364595-09-5Relevant academic research and scientific papers
Banana-shaped 1,2,4-oxadiazole analogues of 1,3,4-oxadiazoles
Torgova, Sofia I.,Karamysheva, Ludmila A.,Geivandova, Tatiana A.,Strigazzi, Alfredo
, p. 99 - 106 (2001)
In the last years bent banana-shaped mesomorphic molecules found an increasingly great interest among theoreticians and experimentalists due to the nature of this type of liquid crystals to exhibit a spontaneous polarization in the absence of any chiral g
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
, 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.
