Medicinal Chemistry
106 3 Basic Principles of Drug Design III Designing drug molecules to fit receptors 3.1 OVERALL STRATEGY: THE MULTIPHORE METHOD ...
and will constitute the pharmacophore. These drug-based functional groups are then “clicked together” in three-dimensional space ...
Design or identification of a lead (prototype) compound (section 3.2) Synthesis and initial biological evaluation of the lead c ...
of people with epilepsy, thereby realigning the bone plates of the skull, taking pressure off the brain, and alleviating the cur ...
During an era in which Isaac Newton and Charles Darwin were making colossal advances in physics and biology, medical therapy and ...
3.2.2 Lead Compound Identification by Serendipity Many of the significant advances in drug discovery over the past one and a hal ...
physiologically inert valproic acid as a solvent for their bismuth compounds. In doing so, they gained immense practical experie ...
enzyme inhibitors that prolong the effective half-life of remaining acetylcholine molecules within the brain. As discussed in ch ...
The first approach is shown in figure 3.1. This approach uses various techniques (e.g., alanine scanning) to identify the smalle ...
to render the molecule less like a naturally occurring peptide. Next, this segment is then rebuilt isosteric fragment by isoster ...
good supply of blood to the biting insect; such compounds could be useful in the treatment of stroke secondary to blood clots wi ...
territory. Several research institutes and well-established groups (notably the Scripps Institute of Oceanography and the Univer ...
opportunity to explore these non-naturally occurring synthetic compounds as potential lead compounds. The concept of rational dr ...
properties in a therapeutically beneficial manner. This is a design method that is lofty and difficult to attain. Rational drug ...
mechanics, appeared able to rigorously represent the physical properties of reality, including natural objects as large as plane ...
The most important aspect of computer-assisted modeling is the capability to perform three-dimensional docking experiments, a to ...
facetious. As mentioned, screening of compounds has a long and rather illustrious history and has produced many useful anticance ...
If a reliable bioassay is available, it is possible to screen thousands or even millions of compounds against this bioassay. The ...
occurring amino acids, it is possible to produce 8000 different tripeptides. If atypical amino acids and amino acids in the unna ...
diffusion, an appropriate developing agent is sprayed on the agar surface and areas in which bioactivity has occurred will show ...
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