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Bioorg Med Chem Lett DOI:10.1016/j.bmcl.2007.09.010

N-Benzyl-3-sulfonamidopyrrolidines as novel inhibitors of cell division in E. coli.

Publication TypeJournal Article
Year of Publication2007
AuthorsMukherjee, S, Robinson, CA, Howe, AG, Mazor, T, Wood, PA, Urgaonkar, S, Hebert, AM, Raychaudhuri, D, Shaw, JT
JournalBioorg Med Chem Lett
Volume17
Issue23
Pages6651-5
Date Published2007 Dec 01
ISSN1464-3405
KeywordsAnti-Bacterial Agents, Cell Division, Escherichia coli, Escherichia coli Proteins, Growth Inhibitors, Microbial Sensitivity Tests, Pyrrolidines, Sulfonamides
Abstract

A new small molecule inhibitor of bacterial cell division has been discovered using a high-throughput screen in Escherichia coli. Although the lead screening hit (534F6) exhibited modest inhibition of the GTPase activity of FtsZ (20+/-5% at 100microM of compound), a primary target for bacterial cell division inhibitors, several analogs caused potent bacterial growth inhibition with negligible antagonism of FtsZ GTPase activity. A library of analogs has been prepared and several alkyne-tagged photoaffinity probes have been synthesized for use in experiments to elucidate the primary target of this compound.

URLhttp://linkinghub.elsevier.com/retrieve/pii/S0960-894X(07)01042-6
DOI10.1016/j.bmcl.2007.09.010
Pubmed

http://www.ncbi.nlm.nih.gov/pubmed/17923406?dopt=Abstract

Alternate JournalBioorg. Med. Chem. Lett.
PubMed ID17923406
PubMed Central IDPMC3335298
Grant ListR03 AI062905-01 / AI / NIAID NIH HHS / United States
R01 GM068025 / GM / NIGMS NIH HHS / United States
R03 AI062905 / AI / NIAID NIH HHS / United States
N01CO12400 / CA / NCI NIH HHS / United States
N01-CO-12400 / CO / NCI NIH HHS / United States