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Amidine substituted beta - lactam compounds, their preparation and use as antibacterial agents
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A compound and substituent technology, applied in the field of new β-lactam compounds, can solve problems that endanger the mid-term availability of existing compounds
Inactive Publication Date: 2014-12-10
AICURIS GMBH & CO KG
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However, a continuously updated list of a wide range of over 1000 β-lactamases can be found at http: / / www.lahey.org / Studies / ) and other resistance mechanisms seriously jeopardize the mid-term availability of existing compounds in these subclasses
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[1114] 1 H NMR (400MHz, DMSO-d 6 ):δ=1.35(d,J=6.2Hz,3H),3.66(dd,J=6.0 and 2.5Hz,1H),4.26-4.57(m,5H),6.78(s,1H),7.76(dd, J=8.9 and 2.7Hz, 1H), 8.26(d, J=8.9Hz, 1H), 8.52(d, J=2.3Hz, 1H), 8.95(s, 2H), 9.21-9.49(m, 3H).
[1115] MS (ES - ) m / z: C 17 h 20 N 8 o 7 S 2 [M-H] - Calculated value: 512.09. Experimental value: 512.53.
[1116] HPLC: 96.60%
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Abstract
The present invention relates to novel beta-lactam compounds of formula (I), their preparation and use. In particular, this invention relates to novel beta-lactam compounds which are amidine substituted monobactam derivatives useful as antimicrobial agents and their preparation.
Description
technical field [0001] The present invention relates to novel beta-lactam compounds, their preparation and use. In particular, the present invention relates to novel β-lactam compounds which are amidine substituted monobactam derivatives and their preparation as antimicrobial agents. Background technique [0002] Public health experts and officials consider the emergence and spread of antibiotic-resistant bacteria to be one of the major public health problems of the 21st century. While not a new phenomenon per se, the spread of antibiotic-resistant bacteria has reached unprecedented proportions. Despite the continued emergence of the most resistant isolates in hospital settings, physicians and epidemiologists encounter increased numbers of resistant bacteria in community populations with no previous healthcare exposure. The number of patients dying from untreatable nosocomial infections continues to grow. Treatment options are especially limited for infections due to mult...
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