4 Functional Modifications and Nuclear Analogues of β -Lactam Antibiotics -Part II

Gunda, E.T.; Jaszberenyi, J. C.

doi:10.1016/s0079-6468(08)70149-8

Cited by 10 publications

(2 citation statements)

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“…As many as 40 structurally different β-lactam compounds in 73 formulations are currently available for medical use. Improving upon the effectiveness of this class of antimicrobial agents has been an ongoing challenge, one which has continued to attract increasing attention, because of the emergence of multidrug-resistant strains of bacteria [ 19 , 20 , 21 , 22 , 23 , 24 ]. Over the years, countless penicillin derivatives [ 25 , 26 , 27 ] have been prepared and tested, and a variety of new β-lactam ring systems have been introduced ( Figure 1 ).…”

Section: Pbps and β-Lactamases: The Two Main Molecular Targets Formentioning

confidence: 99%

Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects

Konaklieva

2014

Antibiotics

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The common practice in antibacterial drug development has been to rapidly make an attempt to find ever-more stable and broad-spectrum variants for a particular antibiotic, once a drug resistance for that antibiotic is detected. We are now facing bacterial resistance toward our clinically relevant antibiotics of such a magnitude that the conversation for antimicrobial drug development ought to include effective new antibiotics with alternative mechanisms of action. The electrophilic β-lactam ring is amenable for the inhibition of different enzyme classes by a suitable decoration of the core scaffold. Monocyclic β-lactams lacking an ionizable group at the lactam nitrogen exhibit target preferences toward bacterial enzymes important for resistance and virulence. The present review intends to draw attention to the versatility of the β-lactams as antimicrobials with “unusual” molecular targets.

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Section: Pbps and β-Lactamases: The Two Main Molecular Targets Formentioning

confidence: 99%

Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects

Konaklieva

2014

Antibiotics

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“…Hence the conformation depends on the two variable angles CP 2 and t{l 3 which determine the orienta tions of the aminoacyl substituent and the carboxyl grouping, respectively. A review on the functional modifi cations and nuclear analogues of ,B-Iactam antibiotics can be fo und in (17,18). Antibacterial activity (0) requires a ,B-lactam ring of sufficient strain and possibilities for electron delocalization outside the lactam ring; (b) appears to be associated with CP2 rotational angles ranging, in solution, between -180° and -160°, i.e.…”

Section: Scope and Limitationmentioning

confidence: 99%

Use of Model Enzymes in the Determination of the Mode of Action of Penicillins and Delta3-Cephalosporins

Ghuysen

Frère

Leyh‐Bouille

et al. 1979

Annu. Rev. Biochem.

114

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β‐Lactamase inhibitors

Cartwright

Waley

1983

Medicinal Research Reviews

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In summary, Table XVI shows the inhibition profiles of representative beta-lactamases from each major class of Richmond and Sykes. Either resistance (R) or sensitivity (S) is given as a general guide to the type of compounds likely to inhibit each class. Thus the (qualitative) statements regarding the effectiveness of clavulanic acid can be taken to represent those for the penam sulfones and similarly for MM4550 and the other olivanic acids, carpetimycins, PS series, and asparenomycins. This can also be said of cloxacillin and the other aromatic carboxamido penicillins. Compounds are also included which are specifically or particularly inhibitory to certain beta-lactamases.

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4 Functional Modifications and Nuclear Analogues of β -Lactam Antibiotics -Part II

Cited by 10 publications

References 354 publications

Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects

Molecular Targets of β-Lactam-Based Antimicrobials: Beyond the Usual Suspects

Use of Model Enzymes in the Determination of the Mode of Action of Penicillins and Delta3-Cephalosporins

β‐Lactamase inhibitors

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