Structural studies and investigation on the antifungal activity of silver(I) complexes with 5-nitrofuran-derived hydrazones
摘要:
Silver(I) complexes [Ag(HL1)(2)]NO3 (1), with N'-((5-nitrofuran-2-yl)methylene)acetohydrazide (HL1), and [Ag(HL2)(2)NO3] (2) with N'-((5-nitrofuran-2-yl)methylene)benzohydrazide (HL2) were synthesized. The crystal structures of HL1 and complexes (1) and (2) were determined. The ligands showed no or poor antifungal activity against Candida spp. The silver(I) complexes demonstrated themselves to be more active than silver nitrate and, in some cases, more active than miconazole nitrate and nystatin. (C) 2019 Elsevier Ltd. All rights reserved.
Designing and exploring active N′-[(5-nitrofuran-2-yl) methylene] substituted hydrazides against three Trypanosoma cruzi strains more prevalent in Chagas disease patients
摘要:
Chagas disease affects around 8 million people worldwide and its treatment depends on only two nitroheterocyclic drugs, benznidazole (BZD) and nifurtimox (NFX). Both drugs have limited curative power in chronic phase of disease. Nifuroxazide (NF), a nitroheterocyclic drug, was used as lead to design a set of twenty one compounds in order to improve the anti-Trypanosoma cruzi activity. Lipinski's rules were considered in order to support drug-likeness designing. The set of N'-[(5-nitrofuran-2-yl) methylene] substituted hydrazides was assayed against three T. cruzi strains, which represent the discrete typing units more prevalent in human patients: Y (TcII), Silvio X10 cl1 (TcI), and Bug 2149 cl10 (TcV). All the derivatives, except one, showed enhanced trypanocidal activity against the three strains as compared to BZD. In the Y strain 62% of the compounds were more active than NFX. The most active compound was N'((5-nitrofuran-2-yl) methylene)biphenyl-4-carbohydrazide (C20), which showed IC50 values of 1.17 +/- 0.12 mu M; 3.17 +/- 0.32 mu M; and 1.81 +/- 0.18 mu M for Y, Silvio X10 cl1, and Bug 2149 cl10 strains, respectively. Cytotoxicity assays with human fibroblast cells have demonstrated high selectivity indices for several compounds. Exploratory data analysis indicated that primarily topological, steric/geometric, and electronic properties have contributed to the discrimination of the set of investigated compounds. The findings can be helpful to drive the designing, and subsequently, the synthesis of additional promising drugs against Chagas disease. (C) 2015 Elsevier Masson SAS. All rights reserved.
The invention relates to novel rapidly-curing adhesives made from hydrophilic polyisocyanate prepolymers for application in surgery.
该发明涉及一种用于手术中的新型快速固化胶粘剂,该胶粘剂由亲水性聚异氰酸酯预聚物制成。
Diagnostic/therapeutic agents
申请人:Klaveness Jo
公开号:US20050002865A1
公开(公告)日:2005-01-06
Targetable diagnostic and/or therapeutically active agents, e.g. ultrasound contrast agents, comprising a suspension in an aqueous carrier liquid of a reporter comprising gas-containing or gas-generating material, said agent being capable of forming at least two types of binding pairs with a target.
Immunogenic composition comprising live encysted protozoa
申请人:UNILEVER N.V.
公开号:EP0134703A1
公开(公告)日:1985-03-20
An oral vaccine against parasitic protozoa, such as coccidia, comprises live encysted protozoa embedded in a firm gel matrix from which the protozoa are released following ingestion by a host. The gel matrix helps to maintain the essential viability of the protozoa without seriously hindering the natural mechanism by which they infect their host. Preferably the gel matrix is based on alginate. Alginate beadlets containing viable sporulated coccidia oocysts, for administration to poultry, are a preferred feature.
A composition useful in oral immunisation of animals such as poultry comprises dry free-flowing particles each consisting of a solid beadlet of lipid-continuous emulsion containing from about 25% to about 50% by weight water in a lipid, such as hardened palm kernel oil, having a slip point in the range 35 to 45°C, each beadlet having an average diameter of about 2 to 3 millimetres and containing at least 1 viable encysted protozoan, such as a sporulated oocyst of a species of coccidium infective to poultry, each beadlet having a protective coating of animal feed, cement and/or gypsum, the protective coating having an average thickness of about 0.2 to 2mm.