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5944 2.4. Other Attachment Methods 5945 2.4.1. Sonogashira Coupling 5945 2.4.2. Other Methods for Labeling the C-Terminus 5946 2.4.3. Other Methods for Labeling the N-Terminus 5947 2.4.4. Labels for the Thiol Group in Cysteine 5947 2.4.5. Miscellaneous 5947 2.5. Application of Ferrocene Compounds in Peptide Synthesis 5948 2.5.1. The Ferrocenylmethyl (Fem) Group as a Protecting Group 5948 2.5.2. Peptide Synthesis via Four-Component Reactions with Ferrocene Alkylamines 5949 3. Conjugates of Ferrocene with Proteins 5950 3.1. Redox Proteins 5950 3.1.1. Glucose Oxidase (GOD) 5950 3.1.2. D-Amino Acid Oxidase (DAAO) 5953 3.1.3. Cytochrome P450 cam 5953 3.1.4.

This review provides an introduction into the fascinating area of organometallic anticancer compounds. Although the subject dates back many years, it has witnessed considerable growth only in the past decade. A brief overview of the subject together with recent pertinent examples is provided. The properties of organometallic compounds that lend themselves to medical applications, the main current approaches used, and possible avenues for future research are identified.

Short antimicrobial peptides rich in arginine (R) and tryptophan (W) interact with membranes. To learn how this interaction leads to bacterial death, we characterized the effects of the minimal pharmacophore RWRWRW-NH 2 . A ruthenium-substituted derivative of this peptide localized to the membrane in vivo, and the peptide also integrated readily into mixed phospholipid bilayers that resemble Gram-positive membranes. Proteome and Western blot analyses showed that integration of the peptide caused delocalization of peripheral membrane proteins essential for respiration and cell-wall biosynthesis, limiting cellular energy and undermining cell-wall integrity. This delocalization phenomenon also was observed with the cyclic peptide gramicidin S, indicating the generality of the mechanism. Exogenous glutamate increases tolerance to the peptide, indicating that osmotic destabilization also contributes to antibacterial efficacy. Bacillus subtilis responds to peptide stress by releasing osmoprotective amino acids, in part via mechanosensitive channels. This response is triggered by membrane-targeting bacteriolytic peptides of different structural classes as well as by hypoosmotic conditions. mechanism of action | respiratory chain | hypoosmotic stress response | metallocenes

Organometallic complexes have unique physico-chemical properties, which have been widely used in homogenous catalysis, for example, for the synthesis of lead compounds and drug candidates. Over the past two decades, a few scientists from all over the world have extended the use of the specific characteristics of these compounds (e.g. structural diversity, possibility of ligand exchange, redox and catalytic properties) for medicinal purposes. The results are stunning. A few organometallic compounds have already entered clinical trials and it can be anticipated that several more will follow in coming years. In this short review, we present the specific advantages that organometallic metal complexes have over purely organic and also coordination compounds. Furthermore, using specific examples, we illustrate how these particular properties can be put to good use in medicinal chemistry. The examples we present have an emphasis on, but are not restricted to, anti-cancer activity.

Ferrocene peptide conjugates display an array of structural features including helical ferrocene based chirality and a number of different intramolecular hydrogen bonding patterns. In this tutorial review we present a rigorous nomenclature for these systems, followed by a section that summarises and categorises the structures known to date. The issues discussed herein are of general relevance for all metallocene-based chiral transition metal catalysts and peptide turn mimetics.

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The emergence of bacterial resistance to commercial antibiotics is an issue of global importance. During the last two decades, the number of antibacterial agents that have been discovered and introduced into the market has steadily declined and failed to meet the challenges posed by rapidly increasing resistance of the pathogens against common antibacterial drugs. The development of new classes of compounds to control the virulence of the pathogens is therefore urgently required. This perspective describes the historical development in brief and recent advances on the preparation of small organometallic compounds as new classes of antibacterial agents with potential for clinical development. ABSTRACT.The emergence of bacterial resistance to commercial antibiotics is an issue of global importance.During the last two decades, the number of antibacterial agents that have been discovered and introduced into the market has steadily declined and failed to meet the challenges posed by rapidly increasing resistance of the pathogens against common antibacterial drugs. The development of new classes of compounds to control the virulence of the pathogens is therefore urgently required. This perspective describes the historical development in brief and recent advances on the preparation of small organometallic compounds as new classes of antibacterial agents with potential for clinical development. 3Introduction.