ABSTRACT
The New Delhi metallo-β-lactamase-1 (NDM-1) was first reported in 2010, detected in a Klebsiella pneumoniae isolate from a Swedish patient of Indian origin. It has recently attracted extensive attention for its biological activities to catalyze the hydrolysis of almost all of β-lactam antibiotics. The gene for NDM-1 can spread from one strain of bacteria to another by horizontal gene transfer. The most troubling aspect is that there are currently no clinically available inhibitors to block the metallo-β-lactamase action. Therefore, there is urgent need to develop new NDM-1 inhibitors, which can protect β-lactam antibiotics from the hydrolysis effect of NDM-1. In this review, the current research, drug-assistant mechanism and potential NDM-1 inhibitors are summarized.
ABSTRACT
A2B adenosine receptor is involved in the control of mast cell degranulation, interleukin-8 synthesis and cell growth. A2B adenosine receptor antagonists may serve as novel drugs for asthma, Alzheimer' s disease, cystic fibrosis and type-II diabetes. Therefore, seeking for the highly selective A2B adenosine receptor antagonists has been one of great interest. The molecular basis, structure-activity relationship of selective A2B adenosine receptor antagonists and their interactions with A2B adenosine receptor were reviewed.