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Phase I Clinical Studies of S-1090: Safety and Pharmacokinetics

Autor: Hiromichi Imoto, Shimaru Sasaki, Takayoshi Oguma, Yasuo Kimura, Yuji Sendo, Mitsuyoshi Nakashima

Publikováno v: Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy. 2(4)

S-1090, an oral cephem antibiotic, was given to healthy male volunteers in single (10 to 400 mg) and multiple (200 mg, twice a day) doses. There were no abnormalities in subjective and objective signs, or physical findings, in any subjects. The intes

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a90f546b8c3659c60ee0802e896a421c
https://pubmed.ncbi.nlm.nih.gov/29681381

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Synthesis and modification of a novel 1 beta-methyl carbapenem antibiotic, S-4661

Autor: Kiyoshi Motokawa, Yasuhiro Nishitani, Yuji Sendo, Makoto Kii, Yasuyoshi Iso, Tsutomu Iwaki, Tadashi Irie

Publikováno v: The Journal of antibiotics. 49(5)

We describe an efficient method for introducing a sulfamoylamino group into the C-2' position of pyrrolidine using the Mitsunobu reaction. S-4661, its N-methyl analogues and stereoisomers were synthesized using this method and their structure-activit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05342533b75d85b24c9547698cc7f14b
https://pubmed.ncbi.nlm.nih.gov/8682725

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Synthesis and antibacterial activity of 1-substituted-methyl carbapenems

Autor: Miki Sakanoue, Yuji Sendo, Makoto Kii, Kiyoshi Motokawa, Yasuo Kimura

Publikováno v: Chemicalpharmaceutical bulletin. 40(9)

The synthesis of the 1 alpha- and the 1 beta-substituted (fluoro, cyano, hydroxy and acetoxy)-methyl carbapenems having a 2-(1,3,4-thiadiazol-2-yl)thiomethyl side chain are described, and their in vitro antibacterial activities are compared with the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bd4b48990d309ceda9140cffd352ffe7
https://pubmed.ncbi.nlm.nih.gov/1446363

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Synthetic studies on β-lactam antibiotics. 18. Convenient, stereocontrolled synthesis of 3-methyl 7α-methoxy-1-oxacephems

Autor: Wataru Nagata, Mitsuru Yoshioka, Yuji Sendo, Tsutomu Aoki

Publikováno v: Tetrahedron Letters. 20:4327-4330

Alcohols 4 and 8 , prepared from 3 , underwent completely stereospecific etherification to give 1-oxacephams 5 and 10 , which were converted into the 1-oxacephem nucleus 1b via 6 and 1c . Functionalization at C-3′ in 6 and 1c was unsuccessful.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::12b2c59dd60faa23c79eb21502bee9da
https://doi.org/10.1016/s0040-4039(01)86579-5

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Practical procedure for epimerization of 7α-amino-1-oxacephems to 7β-amino epimers

Autor: Toshiro Konoike, Mitsuru Yoshioka, Wataru Nagata, Yuji Sendo, Nobuhiro Haga, Tsutomu Aoki

Publikováno v: Tetrahedron Letters. 26:339-342

7α-Amino-1-oxacephems can be epimerized to their 7β-amino epimers by treatment with chloral to give Schiff bases, followed by dehydrochlorination with Hunig base, borohydride reduction, and hydrolysis.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::392f2a4be14b8a69e97da7c5d9c8ae64
https://doi.org/10.1016/s0040-4039(01)80812-1

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Synthetic studies on β-lactam antibiotics. VII. Mild removal of the benzyl ester protecting group with aluminum trichloride

Autor: Mitsuru Yoshioka, Shoichi Hirai, Wataru Nagata, Yuji Sendo, Takashi Maeda, Teruji Tsuji, Yasuhiro Nishitani, Takahiro Kataoka

Publikováno v: Tetrahedron Letters. 20:2793-2796

The benzyl ester protecting group in β-lactam derivatives can be cleanly removed by treatment with aluminum trichloride under mild conditions, preferably in the presence of anisole, to give the corresponding free acids in high yields.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::cb371a2466f84fd4ea3370f248e3163d
https://doi.org/10.1016/s0040-4039(01)86418-2

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