Trehalase inhibitors enzymes

Also, thiazolidine derivatives have been reported to control an insect s energy metabolism through the inhibition of trehalase, an enzyme involved in the energy functions, especially in the insect-flight [217,218]. The affinity of trehazolin (a) for this enzyme has motivated workers to explore 2-aryl-iminothiazolidine/oxazolidine derivatives (comp, b. Fig. 37, Table 26) as its inhibitors [219]. 

The chemical synthesis of derivatives and emalogs has long coimnanded much interest, as such compounds are required for the study of structure—activity relationships in the action of trehalases (23,28), may serve as substitutes for 51 in the synthesis of cord-factor analogs to be used as probes in the field of mycobacterial biochemistry (29, 30), and could possibly prove to possess interesting properties as enzyme inhibitors or antibiotic agents. 

Richardson s interest in these trehalose epoxides stemmed from his desire to prepare a wide range of modified trehalose analogues for evaluation as inhibitors of the trehalase of insects, as trehalose is known to be the storage carbohydrate of many insects and good inhibitors of this processing enzyme could potentially function as green insecticides. 

In the early days of this Advances series, authors were offered the opportunity to record experimental procedures as part of their contributions, but this has been rarely used in recent years. However, the practice is revived here in the article by El Nemr and El Ashry (Alexandria) on the synthesis of trehazolin, a natural nitrogen-containing pseudodisaccharide that is an inhibitor of the enzyme trehalase, together with various analogues. These synthetic targets can be approached in a wide variety of ways, and the authors present for each synthetic sequence sufficient detail to permit an experienced synthetic chemist to repeat the procedure. 

The intestinal oligo- and disaccharidases are fixed components of the cell membrane of the brush border region of the wall of the small intestine. These enzymes digest dietary carbohydrate to monosaccharides which are absorbed through the intestinal wall. They include sucrase, maltase, isomaltase, lactase, trehalase, and hetero-p-glucosidase. In the late 1970s, it was realized that inhibition of all or some of these activities could regulate the absorption of carbohydrate, and that these inhibitors could... 

The presence of trehalase in the tubercle bacillus was discovered by Bloch and SuUman in 1945. Optimal hydrolysis of a,a-trehalose by the enzyme occurred in acid to neutral solutions. Since a,a-trehalose is not utilized by the bacteria so rapidly as is n-glucose, it was inferred that the bacillus only metabolizes the a, -trehalose after the trehalase has converted it into D-glucose. Trehalosamine (see p. 220) has an antimycobac-terial effect. This effect is antagonized by a,a-trehalose. One mole of trehalosamine as inhibitor removes 0.337 mole of Q ,a-trehalose from the surface of the enzyme. Total inhibition of mycobacterial trehalase is not readily produced. Cord factor was also isolated from wax D of a BCG strain of M. tuberculosis in 1959 by Nojima. A list of fatty acid esters of a, a-trehalose is given in Table I. 

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