著者

Naoki TANAKA Riki GOTO Rie ITO Miho HAYAKAWA Taketoshi OGAWA Koichi FUJIMOTO

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.46, no.4, pp.639-646, 1998-04-15 (Released:2008-03-31)

参考文献数

14

被引用文献数

2 2

---

A series of [2-(ω-phenylalkyl)phenoxy]alkylamines was synthesized and their 5-hydroxytryptamine2 (5-HT2) and/or dopamine2 (D2) receptor antagonistic activities were examined in vitro. [2-(4-Phenylbutyl)phenoxy]alkylamines showed strong inhibition of both 5-HT2 and D2 receptors. It particular, [2-(4-phenylbutyl)phenoxy]-methylpiperidine derivatives, 10b, 10i and 10q, exhbited potent inhibition. The structure-activity relationships in this series of compounds are discussed.

著者

Naoki TANAKA Riki GOTO Miho HAYAKAWA Atsuhiro SUGIDACHI Taketoshi OGAWA Fumitoshi ASAI Koichi FUJIMOTO

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.48, no.2, pp.245-255, 2000-02-01 (Released:2008-03-31)

参考文献数

26

被引用文献数

4 5

---

A series of [2-(ω-phenylalkyl)phenoxy]alkylamines was synthesized and thir receptor binding affinity was examined in vitro. These compounds showed an affinity for serotonin-2 (5-HT2) and dopamine-2 (D2) receptors. [2-(2-phenylethyl)phenoxy]alkylamine derivatives with a pyrrolidine or piperidine moiety in the structure showed higher affinity for 5-HT2 receptors but lower affinity for D2 receptors. Among these compounds, (S)-2-[2-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]ethyl]1-methylpyrrolidine, (S)-27, exhibited the most potent and selective affinity for 5-HT2 receptors. Furthermore, (S)-27 was effective in inhibiting 5-HT-induced vasoconstriction in vitro and platelet aggregation both in vitro and ex vivo.

著者

末宗 洋 田中 直樹 酒井 浄

出版者

The Pharmaceutical Society of Japan

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.38, no.11, pp.3155-3157, 1990-11-25 (Released:2008-03-31)

参考文献数

6

被引用文献数

6 6

---

Diastereoselective acetalization of methyl pyruvate and methyl phenylformate with (R)-1, 3-butanediol afforded predominantly (2R, 4R)-2-methoxycarbonyl-2, 4-dimethyl (or 4-methyl-2-phenyl)-1, 3-dioxanes (1a, 4a) under thermodynamically controlled conditions. The (2S, 4R)-isomer (1b) was obtained as the major product under kinetically controlled conditions.

著者

佐藤 博司 川島 洋一郎 久保 和雄 鈴木 利昭 佐中 孜 太田 和夫 杉野 信博

出版者

社団法人 日本透析医学会

雑誌

人工透析研究会会誌 (ISSN:02887045)

巻号頁・発行日

vol.17, no.2, pp.97-102, 1984-04-30 (Released:2010-03-16)

参考文献数

10

---

1971年4月から1983年4月までに当センターおよび関連施設において経験された慢性血液透析患者の不明熱28症例の臨床的検討を行った. 原因疾患は感染症が20例 (71%), 薬剤性2 (7%), 膠原病1 (4%), 不明5 (18%) で悪性腫瘍によるものはなかった. 特に感染症の中では結核症が13例 (46%) と最も頻度が高く, このうち肺外性結核が11例とそのほとんどを占めていた. その他, 尿路感染症は3例にみられ, 移植血管感染例も1例に認められた.発熱の特徴としては, 最高体温の平均が39℃で, 熱型は弛張熱あるいは間歇熱を呈するものが多く, 透析中または透析直後に発熱しやすい傾向にあった. 診断に関しては, 非結核性のものは比較的高い確診率を得ているが, 結核症では生前確定診断ができたものは3例 (21%) にすぎなかった. 結核症のうち3例でCTスキャン, 超音波検査で, 腹部リンパ節腫大を認め, また治療により消失し, 診断の一助となった. 感染症例のうち, Gaシンチで陽性所見を示したのは1例もなかった. 予後および転帰であるが, 死亡は6例 (21%) でこのうち5例 (83%) は結核症である. これらはその大部分が未治療または治療開始時期の遅れがみられ, 発症より2ヵ月以内に死亡した例である.以上より透析患者の不明熱に対しては常に結核症の可能性を考え, 早期治療を行う必要がある.

著者

芝 哲夫

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.50, no.12, pp.1070-1073, 1992-12-01 (Released:2009-11-16)

被引用文献数

1

著者

端早田 隆

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.65, no.7, pp.715-716, 2007-07-01 (Released:2010-10-20)

参考文献数

11

被引用文献数

1 2

---

This short review describes the recent development on β-mannosidic bond formation. Though the formation of β-mannoside is rather difficult in chemical synthesis, following two useful representative methods are reported; 1) introducing an acetal moiety as an acceptor on a donor as the stereocontroling element for intramolecular β-mannosylation; 2) using a donor having cyclic acetal protecting group at O-4, 6 position. As for the later, it was reported that the introduction of propagyl group at O-2 position improved β-selectivity even if a donor having steric protecting group at O-3 position was employed. Catalytic and β-selective mannosylation is also noted.

著者

青山 豊彦 塩入 孝之

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.115, no.6, pp.446-459, 1995-06-25 (Released:2008-05-30)

参考文献数

22

被引用文献数

3 5

---

Tilivalline (1a), a metabolite isolated from Klebsiella pneumoniae var. oxytoca, belongs to a group of pyrrolo [2, 1-c] [1, 4] benzodiazepines, a characteristic skeleton of anthramycin-type antitumor antibiotics. We have accomplished a completely stereoselective, efficient and convenient synthesis of 1a utilizing a new Mannich type intramolecular cyclization as a key step. Further, a computational chemical analysis clarified the effect of zinc chloride on the high stereoselectivity in the tilivalline synthesis. To aim both the extension of the scope of the new Mannich type intramolecular cyclization and the studies on the structure-biological activity relationship, we further extended the method to the synthesis of tilivalline derivatives and 2-(3'-indolyl)-1, 4-benzodiazepines (50). Investigation on the cytotoxicity of 1a and its analogs has revealed that 1a shows the strong cytotoxicity toward mouse leukemia L 1210 cells and the replacement of the indole function of 1a with cyano one increases the cytotoxicity of 1a about 100 times (IC50=0.05 μg/ml).

著者

塩入 孝之

出版者

公益社団法人 日本薬学会

雑誌

YAKUGAKU ZASSHI (ISSN:00316903)

巻号頁・発行日

vol.113, no.11, pp.760-780, 1993-11-25 (Released:2008-05-30)

参考文献数

69

被引用文献数

1

---

Recent studies on the new methods and new reagents in organic synthesis developed by our laboratories have been reviewed. Their application to the synthesis of biologically intriguing natural products has been also described. Dolastatin 10 (1), a potent antitumor peptide of marine origin, has been efficiently synthesized by use of diethyl phosphorocyanidate (DEPC), diphenyl phosphorazidate (DPPA) and (+)-2-hydroxy-3-pinanone ((+)-HyPN). Mugineic acid (27), a typical phytosiderophore from barley, has been synthesized using a phenyl group as a carboxyl synthon. The method is quite efficient to produce mugineic acid on a large scale. Tilivalline (50), isolated from Klebsiella pneumoniae var. oxytoca, has been synthesized by use of DPPA as an +NH2 synthon and DEPC as a coupling reagent. The new Mannich type reaction has been explored to construct the pyrrolo [2.1-c] [1.4] benzodiazepine skeleton. The chiral phase transfer catalyst (65a) based on cinchonine has been utilized for the asymmetric hydroxylation of the α-tetralone derivatives (63). The first synthesis of the chiral ammonium fluoride (71) has been achieved, and its use for the silicon-based asymmetric aldol reaction has been accomplished. Trimethylsilyldiazomethane (TMSCHN2) has been developed as a stable and safe substitute for hazardous diazomethane. As a C1-unit introducing reagent, TMSCHN2 and its lithium salt mostly realize the reactions similar to those carried out with diazomethane. On the other hand, they generally behave as a [C-N-N] azole synthon in an analogous but not as the same way as diazomethane. Using the lithium salt of TMSCHN2, new methods for the preparation of alkynes and pyrroles have been developed.

著者

小松 貞子 中井 弘司 高松 康雄 盛中 泰洋 渡辺 和俊 篠田 真樹 飯田 成宇

出版者

The Japanese Society for the Study of Xenobiotics

雑誌

薬物動態 (ISSN:09161139)

巻号頁・発行日

vol.11, no.5, pp.451-462, 1996-10-31 (Released:2007-03-29)

参考文献数

14

被引用文献数

6 6

---

MCI-186の代謝物および代謝の種差を明らかにするため,代謝物の検索,構造推定,尿中への未変化体および代謝物の排泄率,in vitro代謝について検討を行った.以下にその要約を示す. 1.MCI-86の主代謝物はいずれの動物およびヒトにおいてもMCI-186のsulfateおよびglucuronideであった.ラット,イヌの尿中ではMCI-186 sulfateが多く,ヒト尿中ではMCI-186 glucuronideが多く,種差が認められた. 2.いずれの種においても尿中排泄が主排泄経路であった.未変化体の尿中排泄率は投与量の3%以下とわずかであった.イヌやヒトでは尿中排泄量のほとんどが未変化体およびMCI-186のsulfate,glucuronideで説明できるのに対し,ラットでは未知の代謝物が尿中放射能量の20~27%と多く存在した.ラットの尿中排泄において大きな性差は認められなかった. 3.ラットおよびイヌの肝S9を用いたMCI-186のin vitro代謝においては,ラット,イヌともMCI-186 sulfate生成活性のほうがglucuronide生成活性よりも高く,またラットにおいてはいずれの生成活性も雄性ラットのほうが雌性ラットよりも高値であった.

著者

中野 眞汎

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.42, no.7, pp.665-671, 1984-07-01 (Released:2009-11-13)

参考文献数

18

被引用文献数

5 7

---

Poly (ethylene carbonate), poly (propylene carbonate), and poly (ethylene propylene carbonate) were examined as to their biodegradability, permeability, and drug release characteristics.Poly (ethylene carbonate) degraded but poly (propylene carbonate) did not in the peritoneal cavity of rats and the peritoneal cavity and subcutaneous tissue of guinea pigs. Mixtures of the two polymers degraded at a rate in proportion to poly (ethylene carbonate) content. Degradation rate in the peritoneal cavity was faster than that in subcutaneous tissue in guinea pigs.Membranes free from pores were obtained from poly (ethylene carbonate). Permeability of drugs through them depended on lipophilicity indicating role of solubility of the drugs in the membrane material for permeation.Release rate of tegafur from poly (ethylene carbonate) implants was faster than that from poly (propylene carbonate) implants. Blood level profiles were obtained after implantation of implants in rats.Microspheres containing local anesthetics were prepared by a solvent evaporation process and effects of drug content and polymer on release profiles were examined in vitro. Duration of local anesthesia after administration of dibucaine microspheres in guinea pigs was demonstrated.

著者

田村 類 高橋 弘樹 生塩 孝則

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.56, no.1, pp.22-33, 1998-01-01 (Released:2009-11-16)

参考文献数

16

被引用文献数

1 3

---

We have discovered the first case of accomplishment of an enantiomeric resolution by simple recrystallization of a series of racemic compounds [(±) forms] composed of a regular packing of (+) and (-) molecules in a crystal, although in principle this sort of enantiomeric resolution has been considered to be infeasible for more than a century since the discovery of chiral crystals by Pasteur and preferential crystallization of conglomerates by Gernetz which are a mixture of homochiral (+) and (-) crystals. We have designated this new enantiomeric resolution phenomenon as “Preferential Enrichment”. Here we report a distinct evidence that polymorphism between a racemic compound and a mixed crystal (solid solution), which consists of alternating alignment of the two homochiral dimers in a crystal, is responsible for the “Preferential Enrichment”, and we propose a mechanism of the phenomenon of the reversal of chirality in the deposited crystals, that is the essence of the “Preferential Enrichment”, on the basis of the polymorphic transformation during crystallization.

著者

松田 彰 上田 亨

出版者

公益社団法人 日本化学会

雑誌

日本化学会誌(化学と工業化学) (ISSN:03694577)

巻号頁・発行日

vol.1981, no.5, pp.845-850, 1981-05-10 (Released:2011-05-30)

参考文献数

23

被引用文献数

2

---

5'-デオキシ-5'-(フェニルチオ)グアノシン=2',3'-環状リン酸エステルを合成し,光照射を行なうと収率よく8,5'-環化反応が起こり,5'-デオキシ-8,5'-シクログアノシン-2'.3'-環状リン酸エステルが得られた。これは,塩基部がand形に固定されたグアニル酸のモデルである。この化合物はリボヌクレアーゼT1(RNaseT1)で加水分解され3'-リン酸エステルを与えるが,RNaseT1と3'-リン酸エステルの相互作用の分光学的解析を行なった結架,and形グアニル酸が,RNaseT1とよく相互作用することが明らかとなり,従来の定説を修正する結果となった。5'-デオキシ-8,5ノーシクロアデノシン=2,3'-環状リン酸エステルも同様に合成することができた。

著者

錦織 宏 道信 良子

出版者

日本医学教育学会

雑誌

医学教育 (ISSN:03869644)

巻号頁・発行日

vol.44, no.5, pp.273-273, 2013-10-25 (Released:2015-07-06)

著者

花井 重次

出版者

The Association of Japanese Geographers

雑誌

地理学評論 (ISSN:00167444)

巻号頁・発行日

vol.3, no.3, pp.173-189, 1927-03-01 (Released:2008-12-24)

参考文献数

14

著者

加藤 昭一

出版者

The Association of Japanese Geographers

雑誌

地理学評論 (ISSN:00167444)

巻号頁・発行日

vol.32, no.5, pp.256-260, 1959-05-01 (Released:2008-12-24)

参考文献数

3

---

On the southern slope of Mt. Ogi and Momokura in Yamanashi Prefecture, there runs a thrust fault line where an easy slope lies toward the River Katsuraa Though it seems as if it were the river terrace of the River Katsura, the slope consists of rock dust called Miyatani rock-dust-bed containing rock-dustbed slate, hornfels, diorite and andesite and the fine material bed alternately. According to the results of my observation, it is 24.82 meters thick at Jakotsuzawa, and the Miyatani rock-dust-bed runs down with a dip of 8°_??_14° from Mt. Momokura to the River Katsura or the River Kuzuno, The upper part is seen even when the surface of the earth is cut, and blue-grayband of clay material containing tiny plantseeds lies in the lower. Judging from the facts I conclude as follows: 1) The bed rock is of the conglomerate of the River Katsura. 2) Upon the bed rock were deposited in the still water blue-gray band and Miyatani rock-dust-bed. 3) After that the bed rock was elevated and the present surface was formed, but rejuvenation took place again.

著者

安孫子 淳

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.61, no.1, pp.24-34, 2003-01-01 (Released:2009-11-13)

参考文献数

14

被引用文献数

2 5

---

Boron-mediated aldol reaction of carboxylic esters is described in detail. Contrary to the gener-al belief that carboxylic esters are inert toward the conventional enolization conditions, propionate esters are shqwn to have adequate reactivity on the boron-mediated aldol reaction. More impor-tantly, the stereochemical course of the aldol reaction can be controlled by the judicious choice of the enolization reagents. Complementary anti- and syn-selective asymmetric aldol reaction of structurally related chiral esters are developed. Also, novel double aldol reaction is discovered with acetate esters, which provides a precursor to the synthesis of chiral triols of C3-symmetry. Extensive NMR experiments lead to characterize the first carbon-bound boron enolates and the novel doubly borylate enolates as intermediates of the double aldol reaction. A plausible mecha-nism of the double aldol reaction is proposed.

著者

佐藤 恒夫 安孫子 淳 正宗 悟

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.44, no.5, pp.384-404, 1986-05-01 (Released:2010-04-23)

参考文献数

89

被引用文献数

2 2

著者

佐藤 恒夫 安孫子 淳 正宗 悟

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.44, no.4, pp.309-325, 1986-04-01 (Released:2010-01-22)

参考文献数

46

被引用文献数

2 5

---

This account examines double asymmetric induction from theoretical and practical viewpoints. In the context of four major organic reactions-the aldol, Diels-Alder, catalytic hydrogenation, and epoxidation-it is shown that a double asymmetric induction can be analyzed in terms of the single asymmetric reactions of each of the two chiral reactants. A rule which qualitatively relates the results of these single asymmetric reactions with the outcome of the double asymmetric reaction is proposed. A powerful new strategy based on this rule for the predictable creation of new chiral centers is discussed and the use of this strategy for the synthesis of sugars and macrolides is presented.

著者

安孫子 淳

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.54, no.7, pp.564-573, 1996-07-01 (Released:2010-01-28)

参考文献数

28

被引用文献数

2 3

---

New chiral auxiliaries based on the isoxazolidine skeleton have been developed. Characteristic feature of these auxiliaries are : 1) High reactivity for asymmetric alkylations. 2) Acylation of the auxiliary with an acid chloride and an amine, or DCC condensation. 3) One step transformation of the reaction products to the corresponding chiral alcohols, aldehydes and ketones without loss of the stereochemical integrity with the recovery of the auxiliary. Asymmetric alkylation of chiral β-substituted alkanols via their triflates lead to the easy access to the “reduced polypropionate units” as well as the first synthesis of the marine natural product (+) -siphonarienone. Enantiomerically pure axially dissymmetric cyclohexylidene compounds were synthesized using asymmetric Horner-Emmons reaction of the phosphonate derived from the auxilliary.

著者

酒井 浄 中村 紀雄

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.36, no.2, pp.93-106, 1978-02-01 (Released:2009-11-13)

参考文献数

91

被引用文献数

2 2

---

Advances in Prostaglandin (PG) fields after the discovery of PGG2 and PGH2 are reviewed. Biological activities of PGG2, H2, I2 and TXA2 are briefly explained, and the synthetic studies on these new PGs reviewed. Improvements in the synthesis of primary PGs are also summarized.