Publications

Bicyclic furanopyrimidines were recently discovered by us to be potent and selective inhibitors of VZV. Related studies to investigate the role of the sugar in this activity uncovered dideoxy furanopyrimidines as inhibitors of HCMV and this led to the preparation of highly modified long alkyl chain furanopyrimidines from the N- and O-alkylation of their parent bases. Herein we describe their synthesis and subsequent biological evaluation against HCMV. O-alkylated derivatives were almost invariably found to be at least equiactive with their N-alkylated counterparts. At this point, little change in activity has been found with large variation in N- and O-substituent.

Abstract For Abstract see ChemInform Abstract in Full Text.

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Open-porous structures from ß-type Ti-45Nb, as a new biomaterial with an excellent biocompatibility, are produced by selective laser melting (SLM). However, the products commonly suffer from uncontrolled surface issues such as staircase effect and non-melted (or...

Purpose – This paper aims to present parametric models to estimate the environmental footprint of the selective laser sintering (SLS)’ production phase, covering energy and resource consumption as well as process emissions. Additive manufacturing processes such as (SLS) are often considered to be more sustainable then conventional manufacturing methods. However, quantitative analyses of the environmental impact of these processes are still limited and mainly focus on energy consumption. Design/methodology/approach – The required Life Cycle Inventory data are collected using the CO2PE! – Methodology, including time, power, consumables and emission studies. Multiple linear regression analyses have been applied to investigate the interrelationships between product design features on the one hand and production time (energy and resource consumption) on the other hand. Findings – The proposed parametric process models provide accurate estimations of the environmental footprint of SLS processes based on two design features, build height and volume, and help to identify and quantify measures for significant impact reduction of both involved products and the supporting machine tools. Practical implications – The gained environmental insight can be used as input for ecodesign activities, as well as environmental comparison of alternative manufacturing process plans. Originality/value – This article aims to overcome the current lack of environmental impact models, covering energy and resource consumption as well as process emissions for SLS processes.

On the basis of structural features, binding mode, and structure-activity relationship studies of two pyrimidine-derived non-nucleoside reverse-transcriptase inhibitors, DABOs, and diaryl pyrimidines, a novel class of 1,2,6-thiadiazine-1,1-dione derivatives were rationally designed using the strategies of bioisosterism and molecular hybridization, synthesized, and evaluated for their anti-HIV activity in MT4 cell cultures. Three compounds were found to have moderate activity against HIV-1 replication with EC50 values ranging from 23 to 32 μm. To further confirm the binding target, compound IIg was selected to conduct an HIV-1 reverse-transcriptase inhibitory assay. In addition, preliminary structure-activity relationship analysis among the newly synthesized compounds was discussed, and the binding mode of the active compound IIg was rationalized by molecular docking and physicochemical studies.

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.