ABSTRACT
Bioactive natural products of novel structural types play a highly significant role in the drug discovery and development process. Of the 1,031 new chemical entities covering all diseases in the years 1981-2002, 48% were natural product mimics, 5% were the direct utility of natural products as sources of novel structures. Up to now, the main challenges are more efficient and rapid processes for discovery and isolation of bioactive natural products of novel structural types. Therefore, new strategies and ideas for chemical study on bioactive natural products of novel structural types should be applied. In order to discover a large number of bioactive natural products of novel structural types from naturally occurring sources and elucidate the intrinsic value of natural products as leads to new structures with different activities, new, more efficient and rapid processes for study on natural products will be established by use of modern chromatographies, techniques on line identification of natural products and screening methods based on molecular targets.
Subject(s)
Humans , Biological Products , Chemistry , Drug Design , Drug Evaluation, Preclinical , Pharmaceutical Preparations , Pharmacognosy , Methods , Plant Extracts , Pharmacology , Plants, Medicinal , Chemistry , Classification , Structure-Activity RelationshipABSTRACT
<p><b>AIM</b>To provide basic data for the synthesis of new sinomenine derivatives.</p><p><b>METHODS</b>The C ring in sinomenine was modified.</p><p><b>RESULTS</b>Seven compounds were prepared and screened for anti-inflammatory and analgesic activities. Compounds 2 and 5 showed better activities.</p><p><b>CONCLUSION</b>Modification of the C ring in sinomenine should be worthy to be studied further.</p>
