Design, Synthesis, and Biological Activities of Closantel Analogues: Structural Promiscuity and Its Impact on Onchocerca volvulus
摘要:
Onchocerciasis, or river blindness, is a neglected tropical disease that affects more than 37 million people worldwide, primarily in Africa and Central and South America. We have disclosed evidence that the larval-stage-specific chitinase, OvCHT1, may be a potential biological target for affecting nematode development. On the basis of screening efforts, closantel, a known anthelmintic drug, was discovered as a potent and highly specific OvCHT1 inhibitor. Originally, closantel's anthelmintic mode of action was believed to rely solely on its role as a proton ionophore; thus, the impact of each of its biological activities on O. volvulus L3 molting was investigated. Structure activity relationship studies on an active closantel fragment are detailed, and remarkably, by use of a simple salicylanilide scaffold, compounds acting only as protonophores or chitinase inhibitors were identified. From these data, unexpected synergistic protonophore and chitinase inhibition activities have also been found to be critical for molting in O. volvulus L3 larvae.
The present invention relates to a pipette tip comprising a proximal region and a distal region, wherein the proximal region comprises an exterior surface and an annular flange at the proximal terminus of the proximal region, the proximal region comprises a first set of axially oriented ribs and a second set of axially oriented ribs, the ribs of the first set and the second set are circumferentially spaced and alternately spaced around the exterior surface of the proximal region, and ribs of the first set have a maximum thickness greater than the maximum thickness of ribs of the second set.
A contact lens case having antimicrobial characteristics composed of a polymeric material having a plurality of amorphous zones. An antimicrobial agent is incorporated into said amorphous zones of the polymeric material of said body. The antimicrobial agent exhibits controlled migration through the amorphous zones of the polymeric material of said body. In this manner, the surface of the lens case is consistently saturated with an antimicrobial agent.
Salicylamide--acetylenedicarboxylate reactions as a route to benzoxazinones
作者:Ned D. Heindel、Lee A. Schaeffer
DOI:10.1021/jo00832a089
日期:1970.7
ANTIMICROBIAL CONTACT LENS CASE
申请人:Novartis AG
公开号:EP1458419B1
公开(公告)日:2005-05-04
Anti-microbial paper products having a substituted 1,2-dihydroquinoline
申请人:Abou-Nemeh Ibrahim
公开号:US20070089847A1
公开(公告)日:2007-04-26
The present invention generally provides anti-microbial paper products, compositions comprising anti-microbial paper products, processes for producing anti-microbial paper products, and methods of inhibiting microbial growth or replication in paper products.