Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Masakazu, Atobe"'
Autor:
S. Paul Jones, James D. Firth, Mary C. Wheldon, Masakazu Atobe, Roderick E. Hubbard, David C. Blakemore, Claudia De Fusco, Simon C. C. Lucas, Stephen D. Roughley, Lewis R. Vidler, Maria Ann Whatton, Alison J.-A. Woolford, Gail L. Wrigley, Peter O'Brien
Publikováno v:
RSC medicinal chemistry. 13(12)
Fragment-based drug discovery is now widely adopted for lead generation in the pharmaceutical industry. However, fragment screening collections are often predominantly populated with flat, 2D molecules. Herein, we report the synthesis of piperidine-b
Autor:
Shino Bito, Toshiaki Yamaura, Kenichiro Takaba, Takayuki Serizawa, Atsutoshi Tazumi, Masashi Ishiguro, Eiichi Tanaka, Natsumi Yamakawa, Yukiko Nagano, Masashi Kawanishi, Masakazu Atobe
Publikováno v:
Journal of Medicinal Chemistry. 63:7143-7162
Two chemical series of novel protein kinase C ζ (PKCζ) inhibitors, 4,6-disubstituted and 5,7-disubstituted isoquinolines, were rapidly identified using our fragment merging strategy. This methodology involves biochemical screening of a high concent
Autor:
Alison Jo-Anne Woolford, Stephen D. Roughley, Paul S. Bond, Ngai S. Chan, Mary C. Wheldon, S. Paul Jones, Hanna F. Klein, Peter O'Brien, James D. Firth, Masakazu Atobe, Lewis R. Vidler, David C. Blakemore, Roderick E. Hubbard, Claudia De Fusco, Laura Waddelove, Gail L. Wrigley, Thomas D. Downes, Maria Ann Whatton
Publikováno v:
Chemistry (Weinheim an Der Bergstrasse, Germany)
Fragment‐based drug discovery is now widely adopted for lead generation in the pharmaceutical industry. However, fragment screening collections are often predominantly populated with flat, 2D molecules. Herein, we describe a workflow for the design
Autor:
Masakazu Atobe, Kenji Naganuma, Takahiko Hayashi, Masashi Kawanishi, Hirokazu Arai, Hiroko Suzuki, Masahiro Nishida
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:2408-2412
We describe a medicinal chemistry approach to the discovery of a novel EP1 antagonist exhibiting high potency and good pharmacokinetics. Our starting point is 1, an EP1 receptor antagonist that exhibits pharmacological efficacy in cystometry models f
Autor:
John F. Darby, James D. Firth, Paul S. Bond, Gideon J. Davies, Roderick E. Hubbard, Peter O'Brien, Masakazu Atobe
Publikováno v:
Chem. Sci.. 8:7772-7779
Modulation of enzyme activity is a powerful means of probing cellular function and can be exploited for diverse applications. Here, we explore a method of enzyme activation where covalent tethering of a small molecule to an enzyme can increase cataly
Autor:
Masakazu Atobe
Publikováno v:
Current topics in medicinal chemistry. 19(24)
Transient receptor potential vanilloid (TRPV) 4 belongs to the TRPV subfamily of TRP ion channels. TRPV4 channels play a critical role in chondrocytes and thus TRPV4 is an attractive target of Disease-Modifying Osteoarthritis Drugs (DMOADs). Initial
Autor:
Masakazu Atobe, Shuji Muramatsu, Masayuki Kitagawa, Hiroko Suzuki, Takamichi Nagami, Atsushi Watanabe, Masashi Ishiguro, Takeshi Ohno, Masashi Kawanishi
Publikováno v:
Journal of medicinal chemistry. 62(3)
Osteoarthritis (OA) is a degenerative disease characterized by joint destruction and loss of cartilage. There are many unmet needs in the treatment of OA and there are few promising candidates for disease-modifying OA drugs, particularly, anabolic ag
Autor:
Masakazu, Atobe, Kenji, Naganuma, Masashi, Kawanishi, Takahiko, Hayashi, Hiroko, Suzuki, Masahiro, Nishida, Hirokazu, Arai
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(14)
We describe a medicinal chemistry approach to the discovery of a novel EP
Autor:
Masahiro Takeda, Makoto Saito, Tokuhito Goto, Takanori Tabata, Yasuhiro Wada, Masashi Kawanishi, Takeshi Ito, Natsumi Yamakawa, Masakazu Atobe, Hirokazu Arai
Publikováno v:
Bioorganicmedicinal chemistry letters. 27(21)
A series of indazole derivatives were identified as Sirt 1 activators though high-throughput screening. Optimization of each substituent on the indazole ring led to the identification of compound 13. Compound 13 appeared to give the best Sirt 1 activ
Autor:
Masashi Kawanishi, Eiichi Tanaka, Shiro Miyoshi, Yoshihito Suenaga, Masakazu Atobe, Shinya Sogame
Publikováno v:
European Journal of Medicinal Chemistry. 71:250-258
We describe a medicinal chemistry approach to generate a series of benzimidazoles bearing thiazolidin-4-one using scaffold hopping from thiazole 1, our previously described thiazole. Our goal was to discover a potent and permeable small-molecule ADAM