Bioactivity-focused Semi-synthesis in Drug Discovery
A special issue of Molecules (ISSN 1420-3049).
Deadline for manuscript submissions: closed (30 October 2013) | Viewed by 23357
Special Issue Editor
Interests: antioxidant-inspired drug discovery; RONS scavenging-induced permanent changes in antioxidants' structure and function; chemistry and bioactivity of antioxidant metabolites; natural product isolation; semi-synthesis; drug-drug interactions; efflux-mediated multi-drug resistance
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
Thanks to millions of years of co-evolution between micro-organisms, plants and animals, Nature is a treasure mine of small molecules with potential for therapeutic drug discovery. By providing highly complex patterns of interactions with the various biochemical processes of other organisms, many secondary plant metabolites are easily recognized for their crucial role in the plants’ adaptation to their environment. An overview of which sources have yielded newly approved drugs the past 30 years clearly shows the success of utilizing Nature’s chemical complexity (Newman & Cragg 2012) inasmuch as the majority of these new drugs originated from a natural source or were designed on the basis of natural scaffolds. Dominancy of Nature-originated compounds is particularly true for antibacterial and anticancer drugs. On the other hand, very few natural leads pass through the drug development process per se. Various semi-synthetic modifications or designing synthetic analogs are usually needed for optimizing activity profile and bioavailability, and for decreasing unwanted side-effects and toxicity in order to meet the strict criteria for a modern therapeutic agent.
The present special issue of Molecules is dedicated to outstanding research and review papers within the scope of natural product based drug discovery via semi-synthetic approaches. Communications of any chemical modification of natural products are considered for publication as long as bioactivity is the focus of the work: manuscripts reporting optimization of pharmacodynamic and/or pharmacokinetic properties, decreasing toxicity, preparation of pro-drugs or even changing the biological target(s) of natural products are welcome. Preparation and investigation of semi-synthetic compound libraries from chemically engineered extracts is considered as an emerging area of the field which certainly also falls within the scope of this issue. Manuscripts may review reactions of certain typical natural scaffolds, biological significance of the products, or options that introduce selected moieties onto various natural skeletons in order to influence bioactivity. Authors of review papers are kindly requested to make a pre-submission inquiry with a brief outline to the guest editor.
Dr. Attila Hunyadi
Guest Editor
Manuscript Submission Information
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Keywords
- natural product based drug discovery
- rational drug design
- biomedical engineering
- isolation and chemical modification
- semi-synthesis
- bioactivity optimization
- side-effect profile improvement
- toxicity decrease
- pharmacodynamics
- pharmacokinetics
- ADME
- bioavailability
- pro-drug