H. Piperidine Analogues of Phenyltropanes 967 III. Cocaine Analogues 969 A. Stereoisomers of Cocaine 970 B. Phenyl Ring Substituted Cocaines 970 C. 2â-Substituted Cocaines 973 1. 2â-Substituted Cocaines 973 2. 2â-Substituted 4′-Iodococaines 977 D. N-Modified Cocaines 978 E. 3â-Carbamoyl Analogues of Cocaine 981 F. 3â-Alkylphenyltropanes 982 G. 6/7-Substituted Cocaine and Pseudococaine 982 H. 6-...

This review will describe the recent advances in the synthesis of C-nucleosides with inhibitory activity of inosine monophosphate dehydrogenase (IMPDH), a key enzyme in the biosynthesis of guanine nucleotides. The review will cover synthetic approaches of structural analogues showing modifications in the furanose ring as well as in the heterocyclic base. Heterocyclic sugar nucleoside analogues ...

Natural product-derived drugs exemplified by quinine, isolated from South American Cinchona species and artemisinin discovered in China are of immense importance for the treatment of malaria. Although malaria parasites resistant to artemisinin have not yet been found in malaria patients, the need for new antimalarial agents remains. The burden of malaria is heaviest in Africa where over a milli...

Chronic kidney disease (CKD) is a common and costly medical condition, and currently available therapeutic options remain unsatisfactory. Vitamin D analogues are widely used for the bone and mineral disorder associated with CKD. However, accumulating evidence suggests that vitamin D analogues may have actions other than their effects on bone and mineral metabolism. In this article, we review th...

Novel N-α-haloacylated homoserine lactones, in which a halogen atom was introduced at the α-position of the carbonyl function of the N-acyl chain, have been studied as quorum sensing (QS) modulators and compared with a library of natural N-acylated homoserine lactones (AHLs). The series of novel analogues consists of α-chloro, α-bromo and α-iodo AHL analogues. Furthermore, the biological QS act...

UDP-glucose 4-epimerase from Saccharomyces fragilis has 1 mol of NAD firmly bound per mol of the dimeric apoenzyme. This prevents a direct study of the coenzyme binding site of the protein. Dissociation of the dimer with p-chloromercuribenzoate and its reconstitution with exogenous NAD or one of its analogues and 2-mercaptoethanol provides an indirect method of study of the site. Depending on t...

On their plasma membranes, cells express receptor proteins with high affinity for regulatory peptides, such as somatostatin. Changes in the density of these receptors during disease, for example, overexpression in many tumors, provide the basis for new imaging methods. The first peptide analogues successfully applied for visualization of receptor-positive tumors were radiolabeled somatostatin a...

We report the first detailed study on the ubiquinone (coenzyme Q; abbreviated to Q) analogue specificity of mitochondrial complex I, NADH:Q reductase, in intact submitochondrial particles. The enzymic function of complex I has been investigated using a series of analogues of Q as electron acceptor substrates for both electron transport activity and the associated generation of membrane potentia...