title: Tetrahydroindazole inhibitors of bacterial type II topoisomerases. Part 2: SAR development and potency against multidrug-resistant strains.
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.
authors: Johnson & Johnson Pharmaceutical Research & Development L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. Jwiener@prdus.jnj.com
authors: John J M
authors: JJ
authors: Wiener
authors: Laurent
authors: L
authors: Gomez
authors: Hariharan
authors: H
authors: Venkatesan
authors: Alejandro
authors: A
authors: Santillán
authors: Brett D
authors: BD
authors: Allison
authors: Kimberly L
authors: KL
authors: Schwarz
authors: Shirin
authors: S
authors: Shinde
authors: Liu
authors: L
authors: Tang
authors: Michael D
authors: MD
authors: Hack
authors: Brian J
authors: BJ
authors: Morrow
authors: S Timothy
authors: ST
authors: Motley
authors: Raul M
authors: RM
authors: Goldschmidt
authors: Karen Joy
authors: KJ
authors: Shaw
authors: Todd K
authors: TK
authors: Jones
authors: Cheryl A
authors: CA
authors: Grice
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D018432:Drug Resistance, Multiple / Q000502:physiology; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D007191:Indazoles / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D007191:Indazoles; D059005:Topoisomerase II Inhibitors