Hao Lin1, David F Bruhn2, Marcus M Maddox2, Aman P Singh2, Richard E Lee2, Dianqing Sun3. 1. Department of Pharmaceutical Sciences, The Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, 34 Rainbow Drive, Hilo, HI 96720, USA. 2. Department of Chemical Biology & Therapeutics, St. Jude Children's Research Hospital, 262 Danny Thomas Place, MS#1000, Memphis, TN 38105, USA. 3. Department of Pharmaceutical Sciences, The Daniel K. Inouye College of Pharmacy, University of Hawai'i at Hilo, 34 Rainbow Drive, Hilo, HI 96720, USA. Electronic address: dianqing@hawaii.edu.
Abstract
Bacterial infections, caused by Mycobacterium tuberculosis and other problematic bacterial pathogens, continue to pose a significant threat to global public health. As such, new chemotype antibacterial agents are desperately needed to fuel and strengthen the antibacterial drug discovery and development pipeline. As part of our antibacterial research program to develop natural product-inspired new antibacterial agents, here we report synthesis, antibacterial evaluation, and structure-activity relationship studies of an extended chemical library of macrocyclic diarylheptanoids with diverse amine, amide, urea, and sulfonamide functionalities. Results of this study have produced macrocyclic geranylamine and 4-fluorophenethylamine substituted derivatives, exhibiting moderate to good activity against M. tuberculosis and selected Gram-positive bacterial pathogens.
Bacterial infections, caused by n class="Species">Mycobacterium tuberculosis and other problematic bacterial pathogens, continue to pose a significant threat to global public health. As such, new chemotype antibacterial agents are desperately needed to fuel and strengthen the antibacterial drug discovery and development pipeline. As part of our antibacterial research program to develop natural product-inspired new antibacterial agents, here we report synthesis, antibacterial evaluation, and structure-activity relationship studies of an extended chemical library of macrocyclic diarylheptanoids with diverse amine, amide, urea, and sulfonamide functionalities. Results of this study have produced macrocyclic geranylamine and 4-fluorophenethylamine substituted derivatives, exhibiting moderate to good activity against M. tuberculosis and selected Gram-positive bacterial pathogens.
Authors: Li Shen; Marcus M Maddox; Sudip Adhikari; David F Bruhn; Manish Kumar; Robin E Lee; Julian G Hurdle; Richard E Lee; Dianqing Sun Journal: J Antibiot (Tokyo) Date: 2013-04-03 Impact factor: 2.649
Authors: Richard E Lee; Julian G Hurdle; Jiuyu Liu; David F Bruhn; Tanja Matt; Michael S Scherman; Bernd Meibohm; Erik C Böttger; Anne J Lenaerts; Pavan K Vaddady; Zhong Zheng; Jianjun Qi; Rashid Akbergenov; Sourav Das; Dora B Madhura; Chetan Rathi; Ashit Trivedi; Cristina Villellas; Robin B Lee; Samanthi L Waidyarachchi; Dianqing Sun; Michael R McNeil; Jose A Ainsa; Helena I Boshoff; Mercedes Gonzalez-Juarrero Journal: Nat Med Date: 2014-01-26 Impact factor: 53.440