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HIV-1 Integrase Inhibitor-Inspired Antibacterials Targeting Isoprenoid Biosynthesis.

ACS medicinal chemistry letters

Zhang Y, Fu-Yang Lin, Li K, Zhu W, Liu YL, Cao R, Pang R, Lee E, Axelson J, Hensler M, Wang K, Molohon KJ, Wang Y, Mitchell DA, Nizet V, Oldfield E.
PMID: 22662288
ACS Med Chem Lett. 2012 Apr 03;3(5):402-406. doi: 10.1021/ml300038t.

We report the discovery of antibacterial leads, keto- and diketo-acids, targeting two prenyl transferases: undecaprenyl diphosphate synthase (UPPS) and dehydrosqualene synthase (CrtM). The leads were suggested by the observation that keto- and diketo-acids bind to the active site Mg(2+)/Asp...

Targeted Treatment for Bacterial Infections: Prospects for Pathogen-Specific Antibiotics Coupled with Rapid Diagnostics.

Tetrahedron

Maxson T, Mitchell DA.
PMID: 27429480
Tetrahedron. 2016 Jun 23;72(25):3609-3624. doi: 10.1016/j.tet.2015.09.069. Epub 2015 Oct 09.

Antibiotics are a cornerstone of modern medicine and have significantly reduced the burden of infectious diseases. However, commonly used broad-spectrum antibiotics can cause major collateral damage to the human microbiome, causing complications ranging from antibiotic-associated colitis to the rapid...

Crystal structure and absolute configuration of (3S,4aS,8aS)-N-tert-butyl-2-[(S)-3-(2-chloro-4-nitro-benzamido)-2-hy-droxy-prop-yl]deca-hydro-isoquinoline-3-carboxamide and (3S,4aS,8aS)-N-tert-butyl-2-{(S)-2-[(S)-1-(2-chloro-4-nitro-benzoyl)pyrrolidin-2-yl]-2-hy-droxy-eth-yl}deca-hydro-iso-quinoline-3-carboxamide.

Acta crystallographica. Section E, Crystallographic communications

Maxson T, Bertke JA, Gray DL, Mitchell DA.
PMID: 26594520
Acta Crystallogr E Crystallogr Commun. 2015 Oct 31;71:1401-7. doi: 10.1107/S2056989015020046. eCollection 2015 Nov 01.

The crystal structure and absolute configuration of the two new title nelfinavir analogs, C24H35ClN4O5, (I), and C27H39ClN4O5, (II), have been determined. Each of these mol-ecules exhibits a number of disordered moieties. There are intra-molecular N-H⋯O hydrogen bonds in both...

Showing 1 to 3 of 3 entries