Abstract
The azetidinone core-structure offers a unique approach to the design and synthesis of new derivatives with unique biological properties. During the last two decades researches convincingly demonstrated that the prospect of structural modifications of monocyclic β-lactams with specific substituents is an effective procedure for the detection and improvement of important pharmacological effects different from antibacterial activity. As a matter of fact, new β-lactam compounds demonstrated biological activity as inhibitors of a wide range of enzymes. This review reports the latest developments on monocyclic β-lactam compounds activity as anticancer, antitubercular, HFAAH inhibitors, HDAC inhibitors, anti-inflammatory drugs (tryptase inhibitors), Cathepsin K inhibitors, and vasopressin inhibitors. We attempted to highlight the intertwined relationships between structural features and biological activities, by analysing groups anchored on the three positions of the azetidinone ring as sources of molecular diversity
Keywords: Antibacterial, antibiotics, anticancer, azetidinone, heterocycles, β-lactam, inhibitor activity, enzymatic inhibitors, HFAAH, tryptase, cathepsin, HDAC, PPAR, monocyclic β-lactams, biological activity
Current Medicinal Chemistry
Title: Monocyclic β-Lactams: New Structures for New Biological Activities
Volume: 18 Issue: 28
Author(s): P. Galletti and D. Giacomini
Affiliation:
Keywords: Antibacterial, antibiotics, anticancer, azetidinone, heterocycles, β-lactam, inhibitor activity, enzymatic inhibitors, HFAAH, tryptase, cathepsin, HDAC, PPAR, monocyclic β-lactams, biological activity
Abstract: The azetidinone core-structure offers a unique approach to the design and synthesis of new derivatives with unique biological properties. During the last two decades researches convincingly demonstrated that the prospect of structural modifications of monocyclic β-lactams with specific substituents is an effective procedure for the detection and improvement of important pharmacological effects different from antibacterial activity. As a matter of fact, new β-lactam compounds demonstrated biological activity as inhibitors of a wide range of enzymes. This review reports the latest developments on monocyclic β-lactam compounds activity as anticancer, antitubercular, HFAAH inhibitors, HDAC inhibitors, anti-inflammatory drugs (tryptase inhibitors), Cathepsin K inhibitors, and vasopressin inhibitors. We attempted to highlight the intertwined relationships between structural features and biological activities, by analysing groups anchored on the three positions of the azetidinone ring as sources of molecular diversity
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Cite this article as:
Galletti P. and Giacomini D., Monocyclic β-Lactams: New Structures for New Biological Activities, Current Medicinal Chemistry 2011; 18 (28) . https://dx.doi.org/10.2174/092986711797200480
DOI https://dx.doi.org/10.2174/092986711797200480 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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