D
David F. Bruhn
Researcher at St. Jude Children's Research Hospital
Publications - 21
Citations - 669
David F. Bruhn is an academic researcher from St. Jude Children's Research Hospital. The author has contributed to research in topics: Antibiotics & Mycobacterium tuberculosis. The author has an hindex of 13, co-authored 21 publications receiving 559 citations. Previous affiliations of David F. Bruhn include University of Massachusetts Amherst.
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Journal ArticleDOI
Spectinamides: a new class of semisynthetic antituberculosis agents that overcome native drug efflux
Richard E. Lee,Julian G. Hurdle,Jiuyu Liu,David F. Bruhn,Tanja Matt,Michael S. Scherman,Pavan K. Vaddady,Zhong Zheng,Jianjun Qi,Rashid Akbergenov,Sourav Das,Dora B. Madhura,Chetan Rathi,Ashit Trivedi,Cristina Villellas,Robin B. Lee,Rakesh,Samanthi L. Waidyarachchi,Dianqing Sun,Michael R. McNeil,José A. Aínsa,Helena I. Boshoff,Mercedes Gonzalez-Juarrero,Bernd Meibohm,Erik C. Böttger,Anne J. Lenaerts +25 more
TL;DR: The antitubercular efficacy of spectinamides demonstrates that synthetic modifications to classical antibiotics can overcome the challenge of intrinsic efflux pump-mediated resistance and expands opportunities for target-based tuberculosis drug discovery.
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Synthesis, structure-activity relationship studies, and antibacterial evaluation of 4-chromanones and chalcones, as well as olympicin A and derivatives
Li Feng,Marcus M. Maddox,Zahidul Alam,Lissa S. Tsutsumi,Gagandeep Narula,David F. Bruhn,Xiaoqian Wu,Shayna Sandhaus,Robin B. Lee,Charles J. Simmons,Yuk-Ching Tse-Dinh,Julian G. Hurdle,Richard E. Lee,Dianqing Sun +13 more
TL;DR: Mode of action studies performed on selected compounds revealed that they dissipated the bacterial membrane potential, resulting in the inhibition of macromolecular biosynthesis; further studies showed that selected compounds inhibited DNA topoisomerase IV, suggesting complex mechanisms of actions for compounds in this series.
Journal ArticleDOI
Design, synthesis and anti-tuberculosis activity of 1-adamantyl-3-heteroaryl ureas with improved in vitro pharmacokinetic properties.
E. Jeffrey North,Michael S. Scherman,David F. Bruhn,Jerrod S. Scarborough,Marcus M. Maddox,Victoria Jones,Anna E. Grzegorzewicz,Lei Yang,Tamara Hess,Christophe Morisseau,Mary Jackson,Michael R. McNeil,Richard E. Lee +12 more
TL;DR: This study produced lead isoxazole, oxadiazole and pyrazole substituted adamantyl ureas with improved in vitro PK profiles, increased selectivity and good anti-TB potencies with sub μg/mL minimum inhibitory concentrations.
Journal ArticleDOI
In vitro and in vivo Evaluation of Synergism between Anti-Tubercular Spectinamides and Non-Classical Tuberculosis Antibiotics
David F. Bruhn,Michael S. Scherman,Jiuyu Liu,Dimitri Scherbakov,Bernd Meibohm,Erik C. Böttger,Anne J. Lenaerts,Richard E. Lee +7 more
TL;DR: Results from this study indicate that a 1599 clarithromycin combination is potentially viable, providing the drug exposures can be carefully monitored, and the importance of validating in vitro synergism and the challenge of matching drug exposures to obtain a synergistic outcome in vivo is highlighted.
Journal ArticleDOI
Antitubercular nitrofuran isoxazolines with improved pharmacokinetic properties
Rakesh,David F. Bruhn,Dora B. Madhura,Marcus M. Maddox,Robin B. Lee,Ashit Trivedi,Lei Yang,Michael S. Scherman,Janet C. Gilliland,Veronica Gruppo,Michael R. McNeil,Anne J. Lenaerts,Bernd Meibohm,Richard E. Lee +13 more
TL;DR: Overall, the addition of solubilizing and metabolically blocked outer rings did improve solubility and decrease protein binding as designed, however, the metabolic stability for compounds in this series was generally lower than desired.