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Antibiotics: The Need for Innovation
Published in Nathan Keighley, Miraculous Medicines and the Chemistry of Drug Design, 2020
Synthesis of such a highly strained compound was highly challenging, but manufacturing the compound without the need to laboriously purify it from mould cultures was advantageous for commercialisation of the antibiotic. This was accomplished by Sheehan in 1957. However, the full synthetic procedure was too involved to be commercially viable, but the following year a biosynthetic intermediate of penicillin, 6-aminopenicillonic acid (6-APA) was isolated by Beecham’s and revolutionised the production of semisynthetic penicillin by producing a readily available starting material.
Beta-Lactamase Inhibitors
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
Pascalis Vergidis, Matthew E. Falagas
Brobactam (6-beta-bromo-penicillanic acid) is another beta-lactamase inhibitor. It is a simple substituted compound of the penicillin nucleus, 6-APA (Melchior and Keiding, 1991; Wise et al., 1981). For pharmacologic studies, 800 mg of pivampicillin was combined with 200 mg of brobactam (Wise et al., 1992); however, this combination is not in clinical use.
Improving the 6-Aminopenicillanic acid release process using vermiculite-alginate biocomposite bead on drug delivery system
Published in Drug Development and Industrial Pharmacy, 2021
Nona Soleimanpour moghadam, Amirreza Azadmehr, Ardeshir Hezarkhani
One of the most commonly used antibacterial drugs is 6-Aminopenicillanic acid (6-APA) that forms the skeleton core of β-lactam antibiotics such as penicillin G. 6-APA as the precursor of all semisynthetic penicillin, commonly used in the treatment of bacterial infections over the past decades [4,5]. Worldwide, this antibacterial drug plays an important role in the human lifestyle and also has very beneficial effects on human and animal health due to its anti-microbial activity. Due to its easier use, oral administration, and fewer side effects, 6-APA is used as broad-spectrum antibiotics against both gram-positive and gram-negative bacteria [6]. Nevertheless, the widespread use of penicillin antibiotics for humans and animals has become a severe social problem that has gained concern across the world, in particular, due to their toxic effects on aquatic organisms in lakes and streams [7,8]. The carriers used to control the release of the drug were mainly clays such as montmorillonite [9], sepiolite [10], Laponite [11], and kaolinite [12].