Biologically active drug

Pyrrolo[l,2-A]thiazoles are aromatic compounds but only one fully conjugated derivative has been described. A few dihydro and tetrahydro derivatives have been prepared, mainly in connection with search for biologically active drugs. Saturated compounds are also known. 

Some synthetic macromolecules have shown intrinsic anticancer activity. Their mechanism of action is probably either the direct action upon the tumor cell, or the stimulation of the host s immune system [59] (Table 2). We do not exclude the use of such macromolecules as drug carriers in the future. However, the combination of a biologically active carrier with a biologically active drug makes the evaluation of the structure-property relationships more difficult. 

Key words High-throughput chemistry, chemical library, random library, targeted library, optimization library, library design, biological activity, drug discovery. 

Bambermycin is an antibiotic that, because of its heteropolar behavior, tends to form complexes. It is, therefore, a compound that is extremely difficult for animals to absorb. Balance studies proved that bambermycin is not absorbed but is excreted in the feces as tire intact, biologically active drug. As a result, no withdrawal period is required. 

Continuing research on sulfamidochrysoidine revealed that sulfanilamide (1.21), a metabolite of sulfamidochrysoidine, was the active antibacterial compound (Figure 1.9). Compounds that are chemically altered in the body to form the biologically active drug are called prodrugs.1... 

According to the recommendations, in quantitative measurements of biological activity drug action is expressed in terms of the effect, E, produced when an agonist, A, is applied at a concentration [A]. The relationship between E and [A] can often be described empirically by Hill s equation, which has the form ... 

Schuffenhauer A, Brown N. Chemical diversity and biological activity. Drug Disc. Today Technol. 2006 3 387-395. 

Yolles, S. Leafe, T. Ward, L. Boettner, F. Controlled release of biologically active drugs. Bull. Parent. Drug Assoc. 1976, 30 (6), 306-312. 

Kubinyi, H. (1979). Lipophilicity and Biological Activity. Drug Transport and Drug Distribution in Model Systems and Biological Systems. ArzneirruForsch., 29,1067-1080. 

Kubinyi H. Lipophilicity and biological activity drug transport and drug distribution in model systems and in biological systems. Arzneim-Forsch (Drug Res) 1979 29 1067-1080. 

A probable hypersensitivity pneumonitis secondary to inhaled aerosolized coUstin has been reported in a 68-year-old Indian woman who was successfully treated for a nosocomial pneumonia due to a multidrug-resistant Acinetobacter baumarmii [100 ]. The authors postulated that the hypersensitivity pneumonitis was due to conversion of the prodrug, colistimethate, to the biologically active form of colistin, which is less well tolerated. They recommended ensuring that the prodrug is only reconstituted just before administration to avoid excessive conversion to the biologically active drug. 

A number of examples of the synthesis of polymerizable drug derivatives have been reported which are beyond the scope of this article. Hovrever, it should be borne in mind that in most cases, simply the introduction of the polymerizable group into a drug molecule is not sufficient to produce a biologically active drug conjugate. The drug must be separated from the polymer chain by a spacer and practically this may turn out to be a difficult synthetic operation. 

It is an unfortunate but immutable fact that no biologically active drug is free from the possibility of causing adverse reactions in certain individuals who are genetically and/or environmentally susceptible. 

EM. Veronese, L. Sartore, P. Orsolini, R. Deghenghi, Biologically active drug polymer derivatives and method for preparing the same, U. S. Patent 5286637, assigned to Debiopharm S.A. February 15,1994. 

The NHK reaction has also been reported in the syntheses of biologically active drug candidates such as analogues of laulimalide and epitholine B. 

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