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Tetrahydroindazole inhibitors of bacterial type II topoisomerases. Part 2: SAR development and potency against multidrug-resistant strains
Authors:Wiener John J M  Gomez Laurent  Venkatesan Hariharan  Santillán Alejandro  Allison Brett D  Schwarz Kimberly L  Shinde Shirin  Tang Liu  Hack Michael D  Morrow Brian J  Motley S Timothy  Goldschmidt Raul M  Shaw Karen Joy  Jones Todd K  Grice Cheryl A
Institution:Johnson & Johnson Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. Jwiener@prdus.jnj.com
Abstract:We have previously reported a novel class of tetrahydroindazoles that display potency against a variety of Gram-positive and Gram-negative bacteria, potentially via interaction with type II bacterial topoisomerases. Herein are reported SAR investigations of this new series. Several compounds possessing broad-spectrum potency were prepared. Further, these compounds exhibit activity against multidrug-resistant Gram-positive microorganisms equivalent to that against susceptible strains.
Keywords:
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