Oxazoles

Publication Title: 
Journal of the American Chemical Society

Although the antimalarial agent artemisinin itself is not active against tuberculosis, conjugation to a mycobacterial-specific siderophore (microbial iron chelator) analogue induces significant and selective antituberculosis activity, including activity against multi- and extensively drug-resistant strains of Mycobacterium tuberculosis. The conjugate also retains potent antimalarial activity.

Author(s): 
Miller, Marvin J.
Walz, Andrew J.
Zhu, Helen
Wu, Chunrui
Moraski, Garrett
Möllmann, Ute
Tristani, Esther M.
Crumbliss, Alvin L.
Ferdig, Michael T.
Checkley, Lisa
Edwards, Rachel L.
Boshoff, Helena I.
Publication Title: 
The Journal of Organic Chemistry

The Pd-catalyzed TBHP-mediated Wacker-type oxidation of internal alkenes is reported. The reaction uses 2-(4,5-dihydro-2-oxazolyl)quinoline (Quinox) as ligand and TBHP(aq) as oxidant to deliver single ketone constitutional isomer products in a predictable fashion from electronically biased olefins. This methodology is showcased through its application on an advanced intermediate in the total synthesis of the antimalarial drug artemisinin.

Author(s): 
DeLuca, Ryan J.
Edwards, Jennifer L.
Steffens, Laura D.
Michel, Brian W.
Qiao, Xiaoxiao
Zhu, Chunyin
Cook, Silas P.
Sigman, Matthew S.
Publication Title: 
PloS One

Estrogens are used extensively to treat hot flashes in menopausal women. Some of the beneficial effects of estrogens in hormone therapy on the brain might be due to nongenomic effects in neurons such as the rapid stimulation of calcium oscillations. Most studies have examined the nongenomic effects of estrogen receptors (ER) in primary neurons or brain slices from the rodent brain. However, these cells can not be maintained continuously in culture because neurons are post-mitotic.

Author(s): 
Zhang, Lili
Blackman, Brigitte E.
Schonemann, Marcus D.
Zogovic-Kapsalis, Tatjana
Pan, Xiaoyu
Tagliaferri, Mary
Harris, Heather A.
Cohen, Isaac
Pera, Renee A. Reijo
Mellon, Synthia H.
Weiner, Richard I.
Leitman, Dale C.
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