- Cytoprotective effects of hydrogen sulfide-releasing N-methyl-d-aspartate receptor antagonists mediated by intracellular sulfane sulfur
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Hydrogen sulfide (H2S) exerts a host of biological effects ranging from cytotoxicity to cytoprotection. Cytotoxicity of H2S in neurodegenerative diseases may be mediated by N-methyl-d-aspartate receptor (NMDAR) activation. To exploit
- Marutani, Eizo,Sakaguchi, Masahiro,Chen, Wei,Sasakura, Kiyoshi,Liu, Jifeng,Xian, Ming,Hanaoka, Kenjiro,Nagano, Tetsuo,Ichinose, Fumito
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Read Online
- Dual Sigma-1 receptor antagonists and hydrogen sulfide-releasing compounds for pain treatment: Design, synthesis, and pharmacological evaluation
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The development of σ1 receptor antagonists hybridized with a H2S-donor is here reported. We aimed to obtain improved analgesic effects when compared to σ1 receptor antagonists or H2S-donors alone. In an in vivo
- Dichiara, Maria,Artacho-Cordón, Antonia,Turnaturi, Rita,Santos-Caballero, Miriam,González-Cano, Rafael,Pasquinucci, Lorella,Barbaraci, Carla,Rodríguez-Gómez, Isabel,Gómez-Guzmán, Manuel,Marrazzo, Agostino,Cobos, Enrique J.,Amata, Emanuele
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- H2S-Donating Doxorubicins May Overcome Cardiotoxicity and Multidrug Resistance
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Doxorubicin (DOXO) is one of the most effective antineoplastic agents in clinical practice. Its use is limited by acute and chronic side effects, in particular by its cardiotoxicity and by the rapid development of resistance to it. As part of a program ai
- Chegaev, Konstantin,Rolando, Barbara,Cortese, Daniela,Gazzano, Elena,Buondonno, Ilaria,Lazzarato, Loretta,Fanelli, Marilù,Hattinger, Claudia M.,Serra, Massimo,Riganti, Chiara,Fruttero, Roberta,Ghigo, Dario,Gasco, Alberto
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supporting information
p. 4881 - 4889
(2016/06/13)
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- Heterocycle-bridged and conformationally constrained retinoids: Synthesis of 4-(7,8,9,10-Tetrahydro-7,7,10,10-tetramethyl-4H-benzo[6,7]chromeno-[4,3-d]thiazole-2-yl)benzoic acid
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Retinoids are a class of synthetic and natural compounds structurally related to retinoic acid. In a search for discovery of a new class of heterocycle-bridged and conformationally constrained retinoids, here we report the synthesis of 4-(7,8,9,10-tetrahydro-7,7,10,10-tetramethyl-4H-benzo[6,7]chromeno[4,3-d]thiazole-2-yl)benzoic acid (10) starting from 5,6,7,8-tetrahydro-5,5,8,8-tetramethylnaphthalen-2-ol (13). Several approaches was attempted to obtain target compound 10. Structure elucidation of synthesized compounds has been made on the basis of elemental analysis and spectral data (1H NMR, IR and MS).
- Lamei, Navid,Foroumadi, Alireza,Emami, Saeed,Amini, Mohsen,Shafiee, Abbas
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experimental part
p. 1951 - 1956
(2011/06/19)
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- A mild and versatile synthesis of thioamides
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Aliphatic and aromatic nitriles react with thioacetic acid in the presence of calcium hydride to give the corresponding thioamides in good to excellent yields. The examples studied include haloaryl nitriles in which the halogen is facile towards SNAr reactions under other conditions. Georg Thieme Verlag Stuttgart.
- Mahammed,Jayashankara,Premsai Rai,Mohana Raju,Arunachalam
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experimental part
p. 2338 - 2340
(2009/12/08)
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- Novel thiazole derivatives as inhibitors of superoxide production by human neutrophils: Synthesis and structure-activity relationships
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Neutrophils have an important role in the self-defense systems of organisms through the production of superoxide. On the other hand, it has been proposed that abnormal amounts of superoxide produced by neutrophils are a serious factor in tissue injury. A series of novel thiazole derivatives was prepared and evaluated inhibitory effect on superoxide production by human neutrophils in vitro. Among these compounds, 6-[2-(3,4- diethoxyphenyl)thiazol-4-yl]-pyridine-2-carboxylic acid (OPC-6535) was selected as one of the most promising compounds. The synthesis and structure- activity relationships of these compounds are reported herein.
- Chihiro,Nagamoto,Takemura,Kitano,Komatsu,Sekiguchi,Tabusa,Mori,Tominaga,Yabuuchi
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p. 353 - 358
(2007/10/02)
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