161397-68-8Relevant articles and documents
Structure-Activity Relationship for the Oxadiazole Class of Antibacterials
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
supporting information, p. 322 - 326 (2019/10/16)
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.
Substituted pentacyclic carbazolones as novel muscarinic allosteric agents: Synthesis and structure - Affinity and cooperativity relationships
Gharagozloo, Parviz,Lazareno, Sebastian,Miyauchi, Masao,Popham, Angela,Birdsall, Nigel J. M.
, p. 1259 - 1274 (2007/10/03)
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
Heterocyclic N-acetonylbenzamides and their use as fungicides
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Page 18, (2010/01/31)
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.