2018

 

 

Pharmacological characterization of the neurotrophic sesquiterpene jiadifenolide reveals a non-convulsant signature and potential for progression in neurodegenerative disease studies.

Witkin J. M.; Shenvi, R. A.; Li X.; Gleason, S. D.; Weiss J.; Morrow D.; Gatow J. T.; Wakulchik M.; Ohtawa M.; Lu H-H.; Martinez, M. D.; Schkeryantz J. M.; Garpenter T. S.; Cerne R Biochemical Pharmacology, 155, 61-70, 2018

 

Transient Phenotypic Changes in Endothelial Cells and Pericytes in Neonatal Mouse Retina Following Short-term Blockade of Vascular Endothelial Growth Factor Receptors.

Morita A.; Mori A.; Arima S.; Sakamoto K.; Nagamitsu T.; Ishii K.; Nakahara T. Developmental Dynamics, 247, 699-711, 2018.

 

Establishment of an abnormal vascular patterning model in the mouse retina.

Morita A.; Sawada S; Mori A.; Arima S.; Sakamoto K.; Nagamitsu  T.; Nakahara T.  Journal of Pharmacological Sciences, 136, 177-188, 2018.

 

Design and synthesis of A-ring simplified Pyripyropene A analogs as potent and selective synthetic SOAT2 inhibitors.

Ohtawa M.; Arima S.; Ichida N.; Terayama T; Ohno H.; Yamazaki T.; Ohshiro T.; Sato N.; Omura S.; Tomoda H.; Nagamitsu T. ChemMedChem, 13, 411-421, 2018.

This paper was chosen as the front cover.

 

 

2017

 

オキシピリジン化合物及びアトペニン類縁体の製造方法

長光亨大多和正樹. 特願2017-233415

 

Scopranones with the two atypical scoop-like moieties produced by Streptomyces sp. BYK-11038.

Uchida R.; Lee D.; Suwa I.; Ohtawa M.; Watanabe N.; Demachi A.; Ohte S.; Katagiri T.; Nagamitsu T.; Tomoda H. Organic Letters, 19, 5980-5983, 2017.

 

Deprotection of silyl ethers by using SO3H silica gel: Application to sugar, nucleoside and alkaloid derivatives.

Fujii H.; Shimada N.; Ohtawa M.; Karaki F.; Koshizuka M.; Hayashida K.; Kamimura M.; Makino K.; Nagamitsu T.; Nagase H. Tetrahedron, 73, 5425-5429, 2017.

 

Synthesis of (–)-11-O-debenzoyltashironin: Neurotrophic sesquiterpenes cause hyperexcitation.

Ohtawa M.; Krambis M. J.; Cerne R.; Schkeryantz J. M.; Witkin J. M.; Shenvi R. A. Journal of the American Chemical Society, 139, 9637-9644, 2017.

– Among the top 20 most read article on J. Am. Chem. Soc. for July 2017 –

 

Development of a new air-stable structure-simplified nafuredin-γ analog as a potent and selective nematode complex I inhibitor.

Ohtawa M.; Arima S.; Shimizu R.; Hanatani N.; Shimizu E.; Shiomi K.; Kita K.; Omura S.; Nagamitsu T. Journal of Antibiotics, 70, 647-654, 2017.

 

A delay in vascularization induces abnormal astrocyte proliferlation and migration in the mouse retina.

Morita A.; Ushikubo H.; Mori A.; Arima S.; Sakamoto K.; Nagamitsu T.; Ishii K.; Nakahara T. Developmental Dynamics, 246, 186-200, 2017.

 

 

2016

 

骨代謝阻害活性を有する新規化合物及びその製造方法

供田 洋、内田 龍児、長光 大多和正樹、片桐 岳信 特願2016-250667/特開2017-119691

 

 

 

Simplifungin and valsafungins, antifungal antibiotics of fungal origin.

Ishijima H.; Uchida R.; Ohtawa M.; Kondo A.; Nagai K.; Shima K.; Nonaka K.; Masuma R.; Iwamoto S.; Onodera H.; Nagamitsu T.Tomoda H. Journal of Organic Chemistry, 81, 7373-7383, 2016.

 

Synthesis and Structural Revision of Cyslabdan.

Ohtawa, M.; Hishinuma, Y.; Takagi, E.; Yamada, T.; Ito, F.; Arima, S.; Uchida, R.; Kim, Y. -P.; Omura, S.; Tomoda, T.; Nagamitsu, T. Chemical & Pharmaceutical Bulletin, 64, 1370-1377, 2016.

 

Biosynthesis of mercapturic acid derivative of the labdane‑type diterpene, cyslabdan that potentiates imipenem activity against methicillin‑resistant Staphylococcus aureus: cyslabdan is generated by mycothiol‑mediated xenobiotic detoxification.

Ikeda, H.; Shin-ya, K.; Nagamitsu, T.Tomoda, H. Journal of Industrial Microbiology &

Biotechnology, 43, 325–342, 2016.

 

 

2015

 

New pyripyropene derivatives, highly SOAT2-selective inhibitors, improve hypercholesterolemia and atherosclerosis in atherogenic mouse model.

Ohshiro, T.; Ohtawa, M.; Nagamitsu, T.; Matsuda, D.; Yagyu, H.; Davis, M. A.; Rudel, L. L.; Ishibashi, S.; Tomoda, H. Journal of Pharmacology and Experimental Therapeutics, 355, 299-309, 2015.

 

Total synthesis of (+)-clavulatriene A.

Ito, F.; Ohbatake, Y.; Aoyama, S.; Ikeda, T.; Arima, S.; Yamada, Y.; Ikeda, H.; Nagamitsu, T.  Synthesis, 47(9), 1348-1355, 2015.

 

Design, synthesis, and biological evaluation of air-stable nafuredin-γ analogs as complex I inhibitors.

Ohtawa, M.; Matsunaga, M.; Fukunaga, K.; Shimizu, R.; Shimizu, E.; Arima, S.; Ohmori, J.; Kita, K.; Shiomi, K.; Omura, S.; Nagamitsu, T. Bioorganic & Medicinal Chemistry, 23(5), 932-943, 2015.

Novel terpenes generated by heterologous expression of bacterial terpene synthase genes in an engineered Streptomyces host.

Yamada, Y.; Arima, S.; Nagamitsu, T.; Johmoto, K.; Uekusa, H.; Eguchi, T.; Shin'ya, K.; Cane, D. E.; Ikeda, H. Journal of Antibiotics, 68, 385-394, 2015.

 

Synthesis and biological activity of 5-(4-methoxyphenyl)-oxazole derivatives.

Yamamuro, D.; Uchida, R.; Ohtawa, M.; Arima, S.; Futamura, Y.; Katane, M.; Homma, H.; Nagamitsu, T.; Osada, H.; Tomoda, H. Bioorganic & Medicinal Chemistry Letters, 25, 313-316, 2015.

 

In vitro metabolism of pyripyropene A and ACAT inhibitory activity of its metabolites.

Matsuda, D.; Ohshiro, T.; Ohtawa, M.; Yamazaki, H.; Nagamitsu, T.; Tomoda, H. Journal of Antibiotics, 68, 27-34, 2015.

 

 

2014

 

種選択的な電子伝達系の複合体II阻害活性を有する新規アトペニン類縁体

長光 大多和正樹有馬 志保、塩見和朗、大村 智  特願2014-259956

 

Treatment of mild-pregnant mice with KRN633, an inhibitor of vascular endothelial growth factor receptor tyrosine kinase, induces abnormal retinal vascular patterning in their newborn pups.

Morita, A.; Nakahara, T.; Abe, N.; Kurauchi, Y.; Mori, A.; Sakamoto, K.; Nagamitsu, T.; Ishii, K. Birth Defects Research Part B: Developmental and Reproductive Toxicology, 101(4), 293-299, 2014.

 

ACAT2 選択的阻害剤ピリピロペン A の構造簡略型誘導体創製研究

大多和正樹、大村 智、供田 洋、長光  MEDCHEMNEWS, 24(3), 25-31, 2014.

 

コレステロールアシル転移酵素アイソザイム2 (ACAT2) 阻害活性を有する新規医薬化合物

供田 洋、 大多和正樹、大村 智、長光 特願2014-129126

 

Synthesis and biological activity of citridone A and its derivatives.

Fukuda, T.; Shimoyama, K.; Nagamitsu, T.; Tomoda, H. Journal of Antibiotics, 67(6), 445-450, 2014.

 

Effects of pre- and post- natal treatment with KRN633, an inhibitor of vascular endothelial growth factor recepter tyrosine kinase, on retinal vascular development and patterning in mice.

Morita, A.; Nakahara, T.; Abe, N.; Kurauchi, Y.; Mori, A.; Sakamoto, K.; Nagamitsu, T.; Ishii, K. Experimental Eye Research, 120, 127-137, 2014.

 

Regioselective Mono-deprotection of Di-tert-butylsilylene acetal derived from 1,3-diol with ammonium fluoride.

Ohtawa, M.; Tomoda, H.; Nagamitsu, T. Bulletin of the Chemical Society of Japan, 87(1), 113-118, 2014.

 

 

2013

 

KRN633, an inhibitor of vascular endothelial growth factor receptor tyrosine kinase, induces intrauterine growth restriction in mice.

Abe, N.; Nakahara, T.; Morita, Y.; Mori, A.; Sakamoto, K.; Nagamitsu, T.; Ishii, K. Birth Defects Research Part B: Developmental and Reproductive Toxicology, 98(4), 297-303, 2013.

 

新規脂質異常症予防治療薬を指向した ACAT2 選択的阻害剤ピリピロペン A の構造活性相関研究 

大多和正樹、大村 智、供田 洋、長光  有機合成化学協会誌, 8(8), 830-843, 2013.

 

Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective Acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: Part 3.

Ohtawa, M.; Yamazaki, H.; Matsuda, D.; Ohshiro, T.; Rudel, L. L.; Omura, S.; Tomoda, H.; Nagamitsu, T. Bioorganic & Medicinal Chemistry Letters, 23(13), 3798-3801, 2013.

 

Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective Acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: Part 2.

Ohtawa, M.; Yamazaki, H.; Matsuda, D.; Ohshiro, T.; Rudel, L. L.; Omura, S.; Tomoda, H.; Nagamitsu, T. Bioorganic & Medicinal Chemistry Letters, 23(9), 2659-2662, 2013.

 

Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective Acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: Part 1.

Ohtawa, M.; Yamazaki, H.; Ohte, S.; Matsuda, D.; Ohshiro, T.; Rudel, L. L.; Omura, S.; Tomoda, H.; Nagamitsu, T. Bioorganic & Medicinal Chemistry Letters, 23(5), 1285-1287, 2013.

 

Role of vascular endothelial growth factor in maintenance of pregnancy in mice.

Wada, Y.; Ozaki, H.; Abe, N.; Mori, A.; Sakamoto, K.; Nagamitsu, T.; Nakahara, T.; Ishii, K. Endocrinology, 154(2), 900-910, 2013.

 

ACAT2 阻害活性を有するピリピロペンA構造簡略型誘導体

大多和正樹供田 洋、大村 智、長光 特願2013-012868

 

 

2012

 

Stereoselective total synthesis of atpenins A4 and B, harzianopyridone, and NBRI23477 B.

Ohtawa, M.; Sugiyama, K.; Hiura, T.; Izawa, S.; Shiomi, K.; Omura, S.; Nagamitsu, T. Chemical & Pharmaceutical Bulletin, 60(7), 898-906, 2012.

 

Potentiation of bleomycin in Jurket cells by fungal pycnidione.

Kaneko, M.;Matsuda, D.; Ohtawa, M.; Fukuda, T.; Nagamitsu, T.; Yamori, T.; Tomoda, H. Biological & Pharmaceutical Bulletin, 35(1), 18-21, 2012.

 

 

2011

 

Total synthesis and absolute configuration of avenolide, extracellular factor in Streptomyces avermitilis.

Uchida, M.; Takamatsu, S.; Arima, S.; Miyamoto, T. K; Kitani, S.; Nihara, T.; Ikeda, H.; Nagamitsu, T. Journal of Antibiotics, 64(12), 781-787, 2011.

 

Avenolide, a Streptomyces hormone controlling antibiotic production in Streptomyces avermitilis.

Kitani, S.; Miyamoto, T. K; Takamatsu, S.; Herawati, E.; Iguchi, H.; Noshitomi, K.; Uchida, M.;  Nagamitsu, T.; Omura, S.; Ikeda, H.; Nihira, T. Proceedings of the National Academy of Sciences of the United States of America, 108(39), 16410-16415, 2011.

 

Total synthesis of pyripyropene A.

Odani, A.; Ishihara, K.; Ohtawa, M.; Tomoda, H.; Omura, S.; Nagamitsu, T. Tetrahedron, 67(42), 8195-8203, 2011.

 

Total synthesis of citridone A.

Miyagawa, T.; Nagai, K.; Yamada, A.; Sugihara, Y.; Fukuda, T.; Fukuda, T.; Uchida, R.; Tomoda, H.; Omura, S.; Nagamitsu, T. Organic Letters, 13(5), 1158-1161, 2011.

 

 

2010

 

ACAT2阻害活性を有する代謝酵素に安定なピリピロペン誘導体

供田洋、長光亨、松田大介、大城太一、大多和正樹、大村智. 特願2010-82784

 

ACAT2阻害活性を有する水酸基含有ピリピロペン誘導体

供田洋、長光亨、松田大介、大城太一、大多和正樹、大村智. PCT/JP2010/060461

 

Effect of KRN633, an inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase, on vascular development of placenta and fetus of mid pregnancy in mice.

Wada, Y.; Ozaki, H.; Abe, N.; Nagamitsu, T.; Ohta, H.; Nakahara, T.; Ishii, K. Journal of Pharmacological Sciences, 112(3), 290-298, 2010.

 

Structure and total synthesis of fungal calpinactam, a new antimycobacterial agent.

Koyama, N.; Kojima, S.; Fukuda, T.; Nagamitsu, T.; Yasuhara, T.;Omura, S.; Tomoda, H. Organic Letters, 12(3), 432-435, 2010.