Joining metals and antibiotics: Studies towards a general method for the synthesis of β-lactams that have a metal complex moiety attached to the C3-position are reported (see scheme). The cis/trans selectivity of the reactions ranges from low in complexes containing the alkyne moiety joined directly to the cyclopentadienyl ring to complete when the metal moiety is separated from the reactive alkyne by an alkynyl-aryl fragment.

Towards a General Synthesis of 3‐Metal‐Substituted β‐Lactams

Introduction: Nowadays the use of antihistamines (AH) is increasing steadily. These drugs are able to act on a variety of pathological conditions of the organism. A number of computer-aided (in silico) approaches have been developed to discover and develop novel AH drugs. Among these methods stand the ones based on drug-receptor docking, thermodynamics, as well as the quantitative structure–activity relationships (QSAR). Areas covered: This review collates the most recent advances in the use of computer approaches for the search and characterization of novel AH drugs. Within the QSAR methods, particular attention will be paid to those based on molecular topology (MT) because of their demonstrated efficacy in discovering new drugs. Collateral topics will also be dealt with including: docking studies, thermodynamic aspects, molecular modeling and so on. These issues will be treated to the extent that they have interest as complementary to QSAR-MT. Expert opinion: Given the importance of the use of AHs, the ...

Advances in the molecular modeling and quantitative structure–activity relationship-based design for antihistamines

Doxylamin, Diphenhydramin und Dimenhydrinat sind Antihistaminika der ersten Generation, die in der Lage sind, die Blut-Hirn-Schranke zu uberwinden und zentral gelegene H1-Rezeptoren anzugreifen. Sie wirken daher nicht nurperipher antiallergisch, sondern auch zentral sedierend und – auser Doxylamin, auch antiemetisch. In der Selbstmedikation spielen diese H1-Antihistaminika als rezeptfreie Schlafmittel eine grose Rolle; haufig wird aber zu wenig darauf geachtet, dass sie mit zahlreichen anderen Arzneimitteln teils schwerwiegende Interaktionen auslosen konnen und ihre Anwendung haufig kontraindiziert ist.

H1‐Antihistaminika der ersten Generation. Problemlos in der Empfehlung?

Gegen die beste Waffe Gram-negativer Bakterien gegen β-Lactam-Antibiotika, die β-Lactamasen, war bisher kein Suizid-Inhibitor uneingeschrankt erfolgreich. Wahrend sich β-Lactamasen vom Serin-Protease-Typ, der weitaus groseren Gruppe der β-Lactamasen, wenigstens mittels Clavulansaure, Sulbactam und Tazobactam hemmen liesen, so konnen diese, aber auch Carbapenem und Imipenem, die Lactam-Hydrolyse durch die Metallo-β-Lactamasen nicht mehr verhindern.

Neue Waffe gegen β-Lactamasen?

Bakterien wehren sich gegen Antibiotika, indem sie entweder den Zielort fur das Antibiotikum durch Mutation in der Aminosaurestruktur strukturell verandern, den Zugang in die Bakterienzelle fur das Antibiotikum versperren oder gar das Antibiotikum chemisch vernichten.

Kleine Änderung, große Wirkung – ein neues Vancomycin‐Derivat gegen MRSA

Will ein HI-Virus in eine Wirtszelle eindringen, so benotigt es sowohl einen CD4-Rezeptor, als auch einen der beiden Chemokin-Rezeptoren auf der Seite der Wirtszelle. Von den Chemokin-Rezeptoren CXCR4 und CCR5 (= C-chemokine rezeptor 5) spielt aber nur Letzterer bei der eigentlichen Ubertragung und im fruhen Stadium der Erkrankung eine Rolle.

RANTES‐Protein schützt Affen vor Infektion mit chimären AIDS‐Viren

Am 23. Oktober 2009 hat die Food and Drug Administration (FDA) auf Empfehlung des Centers for Disease Control (CDC) den Neuraminidaseinhibitor (NAI) Peramivir im Rahmen einer “Emergency Use Authorization” (EUA) zur Behandlung der 2009-H1N1-Influenza (“Schweinegrippe”) in den USA zugelassen. Nach Oseltamivir (oral) und Zanamivir (inhalativ) steht nun mit Peramivir der erste NAI zur parenteralen Gabe zur Verfugung.

Notfallzulassung von Peramivir in den USA

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