252872-64-3Relevant academic research and scientific papers
Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors
Sherrill, Ronald G.,Furfine, Eric S.,Hazen, Richard J.,Miller, John F.,Reynolds, David J.,Sammond, Douglas M.,Spaltenstein, Andrew,Wheelan, Pat,Wright, Lois L.
, p. 3560 - 3564 (2007/10/03)
A series of novel N-alkoxy-arylsulfonamide HIV protease inhibitors with low picomolar enzyme activity and single digit nanomolar antiviral activity is disclosed.
New N-arylsulfonyl-N-alkoxyaminoacetohydroxamic acids as selective inhibitors of gelatinase a (MMP-2)
Rossello, Armando,Nuti, Elisa,Orlandini, Elisabetta,Carelli, Paolo,Rapposelli, Simona,Macchia, Marco,Minutolo, Filippo,Carbonaro, Laura,Albini, Adriana,Benelli, Roberto,Cercignani, Giovanni,Murphy, Gillian,Balsamo, Aldo
, p. 2441 - 2450 (2007/10/03)
New N-arylsulfonyl-substituted alkoxyaminoaceto hydroxamic acid derivatives of types 8 and 10 designed as oxa-analogues of known sulfonamide-based MMPi of types 2 and 7 were synthesized and tested for their inhibitory activities on some matrix metalloproteinases. The combination of a biphenylsulfonamide group with oxyamino oxygen in the pharmacophoric central skeleton of sulfonamide-based MMPi obtained in the new sulfonamides 10 seems to be able to give selectivity for MMP-2 over MMP-1. The most potent derivative of this type, 10a, shows similar anti-invasive properties to the analogue reference drug CGS27023A, 2, in an in vitro model of invasion on matrigel, carried out on cellular lines of fibrosarcoma HT1080 (tumoural cells over-expressing MMP-2 and MMP-9).
Sulfonamide inhibitors of aspartyl protease
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, (2008/06/13)
The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical
