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Infections
Published in Evelyne Jacqz-Aigrain, Imti Choonara, Paediatric Clinical Pharmacology, 2021
Evelyne Jacqz-Aigrain, Imti Choonara
Macrolides, lincosamides, ketolides, and streptogramins share overlapping binding sites on ribosomes, and have similar antimicrobial activities, as well as similar mechanisms of resistance [4]. The macrolides are a family of large cyclic molecules, all containing a macrocyclic lactone ring. The macrolide class of antibiotic agents includes compounds with 14-membered (erythromycin, clarithromycin) (Figure 17), 15-membered (azithromycin), and 16-membered (rokitamycin, spiramycin and josamycin) ring structures. Streptogramin antibiotics, such as pristinamycim or dalfopristin-quinupristin, contain two active components, type A and type B, which synergistically inhibit peptide elongation. Streptogramin B agents include quinupristin (Figure 18) and pristinamycin IA. Streptogramin A agents include dalfopristin and pristinamycim II A.
Pristinamycin
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Pristinamycin is a mixture of water-insoluble pristinamycin IA (PIA, 90–97%) and pristinamycin IIA (PIIA, 3–10%), derived from Streptomyces pristinaespiralis. The former is a group B streptogramin (a peptidic macrolactone or depsipeptide), whereas the latter is a group A streptogramin (a macrolide: polyunsaturated macrolactone). Structurally similar to pristinamycin, virginiamycin is derived from Streptomyces virginiae and is composed of virginiamycin S and virginiamycin M—respectively, a peptidic macrolactone and a macrolide. Group A and group B streptogramins are bacteriostatic by reversible binding of the 50S subunit of 70S bacterial ribosomes (Pechere, 1997). The molecular structure of the two pristinamycin components is shown in Figure 78.1.
Oxazolidinones and Streptogramins
Published in Thomas T. Yoshikawa, Shobita Rajagopalan, Antibiotic Therapy for Geriatric Patients, 2005
Stephen Marer, Shobita Rajagopalan
Streptogramins are antibiotics produced in nature by Streptomyces pristinaepiralis. They belong to the antibiotic family of macrolides-lincosamides-streptogramins (10). The streptogramin pristinamycin has been available in Europe for over 25 years for the treatment of gram-positive infections. Because it is water insoluble, it is available only for oral administration. Quinupristin and dalfopristin are both streptogramins that are derived from pristinamycin. Quinupristin is derived from pristinamycin IA, a type B streptogramin. Dalfopristin is derived from pristinamycin IIB, a type A streptogramin. The fixed-ratio 30:70 combination of quinupristin/dalfopristin is now marketed under the trade name Synercid. Because quinupristin and dalfopristin are water-soluble derivatives of pristinamycin, Synercid can be given only by the intravenous (IV) route. Synercid was released in the United States in 1999. For gram-positive organisms, it has essentially the same spectrum of activity as linezolid (with the exception of E. faecalis, which is generally resistant to quinupristin/ dalfopristin, but sensitive to linezolid), but has fewer approved indications for use.
Investigating the potential anticancer activities of antibiotics as topoisomerase II inhibitors and DNA intercalators: in vitro, molecular docking, molecular dynamics, and SAR studies
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Faten Farouk, Ayman Abo Elmaaty, Ahmed Elkamhawy, Haytham O. Tawfik, Radwan Alnajjar, Mohammed A. S. Abourehab, Mohamed A. Saleh, Wagdy M. Eldehna, Ahmed A. Al‐Karmalawy
In addition, regarding screened streptogramins, it was shown that linopristin, pristinamycin IA, quinupristin, and virginiamycin S1 antibiotics exhibited promising docking scores that are better than that attained by the co-crystallised ligand. In particular, it was disclosed that linopristin showed the best docking score among the screened streptogramins.