added directly...

Heterobivalent ligands constituted by two different pharmacophores that bind to different molecular targets or to two distinct sites on the same molecular target could be one of the methods used for the treatment of cancer. In view of the importance of imidazo[1,2-b][1,3]thiazole and imidazo[1,2...

The activity of a series of imidazo[2,1-b]thiazole guanylhydrazones as inhibitors of p90 ribosomal S6 kinase 2 (RSK2) is described. It was found that a small subset of compounds show both potent inhibition of RSK2 kinase activity and tumor cell growth in vitro. Detailed study of one of the most ...

A series of 3,6-diphenylimidazo[2,1-b]thiazol-5-amine derivatives was synthesized and evaluated as potential inhibitors of 15-lipoxygenase. Among the synthesized compounds, 5i bearing 2,4,4-trimethylpentan-2-yl pendent group was the most active compound, being two times more potent than referenc...

Stereoselective inverse-demand [4+2] cycloadditions of 3,6-bis(pyridin-2-yl)-1,2,4,5-tetrazine and dimethyl 1,2,4,5-tetrazine-3,6-dicarboxylate to 4′-methylenedihydro-3′H-spiro[bicyclo[2.2.1]heptane-2,2′-furans] and 4′-methylene-1′-(4-nitrophenyl)spiro[bicyclo[2.2.1]heptane-3,2′-pyrrolidin...

A new 8-aminoquinoline antimalarial WR 238605 (Tafenoquine), developed initially as a primaquine alternative for prevention of Plasmodiumvivax relapses was evaluated for blood schizontocidal activity against two simian malaria infections namely Plasmodium cynomolgi B and Plasmodium fragile in rh...

Clinical manifestations of malaria infection in vertebrate hosts arise from the multiplication of the asexual stage parasites in the blood, while the gametocytes are responsible for the transmission of the disease. Antimalarial drugs that target the blood stage parasites and transmissible gameto...

The 8-aminoquinoline tafenoquine (TFQ), a primaquine derivative, is currently in late-stage clinical development for the radical cure of P. vivax. Here drug interactions between TFQ and chloroquine and six artemisinin-combination therapy (ACT) partner drugs in P. falciparum asexual stages and ga...

BackgroundTafenoquine is a new drug for malaria prevention. The goal of the present work was to conduct a specific neurobehavioral study in rats with histopathological assessment of the brain.

BackgroundTafenoquine is a new prophylactic antimalarial drug. The current analysis presents an integrated safety assessment of the Tafenoquine Anticipated Clinical Regimen (Tafenoquine ACR) from 5 clinical trials, including 1 conducted in deployed military personnel and 4 in non-deployed reside...

Water-soluble carbodiimides are frequently employed in coupling or conjugation reactions, e.g., to link a peptide immunogen to a carrier protein. However, their utility is limited by low coupling yields obtained under some conditions. We have found that addition of N-hydroxysul-fosuccinimide to ...

A method of the covalent immobilization of proteins on the surface of liposomes, containing 10% (by mol) of N-glutaryl phosphatidylethanolamine, is described. Carboxylic groups of liposomal N-glutaryl phosphatidylethanolamine were activated in the presence of water-soluble carbodiimide and N-hyd...

In the current work, we employed optimized block-wise variable combination (OBVC) by particle swarm optimization (PSO) based on partial least squares (PLS) modeling for variable combination and compared it to the traditional methods. It has been demonstrated that the modified PSO is a useful too...

A series of 2,4,6 trisubstituted pyrimidines and triazines have been synthesized and screened for its in vitro antileishmanial activity profile in promastigote model. Nine compounds have shown >94% inhibition against promastigotes at a concentration of 10 μg/mL.

Prevention of environmentally induced cancers is a major health problem of which solutions depend on the rapid and accurate screening of potential chemical hazards. Lately, theoretical approaches such as the one proposed here – Quantitative Structure–Activity Relationship (QSAR) – are increas...

The products of decomposition in anaerobic aqueous solution at pH 7.1 and 37° were determined for two series of novel anticancer agents incorporating both nitroimidazole and 2-chloroethylnitrosourea moieties (NI-CENUs) and examples of which exhibit preferential hypoxic toxicity against HeLa-MR ...

The structural results clearly indicate that 1-butyl-3-cyano-6-hydroxy-4-methyl-5-(2-thiazolylazo)-2(1H)-pyridone, (C14H15N5O2S), exists primarily as the hydrazone tautomer in the solid state. The molecule is nearly planar not regarding the butyl group. Some of the bond lengths and angles are di...