- Structure-Activity Relationship for the Oxadiazole Class of Antibacterials
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A structure-activity relationship (SAR) for the oxadiazole class of antibacterials was evaluated by syntheses of 72 analogs and determination of the minimal-inhibitory concentrations (MICs) against the ESKAPE panel of bacteria. Selected compounds were further evaluated for in vitro toxicity, plasma protein binding, pharmacokinetics (PK), and a mouse model of methicillin-resistant Staphylococcus aureus (MRSA) infection. Oxadiazole 72c shows potent in vitro antibacterial activity, exhibits low clearance, a high volume of distribution, and 41% oral bioavailability, and shows efficacy in mouse models of MRSA infection.
- Boudreau, Marc A.,Ding, Derong,Meisel, Jayda E.,Janardhanan, Jeshina,Spink, Edward,Peng, Zhihong,Qian, Yuanyuan,Yamaguchi, Takao,Testero, Sebastian A.,O'Daniel, Peter I.,Leemans, Erika,Lastochkin, Elena,Song, Wei,Schroeder, Valerie A.,Wolter, William R.,Suckow, Mark A.,Mobashery, Shahriar,Chang, Mayland
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supporting information
p. 322 - 326
(2019/10/16)
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- Substituted pentacyclic carbazolones as novel muscarinic allosteric agents: Synthesis and structure - Affinity and cooperativity relationships
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Two series of pentacyclic carbazolones, 22 and 23, have been synthesized utilizing a facile intramolecular Diels-Alder reaction and are allosteric modulators at muscarinic acetylcholine receptors. Their affinities and cooperativities with acetylcholine an
- Gharagozloo, Parviz,Lazareno, Sebastian,Miyauchi, Masao,Popham, Angela,Birdsall, Nigel J. M.
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p. 1259 - 1274
(2007/10/03)
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- Heterocyclic N-acetonylbenzamides and their use as fungicides
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Certain N-acetonylbenzamides and their use as fungicides are disclosed. The N-acetonylbenzamides disclosed contain a heterocyclic ring fused to an aromatic ring. These compounds are particularly effective against phytopathogenic fungi of the class Oomycetes. Also disclosed is a method for controlling phytopathogenic fungi by applying one or more of the heterocyclic N-acetonylbenzamides of the present invention, optionally with one or more additional fungicidal compounds.
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