Discovery and Optimization of Phosphopantetheine Adenylyltransferase Inhibitors with Gram-Negative Antibacterial Activity.

doi:10.1021/acs.jmedchem.7b01861

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Article

Discovery and Optimization of Phosphopantetheine Adenylyltransferase Inhibitors with Gram-Negative Antibacterial Activity.

Journal of medicinal chemistry - 26 Apr 2018

Skepper Colin K, Moreau Robert J, Appleton Brent A, Benton Bret M, Drumm Joseph E, Feng Brian Y, Geng Mei, Hu Cheng, Li Cindy, Lingel Andreas, Lu Yipin, Mamo Mulugeta, Mergo Wosenu, Mostafavi Mina, Rath Christopher M, Steffek Micah, Takeoka Kenneth T, Uehara Kyoko, Wang Lisha, Wei Jun-Rong, Xie Lili, Xu Wenjian, Zhang Qiong, de Vicente Javier

Abstract excerpt

In the preceding manuscript [ Moreau et al. 2018 , 10.1021/acs.jmedchem.7b01691 ] we described a successful fragment-based lead discovery (FBLD) strategy for discovery of bacterial phosphopantetheine adenylyltransferase inhibitors (PPAT, CoaD). Following several rounds of optimization two promising lead compounds were identified: triazolopyrimidinone 3 and 4-azabenzimidazole 4. Here we disclose our efforts to...

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PMID: 29551072
DOI: 10.1021/acs.jmedchem.7b01861

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

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