今月（2022年9月）になって新しい論文が出ましたが、おそらくこれが最後になるのではないかと思われますので、これまでのpublicationを記しておきます。全部で35報になりました。
Anacor関連が25報。それらのうち18報で共著者となった元同僚で同い年のケミスト、YK Zhangが今月他界されました。彼への追悼の思いも込めて。
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Padilla,A. M.; Wang, W.; Akama, T.; Carter, D. S.; Easom, E.; Freund, Y.;Halladay, J. S.; Liu, Y.; Hamer, S. A.; Hodo, C. L.; Wilkerson, G. K.; Orr, D.;White, B.; George, A.; Shen, H.; Jin, Y.; Wang, M. .; Tse, S.; Jacobs, R. T.;Tarleton, R. Discovery of an orallyactive benzoxaborole prodrug effective in the treatment of Chagas disease innon-human primates. Nat. Microbiol. 2022, https://doi.org/10.1038/s41564-022-01211-y(2) Akama, T.; Freund, Y. R.; Berry,P. W.; Carter, D. S.; Easom, E. E.; Jarnagin ,K.; Lunde, C. S.; Plattner, J.J.; Rock, F.; Stefanakis, R.; Ficher, C.; Bulman, C. A.; Lim, K. C.; Suzuki, B.M.; Tricoche, N.; Mansour, A.; DiCosty, U.; McCall, S.; McCall, B. C. J. W.;McKerrow, J.; Hubner, M. P.; Specht, S.; Hoerauf ,A.; Lustigman, S.; Sakanari,J. A.; Jacobs, R. T. Macrofilaricidal Benzimidazole−BenzoxaboroleHybrids as an Approach to the Treatment of River Blindness: Part 1. AmideLinked Analog. ACS Infect. Dis. 2020, 6, 173-179.
(3) Carter,D. S.; Jacobs, R. T.; Freund, Y. R.; Berry, P. W.; Akama, T.; Easom, E. E.; Jarnagin ,K.; Lunde, C. S.; Rock, F.;Stefanakis, R.; McKerrow, J.; Ficher, C.; Bulman, C. A.; Lim, K. C.; Suzuki, B.M.; Tricoche, N.; Sakanari, J. A.; Lustigman, S.; Plattner, J. J. MacrofilaricidalBenzimidazole−BenzoxaboroleHybrids as an Approach to the Treatment of River Blindness: Part 2. KetoneLinked Analog. ACS Infect. Dis. 2020, 6, 180-185.
(4) Akama, T.; Zhang, YK; Freund, Y.R.; Berry, P.; Lee, J.; Easom, E. E.; Jacobs, R. T.; Plattner, J. J.; Witty, M.J.; Peter, R.; Rowan, T. G.; Gillingwater, K.; Brun, R.; Nare, B.; Mercer, L.,Xu, M.; Wang, J.; Liang, H. Identificationof a 4-fluorobenzyl l-valinate amide benzoxaborole (AN11736) as a potentialdevelopmental candidate for the treatment of Animal African Trypanosimiasis(AAT). Bioorganic. Med. Chem. Lett. 2018, 28(1), 6-10.
(5) Hernandez,V.; Akama, T.; Li ,X.; Perry, M.;Xia, Y.; Zhang, YK. Boron in medicinalchemistry. 2016 MEDICINAL CHEMISTRYREVIEWS, 2016, 51, 329–344.
(6) Dong,C.; Virtucio, C.; Zemska, O.; Baltazar, G.; Zhou, Y.; Baia, D.; Jones-Iatauro,S.; Sexton, H.; Martin, S.; Dee, J.; Makl, Y.; Meewan, M.; Rock. F.; Akama, T.; Jarnagin, K. Treatment of skin inflammation withbenzoxaborole phosphodiesterase inhibitors: selectivity, cellular activity, andeffect on cytokines associated with skin inflammation and skin architecturechanges. J. Phram. Exp. Ther. 2016,358(3),413–422.
(7) Zhang,YK.; Plattner, J. J.; Easom, E. E.; Akama,T.; Zhou, Y.; White, W. H.; Defauw, J. M.; Winkle, J. R.; Balko, T. W.;Cao, J.; Ge, Z.; Yang, J. Optimizationof isoxazolin amide benzoxaboroles for identification of a developmentcandidate as an oral long acting animal ectoparasiticide. BioorgMed. Chem. Lett. 2016, 26(13), 3182–3186.
(8) Zhang,YK.; Plattner, J. J.; Easom, E. E.; Zhou, Y.; Akama, T.; Bu, W.; White, W. H.; Defauw, J. M.; Winkle, J. R.;Balko, T. W.; Guo, S.; Xue, J.; Cao, J.; Zou, W. Discovery of an orally bioavailableisoxazoline benzoxaborole (AN8030) as a long acting animal ectoparasiticide. BioorgMed. Chem. Lett. 2015, 25(23), 5589–5593.
(9) Akama, T.; Dong, C.; Virtucio, C.; Sullivan,D.; Zhou, Y.; Zhang, Y-K.; Rock, F.; Freund, Y. R.; Bu, W.; Wu, A.; Liu L.; Fan,X-Q.; Jarnagin, K. Linking phenotype tokinase: Identification fo a novel benzoxaborole hinge binding motif for kinaseinhibition and the development of high potency rho-kinase inhibitors. J.Phram. Exp. Ther. 2013, 347(3), 615–625.
(10) Akama, T.; Dong, C.; Virtucio, C.;Freund, Y. R.,; Chen, D.; Orr, M.D.; Jacobs, R.T.; Zhang, Y-K.; Hernandez, V.; Liu, Y.; Wu, A.; Liu L.; Jarnagin, K.; Plattner, J. J. Discovery and structure–activity relationships of6-(benzoylamino)benzoxaboroles as orally active anti-inflammatory agents. Bioorg. Med. Chem. Lett. 2013,23, 5870–5873.
(11) Hernandez, V.; Crepin, T.; Palencia, A.; Cusack, S.; Akama, T.; Baker, S. J.; Bu .W.; Feng,L.; Freund, Y. R.; Liu, L.; Meewan, M.; Mohan, M.; Mao,W.; Rock, F. L.; Sexton, H.; Sheoran, A.; Zhang, Y.; Zhang, Y-K.; Zhou, Y.;Nieman, J. A.; Anugula, M. R.; Keramane, E. M.; Savariraj, K.; Redy, D. S.;Sharma, R.; Subedi, R.; Singh, R.; O’Leary, A.; Simon, N. L.; De Marsh, P. L.;Mushtag, S.; Warner, M.; Livermore, D. M.; Alley, M. R. K.; Plattner, J.J. Discovery of a novelclass of boron-based antibacterials with activity against gram-negativebacteria. Antimicrob. Agents Chemither. 2013, 57(3), 1394–1403.
(12) Dong,C.; Sexton, H.; Gertrudes, A.; Akama, T.;Martin, S.; Virtucio, C.; Chen, C-W.; Fan, X.; Wu A.; Bu, W.; Liu, L.; Feng,L.; Jarnagin, K.; Freunf, Y. Inhibitionof Toll-Like Receptor mediated inflammation in vitro and in vivo by a novelbenzoxaborole. J. Phram. Exp. Ther. 2013,344(2),436–446.
(13) Akama, T.; Virtucio, C.; Dong, C.;Kimura, R.; Zhang, Y-K.; Nieman, J. A.; Shamra, R.; Lu, X.; Sales, M.; Singh, R.;Wu, A.; Fan, X-Q.; Liu, L.; Plattner, J. J.; Jarnagin, K.; Freund, Y. R. Structure-activity relationships of6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatoryagent. Bioorg. Med. Chem. Lett. 2013, 23, 1680–1683.
(14) Freund, Y. R.; Akama,T.; Alley, M. R. K.; Antunes, J.; Dong, C.; Jarnagin, K.; Kimura, R.;Nieman, J. A.; Maples, K. R.; Plattner, J. J.; Rock, F.; Sharma, R.; Singh, R.;Sanders, V.; Zhou, Y.; Boron-based phosphodiesterase inhibitors show novelbinding of boron to PDE4 bimetal center. FEBS Lett. 2012,586, 3410–3414.
(15) Bu, W.; Akama,T.; Chanda, S.; Sullivan, D.; Ciaravino, V.; Jarnagin, K.; Freund, Y.;Sanders, V.; Chen, C-W.; Fan, X.; Heyman, I.;Liu, L. Early rapid identification of in vivo rat metabolism of AN6414, anovel boron-containing PDE4 inhibitor by QTRAP LC/MS/MS to support drugdiscovery. J. Pharm. Biomed. Anal. 2012, 70, 344–353.
(16) Jacobs, R. T.; Nare, B.; Wring, S. A.; Orr, M. D.;Chen, D.; Sliger, J. M.; Jenks, M. X.; Noe, R. A.; Bowling, T. S.; Mercer, L.T.; Rewerts, C.; Gaukel, E.; Owens, J.; Parham, R.; Randolph, R.; Beaudet, B.;Bacchi, C. J.; Yarlett, N.; Plattner, J. J.; Freund, Y.; Ding, C.; Akama, T.; Zhang, Y-K.; Brun, R.;Kaiser, M.; Scandale, I.; Don, R. SCYX-7157, an Orally- Active Benzoxaborole for the Treatment of Stage 2Human African Trypanosimiasis. PLoS Negrected Tropical Diseases, 2011, 5(6), e1151.
(17) Zhang, Y-K.; Plattner, J. J.; Akama, T.; Baker, S. J.;Hernandez, V. S.; Sanders, V.; Freund, Y.; Kimura, R.; Bu W.; Hold, K. M.; Lu,X-S. Design and synthesis ofboron-containing PDE4 inhibitors using soft-drug strategy for potentialdermatologic anti-inflammatory application. Bioorg. Med. Chem. Lett. 2010,20, 2270–2274. (18) Baker, S. J.; Ding, C. Z.; Akama, T.; Zhang, Y-K.; Hernandez,V. S.; Xia, Y. Therapeutic potential ofboron-containing compounds. (Review) Future Med. Chem. 2009, 1(7), 1275–1288.
(19) Akama, T.; Baker, S. J.; Zhang, Y-K.; Hernandez,V. S.; Zhou, H.; Sanders, V.; Freund, Y.; Kimura, R.; Maples, K. R..; Plattner, J. J. Discovery and structure-activity study of anovel benzoxaborole anti-inflammatory agent (AN2728) for the topical treatmentof psoriasis and atopic dermatitis. Bioorg. Med. Chem. Lett. 2009,19(8), 2129–2132.
(20) Hui, X.; Baker, S. J.; Wester, R. C.; Barbadillo, S.;Cashmore, A. K.; Sanders, V.; Hold, K. M.; Akama,T.; Zhang, Y-K.; Plattner, J. J.; Maibach, H. I. In vitro penetration of a novel oxaboroleantifungal (AN2690) into the human nail plate. J. Pharm. Sci. 2007,96, 2622–2631.
(21) Baker, S. J.; Zhang, Y-K.; Akama, T.; Wheeler, C.; Plattner, J. J.; Rosser, R. M.; Reid, R.P.; Nixon, N. S. Synthesis ofisotopically labeled (3-14C)- and (3,3-2H2)-5-fluoro,1,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2690), a new antifungal agent forthe potential treatment of onychomycosis. J. Label. Compd. Radiopharm., 2007, 50, 245–250.
(22) Rock, F. L.; Mao, W.; Yaremchuk, A.; Tukalo, M.; Crépin, T.; Zhou, H.; Zhang,Y-K.; Hernandez, V.; Akama, T.;Baker, S. J.; Plattner, J. J.; Shapiro, L.; Martinis, S.; Benkovic, S. J.;Alley, M. R. K. An Antifungal AgentInhibits an Aminoacyl-tRNA Synthase by Trapping tRNA in the Editing Site. Science,2007, 316, 1759-1761.
(23) Baker, S. J.; Akama,T.; Zhang, Y-K.; Sauro, V.; Pandit, C.; Singh, R.; Kully, M.; Khan, J.;Plattner, J. J.; Benkovic, S. J.; Lee, V.; Maples, K. Identification of a novel boron-containingantibacterial agent (AN0128) with anti-inflammatory activity, for the potentialtreatment of cutaneous diseases. Bioorg. Med. Chem. Lett. 2006,16, 5963–5967.
(24) Baker, S. J.; Zhang, Y-K.; Akama, T.; Lau A.; Zhou, H.; Hernandez, V.; Mao, W.; Alley, M. R.K.; Sanders, V.; Plattner, J. J. Discovery of a New Boron-Containing Antifungal Agent,5-Fluoro-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2690), for the PotentialTreatment of Onychomycosis. J. Med. Chem. 2006,49, 4447–4450.
(25) Benkovic, S. J.; Baker, S. J.; Alley, M. R. K.; Woo,Y-H.; Zhang, Y-K.; Akama, T.; Mao,W.; Bavoval, J.; Rajagopalan, P. T. R.; Wall, M.; Kahng, L. S.; Tavassoli, A.;Shapiro, L. Identification of BorinicEsters as Inhibitors of Bacterial Cell Growth and Bacterial Methyltransferases,CcrM and MenH. J. Med. Chem. 2005,48, 7468–7476.
(26) Agatsuma, T.; Akama, T.; Nara, S.; Matsumiya,S.; Nakai, R.; Ogawa, H.; Otaki, S.; Ikeda, S.; Saitoh, Y.; Kanda, Y. UCS1025A and B, New Antitumor Antibioticsfrom the Fungus Acremonium Species. Org. Lett. 2002, 12,4387–4390.
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(28) Akama, T.; Ueno, K.; Saito, H.; Kasai, M. Synthesis of an Ethyl 6-Amino-3,5-difluorosalicylate Derivative bySequential Regioselective Directed ortho-Metalation;A Practical Synthesis of 4’,5-Amino-3’,6,8-trifluoroflavone, A Potent AntitumorAgent. Synthesis, 1997,1446-1450.
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(30) Akama, T.; Shida, Y.; Sugaya, T.;Ishida, H.; Gomi, K.; Kasai, M. Novel 5-Aminoflavone Derivatives as SpecificAntitumor Agents in Breast Cancer. J. Med. Chem. 1996,39(18), 3461-3469.
(31) Hagiwara, H.; Akama,T.; Okano, A.; Uda, H. Annulation bySequential Double Michael Reaction; Synthesis of Decalones and Its Applicationto the Synthesis of e-Cadinene, Khusitone, and Khusilal. J.Chem. Soc., Perkin Trans. 1 1993,2173-2184.
(32) Hagiwara, H; Akama,T.; Okano, A.; Uda, H. AssymmetricTwo-fold Michael Reaction. Synthesis ofOptically Active 4-Substituted 1-Decalones from Trimethylsilyl Enol Ether of1-Acetylcyclohexene. Chem. Lett. 1989,2149-2152.
(33) Hagiwara, H; Akama,T.; Okano, A.; Uda, H. Synthesis of(±)-Khusial. Chem.Lett. 1988, 2067-2068.
(34) Hagiwara, H; Akama,T.; Okano, A.; Uda, H. Synthesis ofSubstituted 2-Decalones from 1-Acetylcyclohexenes and a-Trimethylsilyl ab-Unsaturated CarbonylCompounds by Two-fold Michael Reactions. Synthesis of (±)-Khusitone. Chem. Lett. 1988,1793-1796.
(35) Hagiwara, H.; Okano, A.; Akama, T.; Uda, H. LewisAcid Assisted Annelation of Trimethylsilyl Enol Ethers of 1-Acetylcyclohexeneswith ab-Unsaturated CarbonylCompounds to Give Substituted 2-Decalones; Synthesis of (±)-e-Cadinene. J. Chem. Soc., Chem. Commun. 1987,1333-1335.
