1072902-89-6Relevant academic research and scientific papers
Inhibitors of an essential mycobacterial cell wall lipase (Rv3802c) as tuberculosis drug leads
West, Nicholas P.,Cergol, Katie M.,Xue, Millie,Randall, Elizabeth J.,Britton, Warwick J.,Payne, Richard J.
, p. 5166 - 5168 (2011/06/10)
The first targeted inhibitors of an essential M. tuberculosis cell wall lipase, Rv3802c, are described. Lead compounds exhibited nanomolar inhibition of the enzyme, and encouraging antibacterial activity against M. tuberculosis in vitro, supporting Rv3802c as a novel TB drug target.
Tetrahydrolipstatin analogues as modulators of endocannabinoid 2-arachidonoylglycerol metabolism
Ortar, Giorgio,Bisogno, Tiziana,Ligresti, Alessia,Morera, Enrico,Nalli, Marianna,Di Marzo, Vincenzo
experimental part, p. 6970 - 6979 (2009/11/30)
A series of 21 analogues of tetrahydrolipstatin (THL, 1) were synthesized and tested as inhibitors of the formation or hydrolysis of the endocannabinoid 2-arachidonoylglycerol (2-AG). Three of the novel compounds, i.e., 11, 13, and 15, inhibited 2-AG formation via the diacylglycerol lipase α (DAGLα) with IC50 values lower than 50 nM (IC50 of THL = 1 μM) and were between 23- and 375-fold selective vs 2-AG hydrolysis by monoacylglycerol lipase (MAGL) as well as vs cannabinoid CB1 and CB2 receptors and anandamide hydrolysis by fatty acid amide hydrolase (FAAH). Three other THL analogues, i.e., 14, 16, and 18, were slightly more potent than THL against DAGLα and appreciably selective vs MAGL, CB receptors, and FAAH (15-26-fold). One compound, i.e., 8, was a potent inhibitor of MAGL-like activity (IC50 = 0.41 μM), and relatively (～7-fold) selective vs the other targets tested.
