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Table representation of search results timeline featuring number of search results per year.

Year Number of Results
1987 1
1988 1
1990 1
1992 1
1994 1
2002 1
2003 2
2004 1
2005 1
2007 3
2008 2
2009 1
2010 3
2011 3
2012 1
2013 2
2014 1
2015 4
2017 2
2018 3
2019 3
2020 1
2021 1
2023 1
2024 0

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39 results

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Page 1
Discovery of antibiotic (E)-3-(3-carboxyphenyl)-2-(4-cyanostyryl)quinazolin-4(3H)-one.
Bouley R, Kumarasiri M, Peng Z, Otero LH, Song W, Suckow MA, Schroeder VA, Wolter WR, Lastochkin E, Antunes NT, Pi H, Vakulenko S, Hermoso JA, Chang M, Mobashery S. Bouley R, et al. J Am Chem Soc. 2015 Feb 11;137(5):1738-41. doi: 10.1021/jacs.5b00056. Epub 2015 Feb 2. J Am Chem Soc. 2015. PMID: 25629446 Free PMC article.
In silico docking and screening, followed by chemical synthesis of a library of quinazolinones, led to the discovery of (E)-3-(3-carboxyphenyl)-2-(4-cyanostyryl)quinazolin-4(3H)-one (compound 2) as an antibiotic effective in vivo against methicillin-resistant Staphylococcu …
In silico docking and screening, followed by chemical synthesis of a library of quinazolinones, led to the discovery of (E)-3-(3-carb …
Tackling antibiotic resistance.
Bush K, Courvalin P, Dantas G, Davies J, Eisenstein B, Huovinen P, Jacoby GA, Kishony R, Kreiswirth BN, Kutter E, Lerner SA, Levy S, Lewis K, Lomovskaya O, Miller JH, Mobashery S, Piddock LJ, Projan S, Thomas CM, Tomasz A, Tulkens PM, Walsh TR, Watson JD, Witkowski J, Witte W, Wright G, Yeh P, Zgurskaya HI. Bush K, et al. Nat Rev Microbiol. 2011 Nov 2;9(12):894-6. doi: 10.1038/nrmicro2693. Nat Rev Microbiol. 2011. PMID: 22048738 Free PMC article. Review.
Structural aspects for evolution of beta-lactamases from penicillin-binding proteins.
Meroueh SO, Minasov G, Lee W, Shoichet BK, Mobashery S. Meroueh SO, et al. J Am Chem Soc. 2003 Aug 13;125(32):9612-8. doi: 10.1021/ja034861u. J Am Chem Soc. 2003. PMID: 12904027
Penicillin-binding proteins (PBPs), biosynthetic enzymes of bacterial cell wall assembly, and beta-lactamases, resistance enzymes to beta-lactam antibiotics, are related to each other from an evolutionary point of view. Massova and Mobashery (Antimicrob. Agents Chemother. …
Penicillin-binding proteins (PBPs), biosynthetic enzymes of bacterial cell wall assembly, and beta-lactamases, resistance enzymes to beta-la …
Exploration of the Structural Space in 4(3H)-Quinazolinone Antibacterials.
Qian Y, Allegretta G, Janardhanan J, Peng Z, Mahasenan KV, Lastochkin E, Gozun MMN, Tejera S, Schroeder VA, Wolter WR, Feltzer R, Mobashery S, Chang M. Qian Y, et al. J Med Chem. 2020 May 28;63(10):5287-5296. doi: 10.1021/acs.jmedchem.0c00153. Epub 2020 May 8. J Med Chem. 2020. PMID: 32343145 Free PMC article.
Subsequent investigation of the pharmacokinetic properties singled out compound 73 ((E)-3-(5-carboxy-2-fluorophenyl)-2-(4-cyanostyryl)quinazolin-4(3H)-one) for further study. ...
Subsequent investigation of the pharmacokinetic properties singled out compound 73 ((E)-3-(5-carboxy-2-fluorophenyl)-2-(4-cyanostyryl …
Production of Proteins of the SARS-CoV-2 Proteome for Drug Discovery.
Kim C, Mahasenan KV, Bhardwaj A, Wiest O, Chang M, Mobashery S. Kim C, et al. ACS Omega. 2021 Jul 20;6(30):19983-19994. doi: 10.1021/acsomega.1c02984. eCollection 2021 Aug 3. ACS Omega. 2021. PMID: 34337272 Free PMC article.
These included all but six: NSP6, which possesses eight transmembrane regions, and five that are small proteins/peptides (E, ORF3b, ORF6, ORF7b, and ORF10). These proteins are intended for experimental validation of small-molecule binders as molecular template hits. ...
These included all but six: NSP6, which possesses eight transmembrane regions, and five that are small proteins/peptides (E, ORF3b, O …
Inactivation of alanine racemase by beta-chloro-L-alanine released enzymatically from amino acid and peptide C10-esters of deacetylcephalothin.
Mobashery S, Johnston M. Mobashery S, et al. Biochemistry. 1987 Sep 8;26(18):5878-84. doi: 10.1021/bi00392a045. Biochemistry. 1987. PMID: 3118951
Each of the compounds examined is a substrate for the Escherichia coli TEM-2 beta-lactamase, and enzyme-catalyzed hydrolysis of the lactam bond gives release of an amino acid or a peptidyl fragment from a cephem nucleus. 7 beta-(2-Thienylacetamido)-3-[[(beta-chloro-L-alanyl)oxy]m …
Each of the compounds examined is a substrate for the Escherichia coli TEM-2 beta-lactamase, and enzyme-catalyzed hydrolysis of the lactam b …
Cinnamonitrile Adjuvants Restore Susceptibility to β-Lactams against Methicillin-Resistant Staphylococcus aureus.
Speri E, Kim C, De Benedetti S, Qian Y, Lastochkin E, Fishovitz J, Fisher JF, Mobashery S. Speri E, et al. ACS Med Chem Lett. 2019 Jul 1;10(8):1148-1153. doi: 10.1021/acsmedchemlett.9b00169. eCollection 2019 Aug 8. ACS Med Chem Lett. 2019. PMID: 31413798 Free PMC article.
Five compounds out of 84 total compounds showed broad potentiation. At 8 muM (E)-3-(5-(3,4-dichlorobenzyl)-2-(trifluoromethoxy)phenyl)-2-(methylsulfonyl)acrylonitrile (26) potentiated oxacillin with a >4000-fold reduction of its MIC (from 256 to 0.06 mg.L(-1)). ...
Five compounds out of 84 total compounds showed broad potentiation. At 8 muM (E)-3-(5-(3,4-dichlorobenzyl)-2-(trifluoromethoxy)phenyl …
Potent mechanism-based inhibitors for matrix metalloproteinases.
Ikejiri M, Bernardo MM, Bonfil RD, Toth M, Chang M, Fridman R, Mobashery S. Ikejiri M, et al. J Biol Chem. 2005 Oct 7;280(40):33992-4002. doi: 10.1074/jbc.M504303200. Epub 2005 Jul 26. J Biol Chem. 2005. PMID: 16046398 Free article.
However, with the onset of covalent chemistry with the best of these inhibitors (e.g. inhibitor 3), very little recovery of activity (<10%) was seen over 48 h of dialysis. ...
However, with the onset of covalent chemistry with the best of these inhibitors (e.g. inhibitor 3), very little recovery of activity …
39 results