Cover Picture: 2,4,5‐Trinitroimidazole‐Based Energetic Salts (Chem. Eur. J. 14/2007)

Abstract

Wabenstrukturen infolge N2‐Fixierung: Der VIII‐Bis(neopentyl)‐Komplex [(PNP)V(CH2tBu)2] (PNP=N[4‐Me‐2‐(PiPr2)C6H3]2−) dient als Baustein für terminale VV‐Alkyliden‐Komplexe, wenn er mit Zweielektronenoxidantien wie N2CPh2, O2−‐Quellen wie OPPh3 oder N2O oder Sulfid‐Quellen wie S8 oder SPPh3 umgesetzt wird. Das vermutliche VIII‐Alkyliden‐Intermediat, [(PNP)V(CHtBu)], kann auch N2 aktivieren und bildet dann entlang der N2‐Einheiten wabenförmige Anordnungen (siehe Bild).

Indole/isatin‐containing hybrids as potential antibacterial agents

“…[ 48,49 ] Azole derivatives could exhibit the antibacterial activities via diverse mechanisms of action such as inhibition of DNA gyrase, topoisomerase IV, and efflux pumps, and they possess promising antibacterial activities against both drug‐sensitive and ‐resistant pathogens. [ 6,50 ] Moreover, several azole‐based drugs such as cefazolin, cloxacillin, linezolid, and tedizolid have already been used in clinics for the treatment of various bacterial infections, even those caused by drug‐resistant pathogens. [ 51,52 ] Accordingly, hybridization of indole/isatin with azole has the potential to retain antibacterial activity, and it may provide novel antibacterial candidates with enhanced activity against both drug‐sensitive and ‐resistant organisms.…”

“…[ 1,2 ] Antibiotics play indispensable roles in the treatment of bacterial infections, but the frequent and inappropriate application of antibiotics contributes to the fast spread of antibiotic resistance, which results in the reduced effectiveness of empiric antimicrobial treatment. [ 3–6 ] Antibiotic resistance has been considered as an alarming concern in Europe (59%), followed by Southeast Asia (18%), Western Pacific (12%), the Americas (6%), and Africa (6%), and over 700,000 deaths occur annually worldwide due to antibiotic resistance. [ 7,8 ] Thus, drug‐resistant bacteria have already posed a serious threat to human health, and it is imperative to deliver potent and novel antibacterial drug candidates.…”

Recent advances in indole dimers and hybrids with antibacterial activity against methicillin‐resistant Staphylococcus aureus

“…[ 59,60 ] Moreover, several azole‐containing agents that are exemplified by linezolid and tedizolid have already been used in clinics for the treatment of infections caused by drug‐resistant pathogens including MRSA. [ 61,62 ] Accordingly, hybridization of indole with azole pharmacophore represents a promising strategy to provide novel antibacterial candidates with an enhanced activity against both drug‐sensitive and drug‐resistant organisms.…”

“…[59,60] Moreover, several azole-containing agents that are exemplified by linezolid and tedizolid have already been used in clinics for the treatment of infections caused by drug-resistant pathogens including MRSA. [61,62] were active against MRSA, and among them, five hybrids, 28a,b (MIC: 1.0 µg/ml), 29a,b (MIC: 1.0 µg/ml), and 30a (MIC: 0.5 µg/ml), were 8-to 32-fold more potent than clinafloxacin (MIC: 16 µg/ml) and norfloxacin (MIC: 8.0 µg/ml). [63] In particular, hybrid 29a could effectively prevent the development of bacterial resistance, and the mechanistic study indicated that this hybrid could not only intercalate into MRSA DNA, but it could also permeate the MRSA membrane and bind with penicillin-binding protein 2a (PBP2a), and then decrease the expression of three relevant genes in MRSA.…”

Synthesis of 1,5‐Disubstituted Tetrazole−Indolizine Bis‐Heterocycles and Their Copper (II) Recognizing Properties

“…They are considered as a privileged scaffolds in medicinal chemistry and are often used in modern drug discovery processes [1,2] . Some examples of their biological activity include antibacterial, [3] antifungal, [4] anticancer, [5] antiviral, [6] antioxidant, [7] anti‐inflamatory [8] and as antitubercular [9] (Figure 1). In the field of material science, both 1,5‐DS‐T and indolizines have shown interesting properties as fluorescent sensors, materials and/or bioprobes [10] .…”