85208-14-6Relevant academic research and scientific papers
PENICILLIN-BINDING PROTEIN INHIBITORS
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Paragraph 00266, (2021/06/04)
Described herein are certain boron-containing compounds, compositions, preparations and their use as modulators of the transpeptidase function of bacterial penicillin-binding proteins and as antibacterial agents. In some embodiments, the compounds describ
PENICILLIN-BINDING PROTEIN INHIBITORS
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Paragraph 00192, (2019/12/15)
Described herein are certain boron-containing compounds, compositions, preparations and their use as modulators of the transpeptidase function of bacterial penicillin-binding proteins and as antibacterial agents. In some embodiments, the compounds describ
PENICILLIN-BINDING PROTEIN INHIBITORS
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Paragraph 00184, (2018/12/13)
Described herein are certain boron-containing compounds, compositions, preparations and their use as modulators of the transpeptidase function of bacterial penicillin-binding proteins and as antibacterial agents. In some embodiments, the compounds described herein inhibit penicillin-binding proteins. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
Structure-Activity Relationships of a Series of 2-Amino-4-thiazole-Containing Renin Inhibitors
Patt, William C.,Hamilton, Harriet W.,Taylor, Michael D.,Ryan, Michael J.,Taylor, David G.,et al.
, p. 2562 - 2572 (2007/10/02)
A series of renin inhibitors was synthesized that contained a 2-amino-4-thiazolyl moiety at the P2 position.These derivatives are potent inhibitors of monkey renin in vitro and are selective in that they only weakly inhibit the closely related
The Chemistry of Some 2-Aminothiazol-4-ylacetic Acid Derivatives and the Synthesis of Derived Penicillins
Hardy, Kenneth D.,Harrington, Frank P.,Stachulski, Andrew V.
, p. 1227 - 1236 (2007/10/02)
The N-protected 2-aminothiazol-4-ylacetic acid derivatives (6), (11), (14), (16), (18), (26), (27), (30), (33), and (34) have been prepared.They are readily available by reaction of the corresponding 2-aminoethyl esters such as (1) with the appropriate acylating agents, generally giving a bis-carbamate of type (5), followed by saponification.The process is general for α-methylene, α-oximino, and α-aminosubstituents in the side-chain affording in the last case a route to differentially protected α-amino-α-(2-aminothiazol-4-yl)acetic acids such as (30).The optimum conditions for the acylations are described; the course of the saponification of the bis-carbamate esters is discussed and physical evidence for the structures of the derivatives is presented.The use of the protected acids (11) and (34) in the synthesis of the piperacillin analogue (38) is described.
