Novel synthetic route for antimalarial benzo[a]phenoxazine derivative SSJ-183 and two active metabolites.
-
Mizukawa Y
Drug Discovery Science Research Center, Hoshi University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, Japan; Synstar Japan Co., Ltd, Orbic Bldg 3F, 2-9-46 Sakaecho, Odawara 250-0011, Japan.
-
Ge JF
Drug Discovery Science Research Center, Hoshi University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, Japan; College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou 215006, China.
-
Bakar Md A
Drug Discovery Science Research Center, Hoshi University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, Japan; Center for Advanced Research in Sciences, University of Dhaka, Bangladesh.
-
Itoh I
Drug Discovery Science Research Center, Hoshi University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, Japan; Synstar Japan Co., Ltd, Orbic Bldg 3F, 2-9-46 Sakaecho, Odawara 250-0011, Japan.
-
Scheurer C
Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland; University of Basel, CH-4003 Basel, Switzerland.
-
Wittlin S
Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland; University of Basel, CH-4003 Basel, Switzerland.
-
Brun R
Swiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland; University of Basel, CH-4003 Basel, Switzerland.
-
Matsuoka H
School of Medicine, Department of Infection and Immunity, Division of Medical Zoology, Jichi Medical University, 3311-1 Yakushiji, Shimotsuke-shi 329-0498, Japan.
-
Ihara M
Drug Discovery Science Research Center, Hoshi University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, Japan. Electronic address: m-ihara@hoshi.ac.jp.
Show more…
Published in:
- Bioorganic & medicinal chemistry. - 2014
English
A productive synthesis of benzo[a]phenoxazine derivative SSJ-183 (1), a promising lead for antimalarial agents, was developed using a one pot procedure. Furthermore, N-deethylated metabolite 3 and bis-N,N-deethylated metabolite 4 were synthesized by the application of the method. The metabolites 3 and 4 showed comparable and ∼2-fold increased activities against drug-sensitive and drug-resistant Plasmodium falciparum parasites.
-
Language
-
-
Open access status
-
bronze
-
Identifiers
-
-
Persistent URL
-
https://folia.unifr.ch/global/documents/49535
Statistics
Document views: 33
File downloads: