Pharmacologically active molecules

The AT-acyliminium methodology has been exploited to prepare pharmacologically active molecules, e.g., GW 311616A [82] and inhibitors of the... 

Mirkin B.L., Singh S., Placental transfer of pharmacologically active molecules. In Mirkin B.L., ed., Perinatal Pharmacology and Theraputics. New York, Academic Press, 1976, 1-69. 

An alternative method for assessing cell layer integrity is through the use of hydrophilic paracellular transport markers (e.g., radiolabeled D-mannitol or fluorescein-Na+), which passively traverse cells by the paracellular route. Small amounts of compound required for in vitro conjunctival cell culture transport experiments make this approach well suited for screening purposes. Relative absorption index of a series of pharmacologically active molecules can be ranked against known markers for the identification of candidates with potential absorption problems, which is a reliable tool to select drug candidates with optimal characteristics. 

What has been achieved until now In the year 2001, several liposome and antibody based strategies have been or will soon be approved for clinical application, some for the treatment of cancer, some for the treatment of bacterial infections, some for chronic inflammatory diseases. Furthermore many monoclonal antibodies without a drug or pharmacologically active molecule attached are in the clinic. Their intrinsic targeting and effector function is obviously sufficient for the pharmacological effect. 

A large number of pharmacologically active molecules that have found clinical use have been synthesized through the derivatization of quinolines, while others are simply quinoline analogs. Some of the most recent studies of quin-doline analogs in relation to anticancer activity were discussed above. 

The in vitro studies have shown that iV-(4-fluorobenzyl)spiperone 320 has high affinity for the dopamine D2 receptor and low affinity for the serotonin 5-HT2 receptor311. [18F]-319 can be used for incorporating 18F into a pharmacologically active molecule possessing an N atom with a certain degree of bulk-tolerance. 

Fig. 1 The 3D vision of pharmacologically active molecules (here taxol) provides the medicinal chemist with a complex information from which a pharmacophore has to be deduced to generate analogs with more adequate pharmocokinetic and toxicological properties.

A study of the metabolic fate of a drug is required for all new drug products. Often it is found that the metabolites arc also active. Indeed, sometimes the metabolite is the pharmacologically active molecule. The.sc drug metabolites cun provide leads for additional investigations of potentially new products. Examples of an inactive parent drug that is converted to an active metabolite include the nonsteroidal anti-... 

Parrot-Lopez, H., Djedaini, E, Perly, B. et al. An approach to vec-torization of pharmacologically active molecules the covalent binding of Leuenkephalin to a modified (3-cyclodextrin. Tetrahedron Lett. 1990, 31,1999-2002. 

Enzymes as therapeutic products are not only very diverse but also very complex. They are proteins, a large group of pharmacologically active molecules that also includes monoclonal antibodies, cytokines, growth factors, hemostatic and thrombostatic agents, and vaccines. 

Of equal interest are proteins of the cytoskeleton that serve structural roles (e.g. tubulin), or those involved in transport processes. For example, many drugs act indirectly by releasing, or preventing the release, of pharmacologically active molecules (e.g. neurotransmitters) concentrated... 

The well-characterized microorganisms represent only a small fraction of the microbial diversity in the environment. Natural microbial communities are considered an important and innovative source of new pharmacologically active molecules, novel molecular templates for combinatorial chemistry as well as of new biocatalysts. 

The pharmacologically active molecule or drug entity must be synthesized, isolated or extracted from various possible sources (relying on the disciplines of medicinal chemistry, pharmacology, and toxicology). 

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