Actinomycetes: A Never-Ending Source of Bioactive Compounds—An Overview on Antibiotics Production

D De Simeis, S Serra - Antibiotics, 2021 - mdpi.com
The discovery of penicillin by Sir Alexander Fleming in 1928 provided us with access to a
new class of compounds useful at fighting bacterial infections: antibiotics. Ever since, a …

Bacterial resistance: Antibiotics of last generation used in clinical practice and the arise of natural products as new therapeutic alternatives

RCG Corrêa, SA Heleno, MJ Alves… - Current …, 2020 - ingentaconnect.com
Bacterial resistance to therapeutical drugs has been a serious issue over the last decades.
In fact, the quick development of resistance mechanisms by the microorganisms has been …

Total Synthesis of Tiacumicin B: Implementing Hydrogen Bond Directed Acceptor Delivery for Highly Selective β‐Glycosylations

S Norsikian, C Tresse, M François‐Eude… - Angewandte …, 2020 - Wiley Online Library
A total synthesis of tiacumicin B, a natural macrolide whose remarkable antibiotic properties
are used to treat severe intestinal infections, is reported. The strategy is in part based on the …

Chemistry and biology of the clinically used macrolactone antibiotic fidaxomicin

A Dorst, K Gademann - Helvetica Chimica Acta, 2020 - Wiley Online Library
Abstract Fidaxomicin (1, lipiarmycin A3, clostomicin B1, tiacumicin B) constitutes a
glycosylated 18‐membered macrolactone and is a natural product isolated from various soil …

Stereoselective Access to (E)-1,3-Enynes through Pd/Cu-Catalyzed Alkyne Hydrocarbation of Allenes

L Jeanne-Julien, G Masson, R Kouoi, A Regazzetti… - Organic …, 2019 - ACS Publications
PdII and CuI cooperate in catalyzing the alkynes hydrocarbation of allenes (AHA) giving (E)-
1, 3-enynes with high yields, atom economy, and high regio-/stereoselectivities. We devised …

Total Synthesis of Tiacumicin B: Study of the Challenging β‐Selective Glycosylations

C Tresse, M François‐Heude… - … A European Journal, 2021 - Wiley Online Library
We give a full account of the total synthesis of tiacumicin B (Tcn‐B), a natural glycosylated
macrolide with remarkable antibiotic properties. Our strategy is based on our experience …

Synthesis and biological evaluation of iodinated fidaxomicin antibiotics

A Dorst, IS Shchelik, D Schäfle, P Sander… - Helvetica Chimica …, 2020 - Wiley Online Library
Abstract Fidaxomicin (1, tiacumicin B, lipiarmycin A3) is a marketed antibiotic that is used in
the treatment of Clostridium difficile infections. Based on the analysis of a cryo‐EM structure …

A convergent approach toward fidaxomicin: Syntheses of the fully glycosylated northern and southern fragments

R Hollibaugh, X Yu, JK De Brabander - Tetrahedron, 2020 - Elsevier
Efficient approaches that enable the synthesis of analogs of natural product antibiotics are
needed to keep up with the emergence of multiply-resistant strains of pathogenic organisms …

Chemical approaches for the stereocontrolled synthesis of 1, 2-cis-β-D-rhamnosides

CAI Juntao, Y Xin, K Yuanfang, HU Yulong… - Chinese Journal of …, 2023 - Elsevier
In carbohydrate chemistry, the stereoselective synthesis of 1, 2-cis-glycosides remains a
formidable challenge. This complexity is comparable to the synthesis of 1, 2-cis-β-D …

Physicochemical characterization, solubilization, and stabilization of a macrolide antibiotic

BA Selvi, YCS Hlaing, K Infante, M Kaner… - Journal of Drug Delivery …, 2020 - Elsevier
Physicochemical and thermodynamic characterizations of fidaxomicin crystals were
investigated to develop novel formulations for efficient therapeutic activity. The pKa of …