Daiichi Sankyo Company, Limited

Nobuhisa Masuda

Toshiyuki Konosu

Yoshiko Kagoshima

Tsuyoshi Soneda

Yuko Yamamoto

Hiroshi Takeshita

Takuya Uchida

Junichi Kuroyanagi

Tetsunori Fujisawa

Aki Yokomizo

Issei Achiwa

Tetsuji Noguchi

Takafumi Hosokawa

Tetsuya Suzuki

Jitendra Anant Sattigeri

Makoto Yamaoka

Manoj Kumar Khera

Ryo Itooka

Tarun Mathur

Jitendra A Sattigeri

Problem to be Solved There is a need for a new antibiotic having a novel mechanism of action which exhibit strong antibacterial activity not only against sensitive bacteria but also against resistant bacteria thereof, and at the same time possesses excellent solubility an a safety profile amenable to human use. Solution to the Problem As a result of intensive research, the present inventors have found that a compound represented by general formula (I), 

Hydroxyalkyl thiadiazole derivatives

To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.

Imidazole carbonyl compound

An antibiotic compound having a novel mechanism of action, weak cytotoxicity, high solubility in water, effective in inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and having antibacterial activity.

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Tokyo, Japan

Nobuhisa Masuda