Examples of biologically active

Scheme 9.24. Examples of biologically active Biginelli products.

The above examples of biological activities of nitric oxide and peroxynitrite are of course just a small part of publications in this field. Although both nitrogen compounds can act as... 

Scheme 9. Selected examples of biologically active benzonitriles...

Fig. 32.10 Examples of biologically active compounds obtainable through BINAP-Ru-catalyzed hydrogenation of/ -keto esters.

Fig. 32.44 Examples of biologically active compounds and a chiral ligand obtainable through hydrogenation of simple ketones catalyzed by BINAP/chiral diamine-Ru complexes.

Ring systems 63-74 have attracted much attention from medicinal chemists, and examples of biological activities for a large range of new derivatives have been published for several of these systems since 1995. A selection of these is presented below. 

A particular dimer of thymine was the first heat-stable photoproduct isolated from photolysis of nucleic acid derivatives, and still appears to be the principal isolable product from photolysis of most examples of biologically active DNA.8,10 Investigation of this product has drawn much attention in recent years. Most of this work has been carried out on polynucleotides and nucleic acids and will be dealt with in those sections. The remaining work has been largely carried out with... 

Figure 1.12. Examples of biologically active compounds obtainable via BINAP-Ru catalyzed hydrogena -tion of difunctionalized ketones.

Figure 1.16. Examples of biologically active compounds and chiral diphosphines obtainable viaBINAP-Ru catalyzed hydrogenation through dynamic kinetic resolution.

The vancomycin mimics, 7, discussed above are an important example of biologically active calix[4]arene derivatives. In this case the whole macrobicy-clic structure including the calixarene skeleton with its cavity seems to be important for the pharmacological effect. In the following sections we discuss derivatives in which the calixarene serves more or less as an easily available scaffold for the assembly of biologically relevant fragments such as peptides or carbohydrates. 

Figure 4 Examples of biologically active natural products synthesised using supported reagents...

Figure 3 Three examples of biologically active oligomers discovered from screening peptoid and oiigocarbamate combinatorial libraries...

Figure 13 Four examples of biologically active compounds discovered from libraries based on the tetrahydro-P-carboline natural product privileged scaffold...

Examples of biologically active aryl chlorides— the drugs bupropion and chlorpheniramine, and 2,4-D and 2,4,5-T, herbicide components of the defohant Agent Orange (Section 18.3)... 

The 1-phenylpyrazole core has been shown to bestow pharmacological activity in a number of areas in the pharmaceutical and agrochemical industries. In the latter field, select examples of biological activities include insecticidal, miticidal, and herbicidal. More specifically, 1-phenylpyrazoles with alkyl, acyl, thioalkyl, or cyano substituents at the 4-position exhibit potent insecticidal activity. In particular, 5-amino-I-(2,6-dichloro-4-trifluoro-methylphenyl)-4-trifluoromethanesulfinyl-l//-pyrazole-3-carbonitrile (Fipronil ) is one of the most commercially successful insecticides. In fleas, ticks, and other arthropods, it acts as a gamma-aminobutyric acid (GABA)-gated... 

FIGURE 9.18 Examples of biologically active sugar-related natural products with nitrogen in the ring. 

Figure 11.2 Examples of biologically active heteroaromatic systems.

The first example of biologically active gem-di (1 uorocyciopropanc derivative was reported in 1986 by Johnson and his co-workers [5a], Halogen-substituted analogues of DDT-... 

Figure 12.6 Examples of biologically active gem-difluorocyclopropanes (simple molecules).

Although benzopiperazinones (l,2,3,4-tetrahydroquinoxalin-2-ones) are structurally related to benzodiazepines, their use in drug discovery is less well established. Examples of biological activity of benzopiperazinones include their action as inhibitors of aldose reductase [208], as partial agonists of the y-aminobutyric acid (GABA)/benzodiazepine receptor complex [209, 210], and as angiotensin II receptor antagonists [211]. In addition, derivatives with antiviral acti vity associated vfith HIV have been reported [212, 213]. 

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