Synthetic drugs’ natural origins

These drugs, which may be of synthetic or natural origin, produce psychic alterations and behavior modifications often they induce the consumer to periodically... 

A major hurdle on the road to enantiomerically pure drugs is the development of efficient methods of asymmetric synthesis. In many cases, small chiral compounds of synthetic or natural origin are used as starting... 

Drugs may also be classified according to origin, as is done in Table 14.2. Drugs that are natural products come directly from terrestrial or marine plants or animals. Drugs that are chemical derivatives are natural products that have been chemically modified to increase potency or decrease side effects. Synthetic drugs are those that originate in the laboratory. 

A third role of natural products is their utility as prototypes or models for synthetic drugs possessing physiological activities similar to the original drug. Procaine and similar local anesthetics are commonly cited representatives of this category. 

The majority of the new drugs approved and the most often prescribed drugs in the United States have at least one asymmetric center [169]. Approximately half of these chiral drugs are of a racemic composition. Many of the optically pure drug substances are of natural origin, while the majority of the synthetically derived products are in racemic form [172]. Enantiomers can differ in their pharmacological activity or one may be inactive or... 

Tan s analysis of the first two components accounted for 84.2% of the original information, indicating that synthetic drugs and natural products show limited overlap of chemical space. 

Toxicological Sciences, the official SOT journal, is distributed monthly in print and electronically. The journal publishes premier peer-reviewed, hypothesis-driven, original research articles that are broadly relevant to assessing the potentially adverse health effects resulting from exposure of humans or animals to chemicals, drugs, natural products, or synthetic materials. Studies may involve experimental animals or human subjects, or they may focus on in vitro methods or alternatives to the use of experimental animals. Sections include original research, reviews, forum articles on policy or research issues, editorials, letters to the editor, and supplementary data guidelines. 

Table 3.2 Average number of chiral centers in synthetics, drugs and natural products. (Natural products are divided into subclasses related to their biological origin.)...

Fig. 9.1-7 Example of principle component analysis comparison of synthetic drugs and natural products. A set of 20 synthetic drugs, including the top 10 best-sellers in 2004, and 20 natural products was analyzed for nine molecular descriptors molecular weight, hydrophobicity (X log P or C log P), hydrogen-bond donors, hydrogen-bond acceptors, rotatable bonds, topological polar surface area [43], stereogenic centers, nitrogen atoms, oxygen atoms. PCA was used to reduce the nine-dimensional vectors to two-dimensional vectors, which were then replotted as shown. The first principal component accounts for 55.1% of the original information and the first two...

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