Chance, Jeffrey P Fejzic, Hannah Hernandez, Obiel Istvan, Eva S Andaya, Armann Maslov, Nikolay Aispuro, Ruby Crisanto, Teodulo Nguyen, Huyen Vidal, Brian
...
Published in
Bioorganic & medicinal chemistry letters
The human parasite Plasmodium falciparum kills an estimated 445,000 people a year, with the most fatalities occurring in African children. Previous studies identified falcilysin (FLN) as a malarial metalloprotease essential for parasite development in the human host. Despite its essentiality, the biological roles of this protease are not well under...
Matsushita, Takahiko Tsuchibuchi, Koji Koyama, Tetsuo Hatano, Ken Matsuoka, Koji
Published in
Bioorganic & medicinal chemistry letters
Bivalent glycoconjugates have a minimal valence with avidity potential on protein-carbohydrate interactions as well as simplicity of chemical structures enabling simple synthesis with low cost. Understanding the way to maximize the affinities of bivalent glycoconjugates is important for the development of cost-effective tools for therapeutic and di...
Upadhyay, Anup K Judge, Russell A Li, Leiming Pithawalla, Ron Simanis, Justin Bodelle, Pierre M Marin, Violeta L Henry, Rodger F Petros, Andrew M Sun, Chaohong
...
Published in
Bioorganic & medicinal chemistry letters
The tandem TUDOR domains present in the non-catalytic C-terminal half of the KDM4A, 4B and 4C enzymes play important roles in regulating their chromatin localizations and substrate specificities. They achieve this regulatory role by binding to different tri-methylated lysine residues on histone H3 (H3-K4me3, H3-K23me3) and histone H4 (H4-K20me3) de...
Kodani, Sean D Bhakta, Saavan Hwang, Sung Hee Pakhomova, Svetlana Newcomer, Marcia E Morisseau, Christophe Hammock, Bruce D
Published in
Bioorganic & medicinal chemistry letters
Multi-target inhibitors have become increasing popular as a means to leverage the advantages of poly-pharmacology while simplifying drug delivery. Here, we describe dual inhibitors for soluble epoxide hydrolase (sEH) and fatty acid amide hydrolase (FAAH), two targets known to synergize when treating inflammatory and neuropathic pain. The structure ...
Pinkerton, Anthony B Sergienko, Eduard Bravo, Yalda Dahl, Russell Ma, Chen-Ting Sun, Qing Jackson, Michael R Cosford, Nicholas D P Millán, José Luis
Published in
Bioorganic & medicinal chemistry letters
Tissue-nonspecific alkaline phosphatase (TNAP) is an ectoenzyme crucial for bone matrix mineralization via its ability to hydrolyze extracellular inorganic pyrophosphate (ePPi), a potent mineralization inhibitor, to phosphate (Pi). By the controlled hydrolysis of ePPi, TNAP maintains the correct ratio of Pi to ePPi and therefore enables normal skel...
Akama, Tsutomu Zhang, Yong-Kang Freund, Yvonne R Berry, Pamela Lee, Joanne Easom, Eric E Jacobs, Robert T Plattner, Jacob J Witty, Michael J Peter, Rosemary
...
Published in
Bioorganic & medicinal chemistry letters
Novel l-valinate amide benzoxaboroles and analogues were designed and synthesized for a structure-activity-relationship (SAR) investigation to optimize the growth inhibitory activity against Trypanosoma congolense (T. congolense) and Trypanosoma vivax (T. vivax) parasites. The study identified 4-fluorobenzyl (1-hydroxy-7-methyl-1,3-dihydrobenzo[c][...
Hu, Xiao He, Yanhua Wu, Liping Hao, Yujun Wang, Zhenghe Zheng, Weiping
Published in
Bioorganic & medicinal chemistry letters
To follow up on our recent discovery of the 18-amino acid all-hydrocarbon [i, i + 4]-stapled p110α[E545K] peptide 1 that was shown to potently block the intracellular p110α[E545K]-IRS1 interaction (a protein-protein interaction uniquely present in cancer cells expressing p110α[E545K]) and the growth of the xenograft tumors formed by cancers harbori...
Bennett, Frank Buevich, Alexei V Huang, Hsueh-Cheng Girijavallabhan, Vinay Kerekes, Angela D Huang, Yuhua Malikzay, Asra Smith, Elizabeth Ferrari, Eric Senior, Mary
...
Published in
Bioorganic & medicinal chemistry letters
(2'R)-Ethynyl uridine 3, and its (2'S)-diastereomer 10, are synthesised in a divergent fashion from the inexpensive parent nucleoside. Both nucleoside analogues are obtained from a total of 5 simple synthetic steps and 3 trivial column chromatography purifications. To evaluate their effectiveness against HCV NS5B polymerase, the nucleosides were co...
Silva, Daniel G Ribeiro, Jean F R De Vita, Daniela Cianni, Lorenzo Franco, Caio Haddad Freitas-Junior, Lucio H Moraes, Carolina Borsoi Rocha, Josmar R Burtoloso, Antonio C B Kenny, Peter W
...
Published in
Bioorganic & medicinal chemistry letters
The effects on potency of cruzain inhibition of replacing a nitrile group with alternative warheads were explored. The oxime was almost an order of magnitude more potent than the corresponding nitrile and has the potential to provide access to the prime side of the catalytic site. Dipeptide aldehydes and azadipeptide nitriles were found to be two o...
Zhang, Bo-Wei Xing, Yan Wen, Chen Yu, Xiao-Xia Sun, Wen-Long Xiu, Zhi-Long Dong, Yue-Sheng
Published in
Bioorganic & medicinal chemistry letters
In this paper, the inhibition of α-amylase and α-glucosidase by nine pentacyclic triterpenes was determined. For α-amylase inhibitory activity, the IC50 values of ursolic acid, corosolic acid, and oleanolic acid were 22.6±2.4μM, 31.2±3.4μM, and 94.1±6.7μM, respectively. For α-glucosidase inhibition, the IC50 values of ursolic acid, corosolic acid, ...
