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There is a Need for Highly Diverse Chiral Libraries!
Definition: A tailor-made synthetic compound library of highly diverse, nitrogen containing, natural product like molecules with gram-scale resupply opportunities and feasible lead generating chemistry that covers the chemical space of your target.
With the introduction of combinatorial chemistry and parallel synthesis, a new era of drug
discovery began. Suddenly, it was feasible to quickly generate thousands of new compounds
with relatively simple synthetic efforts. Concurrently, an increasing number of druggable
targets emerged from the human genome project; achievements which seemed to form a
powerful alliance to address unmet medical needs. The promise of new chemical entities
(NCE) seemed to appear on the horizon.
Despite this tremendous technical progress, the expected flood
of NCEs never did materialize, presumably because synthetic
molecules often lack diversity and 3- dimensionality required
for complex binding action. This is simply due to a limited number of
applicable reaction pathways and building blocks in the hands of synthetic chemists. Nature - so it seems - is the better chemist providing us with
enzymatically engineered and biologically validated small
molecules called natural products (NP).
As a matter of fact, the enormous potential of NP’s to generate new drugs (more than 40%
of all blockbuster drugs are NPs or their derivatives) is unquestioned in the drug discovery
community.
It is only because of logistical problems like lack of sufficient numbers of discrete
natural product molecules for HTS, unsatisfactory resupply when a hit is identified,
and complex, time consuming medicinal chemistry, that pharmaceutical companies
preferred to avoid the efforts required to fully access nature's pool of diversity.
Now, AnalytiCon
Discovery has removed these obstacles by creating NatDiverse™ libraries.
NatDiverse™:
When modern synthetic chemistry meets nature!
With NatDiverse™, AnalytiCon Discovery marries the diversity of nature with the power of
modern parallel synthesis. Chiral, nitrogen containing, natural compound-like molecules can
be quickly reproduced in accordance with state-of-the-art medicinal chemistry rules to
generate molecules that are druglike.
NatDiverse™ enables drug discovery departments to access a huge number of natural
carriers of pharmacophore groups with an extraordinary high level of patentability. Medicinal
chemistry complications, resupply problems and scale-up restrictions belong to an earlier era
of traditional natural extract screening.
AnalytiCon's carefully selected natural small molecule
scaffolds share four main selection criteria that form the basis of each
NatDiverse™ library design:
With
this approach, AnalytiCon takes into account that the drug discovery chain
has to be fed with increasing amounts of a compound when moving upstream;
i.e. the production of molecules must be scalable. Furthermore, NatDiverse™
compounds provide an excellent platform for subsequent lead generation
chemistry. A selected scaffold undergoes a substantial synthetic transformation
process leading to 6 up to 8 templates (see example). In a subsequent
decoration step approx. 100 to 300 novel chiral compounds with exactly
defined stereochemistry will sprout from each of these templates.
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| Search NatDiverse™ with our Online Substructure Database |
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Download
NatDiverse™ General Description |
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