Search results
Search for "antibacterials" in Full Text gives 9 result(s) in Beilstein Journal of Organic Chemistry.
On drug discovery against infectious diseases and academic medicinal chemistry contributions
Beilstein J. Org. Chem. 2022, 18, 1355–1378, doi:10.3762/bjoc.18.141
- the recurrent paucity of useful/exploitable results reported. This is followed by the successful hit to lead stories leading to recent and original antibacterials which are, or about to be, used in human medicine. Then, illustrated considerations and suggestions are made on the possible inputs of
- considering the results of academic as well as industrial screening campaigns. Keywords: antibacterials; frequent hitters; hit to lead chemical library; medicinal chemistry; virtual docking; Introduction The current state of affairs in the academia and two problems for medicinal chemists Across the world
- dealing with many aspects of medicinal chemistry such as “new screening paradigms, computational approaches, novel synthetic chemistry, gene family screening, investigating routes of delivery and so on” [108]. Hit to lead, recent success stories in antibacterials Past this essential point, which again
One-pot synthesis of oxazolidinones and five-membered cyclic carbonates from epoxides and chlorosulfonyl isocyanate: theoretical evidence for an asynchronous concerted pathway
Beilstein J. Org. Chem. 2020, 16, 1805–1819, doi:10.3762/bjoc.16.148
- considerable use as antibiotics [1], immunomodulators [2], antibacterials [3], as well as synthetic intermediates and chiral auxiliaries for various organic conversions [4][5][6][7]. Linezolid [1][2][3] (3) and cytoxazone [8][9] (4) are oxazolidinone derivatives having significant biological activities
Chemical synthesis of tripeptide thioesters for the biotechnological incorporation into the myxobacterial secondary metabolite argyrin via mutasynthesis
Beilstein J. Org. Chem. 2019, 15, 2922–2929, doi:10.3762/bjoc.15.286
- , cytotoxicity and antibiotic activity, the selectivity profile of this class of compounds should be considered for optimization of future antibacterials. The first total synthesis was reported by Ley and co-workers [14] for argyrin B in 18 linear steps, followed by an alternative strategy towards argyrin F (6
One-pot activation–alkynylation–cyclization synthesis of 1,5-diacyl-5-hydroxypyrazolines in a consecutive three-component fashion
Beilstein J. Org. Chem. 2019, 15, 1360–1370, doi:10.3762/bjoc.15.136
- –15.2 μM (Figure 1) [23]. 1-Acyl-5-hydroxypyrazolines have been shown to be analgesics with a slightly improved pain-relieving efficacy than Aspirin® [24][25], and 5-nitro-2-furyl-substituted derivatives are active antibacterials against the strains S. aureus, A. aerogenes, E. coli and B. subtilis
Protein–protein interactions in bacteria: a promising and challenging avenue towards the discovery of new antibiotics
Beilstein J. Org. Chem. 2018, 14, 2881–2896, doi:10.3762/bjoc.14.267
- in both Gram-positive and Gram-negative microorganisms, findings that could be of value in the development of optimized antagonists for potential use as antibacterials. N-Utilization substances (Nus) B and E Another point of therapeutic intervention to develop new anti-infectives that target cell
Synthesis of a leopolic acid-inspired tetramic acid with antimicrobial activity against multidrug-resistant bacteria
Beilstein J. Org. Chem. 2018, 14, 2482–2487, doi:10.3762/bjoc.14.224
- , Università degli Studi di Milano, via Celoria 10, I-20133 Milano, Italy 10.3762/bjoc.14.224 Abstract The increasing emergence of multidrug-resistant pathogens is one of the biggest threats to human health and food security. The discovery of new antibacterials, and in particular the finding of new scaffolds
Reactions of nitroxides 15. Cinnamates bearing a nitroxyl moiety synthesized using a Mizoroki–Heck cross-coupling reaction
Beilstein J. Org. Chem. 2015, 11, 1155–1162, doi:10.3762/bjoc.11.130
- ][6], simple cinnamic acid derivatives (esters, amides, etc.), and prenylated cinnamates [4], have been proved to be effective as antioxidants [2][7], radical scavengers [2], antimicrobials [2][7][8], antibacterials [2], antivirals [2][7], and fungicides [2][7][8]. Cinnamic derivatives have also been
Binaphthyl-anchored antibacterial tripeptide derivatives with hydrophobic C-terminal amino acid variations
Beilstein J. Org. Chem. 2012, 8, 1265–1270, doi:10.3762/bjoc.8.142
- and Enterococci (VRE, VSE), and against Staphylococcus epidermidis. Keywords: antibacterials; binaphthyls; cationic peptides; peptides; resistance; VISA; VRE; Introduction Among the most pressing challenges in current healthcare is the resistance of bacterial human pathogenic organisms to
- /mL [6]), which show significant promise as antibacterials [6][7][8]. In the development of these antibacterials, it became apparent that the nature of the C-terminal amino acid derivative was significant, with indications that the hydrophobic groups at the terminus (Figure 1, group B) [6] and at the
New acylides: synthesis of 3-O-[γ-(4-oxo-2-aryl- thiazolidin- 3-yl)butyryl]erythromycin A derivatives
Beilstein J. Org. Chem. 2008, 4, No. 14, doi:10.3762/bjoc.4.14
- been the most important approach for the development of novel antibacterials active against resistant strains of bacteria. Further structural modifications on decladinosylmacrolides have resulted in the identification of ketolides such as telithromycin (Aventis) [5] and cethromycin (Abbott) [6][7], and
- molecule may be advantageous for antibacterial activity in view of similar system having been reported as antibacterials [10][11]. The thiazolidin-4-ones can be generated under very mild conditions using the DCC mediated one-pot synthesis reported by us [12]. Results and Discussion Decladinosyl-6-O
Other Beilstein-Institut Open Science Activities
