Physiologically-active substances

The stimulus for the recent surge of activity in this previously dormant area of organic chemistry can be traced to the prostaglandin connection . That is to the discovery that saturated bicyclic peroxides are key intermediates in the biosynthesis of prostaglandins and other physiologically active substances by the enzymatic oxygenation of polyunsaturated fatty acids. 

Andreev, R.V. Borodkin, G.I. Shubin, V.G. Book of Abstracts of the 2nd International Conference on Natural Products and Physiologically Active Substances (ICNPAS-2004) and 3rd EuroAsian Heterocyclic Meeting Heterocycles in Organic and Combinatorial Chemistry" (EAHM-2004), Novosibirsk, Russia, September 12-17,2004, p 131. 

Enantiomerically pure trifluoromethyl- and trifluoroethylcyclopropylcarbi-nols 132 and derivatives (R=Ci 2 fluoroalkyl, alkyl, aryl) appeared useful as intermediates for enzyme inhibitors, physiological active substances and anti-tumoral agents, Eq. (53), [183]. 

More recently experiments in the field of immunology and cancer research have shown that several polysaccharides are very promising nontoxic products. This has opened a completely new horizon for their applications as direct physiologically active substances. Compared to other applications in industry, the percentage of polysaccharides actually used for pharmaceutical purposes is rather low (Table 1). 

Content of physiologically active substance in the polymer, mg/g Heparin 1.9 Heparin 3.2 + trypsin 0.5 Heparin 1.5 + trypsin 1.6... 

Polymers modified with two co-immobilized physiologically active substances may... 

The purpose of the present paper is to compare the toxicity and pharmacology of saturated compounds with their unsaturated analogs (wherever possible) and to list some important, physiologically active substances, bearing one or more double bonds. 

The active site structure of trypsin-like enzymes is considered to be very similar to that of bovine trypsin, yet little is known about them. Refinement of these structures is important also for the purpose of designing physiologically active substances. With a view to comparing the spatial requirements of active sites of these enzymes, dissociation constants of the acyl enzyme-ligand complex, K-, which were defined before, were successfully analyzed By taking advantage of inverse substrates which have an unlimited choice of the acyl component, development of stable acyl enzymes could be possible. These transient inhibitors for trypsin-like enzymes could be candidates for drugs. In this respect, the determination of the deacylation rate constants for the plasmin- and thrombin-catalyzed hydrolyses of various esters were undertaken 77). 

Recent advances in molecular and cell biology have shown that adipose tissue not only stores excess energy in the form of fat, but also secretes physiologically active substances called adipocytokines (Matsuzawa et al., 1999). In obesity, adipocytes (cells of adipose tissues) are increased and enlarged, and they secrete excessive amounts of inflammatory adipocytokines, such as tumor necrosis factor-alpha (Hotamisligil et al., 1993) and monocyte chemoattractant protein-1 (Sartipy and Loskutoff, 2003). This induces type-2 diabetes, such as... 

Various authors (1996) Symposium proceedings physiologically active substances in plant foods. Proceedings of the Nutrition Society 55, 371-446. 

Of physiologically active substances isolated from marine sources, the pyrroloimino-quinone alkaloids family exhibits antitumor activities derived from the unique highly-fused structure. The first synthesis of discorhabdin C (127) was performed by means of an electrochemical method as a key step . The key substrate 128, efficiently prepared starting from 4,4-dimethoxy-5-nitrobenzaldehyde, was submitted to constant current electrolysis (3 mA 4-1.2-1.8 V vi. SCE) in anhydrous MeCN to give rise to discorhabdin C in 24% yield, together with a minor compound 129 (6%) (Scheme 24). After a while, discohabdin C was also synthesized by using PhI(OCOCF3)2-promoted oxidation as a key step. ... 

PAH compoimds. The most studied PAH is benzo[fl]pyrene, which is a physiologically active substance that can contribute to the development of cancer in human cells. 

P.V. Sergeev and N.L. Shimanovskii, Receptors of Physiologically Active Substances Meditsina, Moscow, 1987 (in Russian ). 

Thus we have a continuous number of phenomena in which structural correspondence plays an important part, these phenomena belonging to different fields of science to crystal chemistry, to the science of alloys, to epitaxy, to stereospecific adsorption, to heterogenous catalysis, to enzyme reactions, to antimetabolites, to the action of physiologically active substances and to a number of other biochemical agents, as well as to immunology. Similar views were recently expressed by Seifert concerning epitaxy [16). 

A. Miyawaki, H. Date, and Y. Kobayashi, Biosensor with Immobilized Physiologically Active Substances [in Japanese]. Jpn. Kokai Tokkyo Koho, Pat. No. 8603047 (1986). 

Rosazza, J.P. Microbial Transformations of Physiologically Active Substances, CRC Press Boca Raton, FL, 1982. 

---