Literature DB >> 32184964

Structure-Activity Relationship for the Oxadiazole Class of Antibacterials.

Marc A Boudreau1, Derong Ding1, Jayda E Meisel1, Jeshina Janardhanan1, Edward Spink1, Zhihong Peng1, Yuanyuan Qian1, Takao Yamaguchi1, Sebastian A Testero1, Peter I O'Daniel1, Erika Leemans1, Elena Lastochkin1, Wei Song1, Valerie A Schroeder2, William R Wolter2, Mark A Suckow2, Shahriar Mobashery1, Mayland Chang1.   

Abstract

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.
Copyright © 2019 American Chemical Society.

Entities:  

Year:  2019        PMID： 32184964      PMCID： PMC7073871          DOI： 10.1021/acsmedchemlett.9b00379

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  9 in total

1.  Predicting plasma protein binding of drugs: a new approach.

Authors:  Nicole A Kratochwil; Walter Huber; Francis Müller; Manfred Kansy; Paul R Gerber
Journal:  Biochem Pharmacol       Date:  2002-11-01       Impact factor: 5.858

2.  Impact of pH on plasma protein binding in equilibrium dialysis.

Authors:  Christopher J Kochansky; Daniel R McMasters; Ping Lu; Kenneth A Koeplinger; Haley H Kerr; Magang Shou; Kenneth R Korzekwa
Journal:  Mol Pharm       Date:  2008-03-18       Impact factor: 4.939

Review 3.  Bad bugs, no drugs: no ESKAPE! An update from the Infectious Diseases Society of America.

Authors:  Helen W Boucher; George H Talbot; John S Bradley; John E Edwards; David Gilbert; Louis B Rice; Michael Scheld; Brad Spellberg; John Bartlett
Journal:  Clin Infect Dis       Date:  2009-01-01       Impact factor: 9.079

4.  Effect of protein binding of daptomycin on MIC and antibacterial activity.

Authors:  B L Lee; M Sachdeva; H F Chambers
Journal:  Antimicrob Agents Chemother       Date:  1991-12       Impact factor: 5.191

5.  In Vitro and In Vivo Synergy of the Oxadiazole Class of Antibacterials with β-Lactams.

Authors:  Jeshina Janardhanan; Jayda E Meisel; Derong Ding; Valerie A Schroeder; William R Wolter; Shahriar Mobashery; Mayland Chang
Journal:  Antimicrob Agents Chemother       Date:  2016-08-22       Impact factor: 5.191

Review 6.  Update on the antibiotic resistance crisis.

Authors:  Gian Maria Rossolini; Fabio Arena; Patrizia Pecile; Simona Pollini
Journal:  Curr Opin Pharmacol       Date:  2014-09-23       Impact factor: 5.547

7.  Structure-activity relationship for the oxadiazole class of antibiotics.

Authors:  Edward Spink; Derong Ding; Zhihong Peng; Marc A Boudreau; Erika Leemans; Elena Lastochkin; Wei Song; Katerina Lichtenwalter; Peter I O'Daniel; Sebastian A Testero; Hualiang Pi; Valerie A Schroeder; William R Wolter; Nuno T Antunes; Mark A Suckow; Sergei Vakulenko; Mayland Chang; Shahriar Mobashery
Journal:  J Med Chem       Date:  2015-01-30       Impact factor: 7.446

8.  Protein binding and serum bactericidal activities of vancomycin and teicoplanin.

Authors:  R S Dykhuizen; G Harvey; N Stephenson; D Nathwani; I M Gould
Journal:  Antimicrob Agents Chemother       Date:  1995-08       Impact factor: 5.191

9.  Discovery of a new class of non-β-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity.

Authors:  Peter I O'Daniel; Zhihong Peng; Hualiang Pi; Sebastian A Testero; Derong Ding; Edward Spink; Erika Leemans; Marc A Boudreau; Takao Yamaguchi; Valerie A Schroeder; William R Wolter; Leticia I Llarrull; Wei Song; Elena Lastochkin; Malika Kumarasiri; Nuno T Antunes; Mana Espahbodi; Katerina Lichtenwalter; Mark A Suckow; Sergei Vakulenko; Shahriar Mobashery; Mayland Chang
Journal:  J Am Chem Soc       Date:  2014-02-21       Impact factor: 15.419
  9 in total
  5 in total

1.  Unconventional Antibacterials and Adjuvants.

Authors:  Mayland Chang; Kiran V Mahasenan; Juan A Hermoso; Shahriar Mobashery
Journal:  Acc Chem Res       Date:  2021-01-29       Impact factor: 22.384

2.  Physicochemical and Structural Parameters Contributing to the Antibacterial Activity and Efflux Susceptibility of Small-Molecule Inhibitors of Escherichia coli.

Authors:  Sara S El Zahed; Shawn French; Maya A Farha; Garima Kumar; Eric D Brown
Journal:  Antimicrob Agents Chemother       Date:  2021-03-18       Impact factor: 5.191

3.  Highly Active Small Aminated Quinolinequinones against Drug-Resistant Staphylococcus aureus and Candida albicans.

Authors:  Hatice Yıldırım; Nilüfer Bayrak; Mahmut Yıldız; Fatıma Nur Yılmaz; Emel Mataracı-Kara; Deepak Shilkar; Venkatesan Jayaprakash; Amaç Fatih TuYuN
Journal:  Molecules       Date:  2022-05-03       Impact factor: 4.927

4.  Mechanistic Studies and In Vivo Efficacy of an Oxadiazole-Containing Antibiotic.

Authors:  George A Naclerio; Nader S Abutaleb; Kenneth I Onyedibe; Caroline Karanja; Hassan E Eldesouky; Hsin-Wen Liang; Alexandra Dieterly; Uma K Aryal; Tiffany Lyle; Mohamed N Seleem; Herman O Sintim
Journal:  J Med Chem       Date:  2022-04-28       Impact factor: 8.039

5.  3D-QSAR Studies of 1,2,4-Oxadiazole Derivatives as Sortase A Inhibitors.

Authors:  Neda Shakour; Farzin Hadizadeh; Prashant Kesharwani; Amirhossein Sahebkar
Journal:  Biomed Res Int       Date:  2021-12-06       Impact factor: 3.411
  5 in total

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