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6 data found. 1 - 6 listed

Published online: 6th July, 2015

Paper | Regular issue | Prepress
DOI: 10.3987/COM-15-13197
Nir-fluorescent Ethyl 4,7-Bis(5-arythiophene-2-yl)-1,2,5-oxadiazolo[3,4-c]pyridine-6-carboxylate

Kentaro Nishi,* Nobuyuki Seto, Wataru Iwasaki, Yohei Matsuoka, Yuki Kashiwa, Youichi Sano, Tadashi Kawaharada, Takashi Yazumi, Keiji Mizuki, and Shin-ichiro Isobe

*Faculty of Engineering, Kyushu Sangyo University , 3-1 Matsukadai, 2-Chome, Higashiku, Fukuoka 813-8503, Japan

Abstract

Ethyl 4,7-bis(5-bromothiophen-2-yl)-1,2,5-oxadiazolo[3,4-c]pyridine-6-carboxylate 2 reacted with phenyl-, 4-methylphenyl-, 4-methoxyphenyl-, 3,4-dimethoxyphenyl-, 1-naphthyl-, and 2-naphthyl-boronic acid to give the corresponding π-extended 4,7-bis(5-arylthiophen-2-yl) derivatives 3a–f, which emitted fluorescence at around 700 nm in DMSO solution. The 4-methoxy and 2-naphthyl derivatives (3c and 3f) emitted fluorescence at 729 nm (13717 cm-1, Φ = 0.02) and 714 nm (14005 cm-1 and Φ = 0.11), respectively, with a large Stokes shift (184 and 182 nm for 3c; 4631 cm-1 and 4791 cm-1 for 3f).

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Published online: 6th July, 2015

Short Paper | Regular issue | Prepress
DOI: 10.3987/COM-15-13263
Preparation and Antibacterial Evaluation of Some Symmetrical Twin-Drug Type Bivalent Molecules

Fumiko Fujisaki, Makoto Furutachi, Ryou Fujiwara, Miriko Okabe, Hatsumi Aki, Nobuhiro Kashige, Fumio Miake, and Kunihiro Sumoto*

*Faculty of Pharmaceutical Sciences, Fukuoka University, 8-19-1 Nanakuma, Jonan-ku, Fukuoka 814-0180, Japan

Abstract

As one of our projects to investigate new bioactive compounds, we here report the synthesis and antibacterial evaluation of a few identical linker mode twin-drug type symmetrical hydantoin derivatives. The antibacterial activity of tested twin-drug type hydantoin derivatives (4~7) and the structure-activity relationships (SARs) of these bivalent symmetrical molecules are also described.

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Published online: 29th June, 2015

Short Paper | Regular issue | Prepress
DOI: 10.3987/COM-15-13222
Novel Grinding Synthesis of Pyranopyrazole Analogues and Their Evaluation as Antimicrobial Agents

Ashok Sharma, Badvel Pallavi, Rajnish Prakash Singh, Prabhat Nath Jha, and Paritosh Shukla*

*Department of Chemistry, Birla Institute of Technology and Science, BITS-Pilani, Pilani-333301, Rajasthan, 333031, India

Abstract

The paper describes the results of a new four-component synthesis of pyranopyrazole heterocycles by solvent-free one-pot grinding of malononitrile, hydrazine, ethyl acetoacetate, and various aldehydes in the presence of a base. The reaction proceeded smoothly at room temperature with good yields in very short reaction time. The synthesised compounds were evaluated for their in-vitro antibacterial activity against three different bacterial and three different fungal strains. The highlight of this work is that the synthesis was activity-driven. The brief SAR correlation found that the tested compounds showed better activity against fungal strains.

Supporting Info. (912KB)PDF (406KB)

Published online: 18th June, 2015

Short Paper | Regular issue | Prepress
DOI: 10.3987/COM-15-13231
Synthesis of Phenylselanylisochroman-1-ones through Highly Selective Selenolactonization of Styrene-Typed Carboxylic Acids

Enshan Zhou,* Xin Han, Yuanyuan Li, Chao Guo, and Chune Dong*

*School of Pharmaceutical Sciences, Wuhan University, Hubei, Wuhan, 430071, China

Abstract

The novel synthesis of phenylselanylisochroman-1-ones was achieved by selenolactonization of styrene-typed carboxylic acids and phenylselenenyl chloride in the presence of 1,4-diazabicyclo[2.2.2]octane (DABCO). The reactions give excellent yields with high exo-selectivity.

Supporting Info. (1.6MB)PDF (408KB)

Published online: 10th June, 2015

Short Paper | Special issue | Prepress
DOI: 10.3987/COM-15-S(T)1
Crystal Structures of N,N’-bis(5-Dodecyloxytropon-2-yl)piperazine and N,N’-bis(4-Butoxyphenyl)piperazine

Kanji Kubo,* Emi Yamamoto, Taisuke Matsumoto, Seiji Ujiie, and Akira Mori

*Department of Life Science and Technology, Faculty of Engineering, Hokkai-Gakuen Univiersity, Sapporo, Hokkaido 062-8605, Japan

Abstract

The crystal structures of N,N’-bis(5-dodecyloxytropon-2-yl)piperazine (1) and N,N’-bis(4-butoxyphenyl)piperazine (2) were analyzed by X-ray crystallography. The molecules of 1 and 2 sits on a center of symmetry such that the two aromatic rings are in an anti conformation with respect to one another across the piperazine ring. The molecules (1, 2) forms a tilted layer structure via intermolecular C-H∙∙∙O and C-H∙∙∙π interactions in 1 and intermolecular C-H∙∙∙O, C-H∙∙∙N, and C-H∙∙∙π interactions in 2.

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Published online: 10th June, 2015

Short Paper | Regular issue | Prepress
DOI: 10.3987/COM-15-13248
Ga(III) Catalyzed Addition of Indole Derivatives and Different Propiolates

Xun Zhu,* Xiuqin Zhou, and Dongsheng Xiang

*Department of Chemistry, Yancheng Institute of Industry Technology, Yancheng, Jiangsu, 224005, China

Abstract

Ga(III) was used to catalyze Michael addition of indole derivatives to different propiolates in aqueous solution. Good to excellent yields were obtained under our reaction conditions.

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6 data found. 1 - 6 listed