Wisconsin Alumni Research Foundation

Christine E McInnis

Helen Blackwell

Non-lactone carbocyclic modulators of bacterial quorum sensing. Pharmaceutical composition containing such modulators. Methods employing such modulators for modulation of quorum sensing. Compounds are exemplified by those of formula:A-[Z]-L1-[Y]&#x2014;NH-L2-HG,where A is an optionally substituted aryl or heteroaryl group having one or two 5- or 6-member rings with up to 1-3 heteroatoms in a ring, or a substituted or unsubstituted C1-C12 acyclic aliphatic group and HG is an optionally substituted cyclopentyl group. Compounds include those where n is 1 or 0, Z is &#x2014;CO&#x2014;, &#x2014;O&#x2014;CO&#x2014;, &#x2014;CO&#x2014;O&#x2014;, &#x2014;NH&#x2014;CO&#x2014;, &#x2014;CO&#x2014;NH&#x2014;, &#x2014;NH&#x2014;CO&#x2014;NH&#x2014;, &#x2014;O&#x2014;, &#x2014;S&#x2014;, or &#x2014;NH, Y is &#x2014;NH&#x2014;CO&#x2014;, &#x2014;CO&#x2014;CH&#x2014;C(Y1)-, or &#x2014;SO&#x2014;, where Y1 is &#x2014;OH, &#x2014;SH, &#x2014;NHor &#x2014;F; and L1 and L2 independently are &#x2014;[CH]p1- and &#x2014;[CH]p2-, where p1 and p2, independently, are 0 or integers ranging from 1-3.

Non-lactone carbocyclic modulators of bacterial quorum sensing

Non-lactone carbocyclic and heterocyclic antagonists and agonists of bacterial quorum sensing. Pharmaceutical composition containing antagonists. Methods employing antagonists and agonists for modulation of quorum sensing. Compounds are exemplified by those of formula:A-[Z]-L1-[Y]-W-[V]-L2-HG,where A is an acyclic aliphatic group, and HG is an optionally substituted phenyl group. Compounds include those where m and n are both 0, W is &#x2014;NH&#x2014;, Y is present and is &#x2014;CO&#x2014;CH&#x2014;CO&#x2014;, and L1 and L2 independently are &#x2014;[CH]&#x2014; and &#x2014;[CH]&#x2014;, where p1 and p2, independently, are 0 or integers ranging from 1-10.

Non-lactone carbocyclic and heterocyclic antagonists and agonists of bacterial quorum sensing

Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.

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Madison, WI, United States of America

Christine E McInnis