Novel diversely substituted 1-heteroaryl-2-imidazolines for fragment-based drug discovery
نویسندگان
چکیده
منابع مشابه
1 Introduction to Fragment - based Drug Discovery
Fragment screening is the process of identifying relatively simple, often weakly potent, bioactivemolecules. It is gainingwide acceptance as a successful hit-finding technique both in its own right and as a method of finding hit molecules when traditional high-throughput screening (HTS) methods fail. Fragment hits are typically highly ‘ligand efficient’, i.e. possess a high binding affinity per...
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Fragment-based drug discovery (FBDD), while still a relatively new approach, has been so successful for identifying ligands for protein targets that it is alreadywidely regarded as representing a sea-change in drug discovery techniques. The strategy involves identifying small (typically ,300Da), low-affinity ligands (‘fragments’) and combining or expanding these to produce larger, higher-affini...
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The genomics revolution has provided a deluge of new targets for drug discovery. To facilitate the drug discovery process, many researchers are turning to fragment-based approaches to find lead molecules more efficiently. One such method, Tethering1, allows for the identification of small-molecule fragments that bind to specific regions of a protein target. These fragments can then be elaborate...
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Objective(s): Here, a reporter cell line containing two reporter vectors were developed, in order to monitor the Human T-Lymphotropic Virus type1(HTLV-1) infectivity and the cell viability simultaneously. Materials and Methods: The reporter cell line was constructed by stably transfected baby hamster's kidney cell line (BHK-21), with the genomes expressing two different reporters in separate pl...
متن کاملFragment approaches in structure-based drug discovery
There has been considerable interest recently in what is known as ;fragment-based lead discovery'. The novel feature of the approach is to begin with small low-affinity compounds. The main advantage is that a larger potential chemical diversity can be sampled with fewer compounds, which is particularly important for new target classes. The approach relies on careful design of the fragment libra...
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ژورنال
عنوان ژورنال: Tetrahedron Letters
سال: 2012
ISSN: 0040-4039
DOI: 10.1016/j.tetlet.2012.03.122