625471-23-0Relevant academic research and scientific papers
Discovery of aminopiperidine-based Smac mimetics as IAP antagonists
Hennessy, Edward J.,Saeh, Jamal C.,Sha, Li,MacIntyre, Terry,Wang, Haiyun,Larsen, Nicholas A.,Aquila, Brian M.,Ferguson, Andrew D.,Laing, Naomi M.,Omer, Charles A.
, p. 1690 - 1694 (2012/04/10)
A series of structurally unique Smac mimetics that act as antagonists of inhibitor of apoptosis proteins (IAPs) has been discovered. While most previously described Smac mimetics contain the proline ring (or a similar cyclic motif) found in Smac, a key feature of the compounds described herein is that this ring has been removed. Despite this, compounds in this series potently bind to cIAP1 and elicit the expected phenotype of cIAP1 inhibition in cancer cells. Marked selectivity for cIAP1 over XIAP is observed for these compounds, which is attributed to a slight difference in the binding groove between the two proteins and the resulting steric interactions with the inhibitors. XIAP binding can be improved by constraining the inhibitor so that these unfavorable steric interactions are minimized.
Side chain SAR of bicyclic β-lactamase inhibitors (BLIs). 1. Discovery of a class C BLI for combination with imipinem
Blizzard, Timothy A.,Chen, Helen,Kim, Seongkon,Wu, Jane,Young, Katherine,Park, Young-Whan,Ogawa, Amy,Raghoobar, Susan,Painter, Ronald E.,Hairston, Nichelle,Lee, Sang Ho,Misura, Andrew,Felcetto, Tom,Fitzgerald, Paula,Sharma, Nandini,Lu, Jun,Ha, Sookhee,Hickey, Emily,Hermes, Jeff,Hammond, Milton L.
scheme or table, p. 918 - 921 (2010/08/06)
Bridged monobactam β-lactamase inhibitors were prepared and evaluated as potential partners for combination with imipenem to overcome class C β-lactamase mediated resistance. The (S)-azepine analog 2 was found to be effective in both in vitro and in vivo assays and was selected for preclinical development.
NOVEL INHIBITORS OF BETA-LACTAMASE
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Page/Page column 34, (2008/06/13)
A class of 7-oxo-2,6-diazabicyclo-[3.2.0]-heptane-6-sulfonic acid compounds substituted at the two position of the bicyclic ring with a heterocyclylaminocarbonyl group or a carbocyclylaminocarbonyl group are β-lactamase inhibitors. The compounds and their prodrugs and pharmaceutically acceptable salts are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds are suitable for use with β-lactam antibiotics (e.g., imipenem and ceftazidime) against micro-organisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.
