- Synthesis, antiarrhythmic activity, and toxicological evaluation of mexiletine analogues
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Four mexiletine analogues have been tested for their antiarrhythmic, inotropic, and chronotropic effects on isolated Guinea pig heart tissues and to assess calcium antagonist activity, in comparison with the parent compound mexiletine. All analogues showed from moderate to high antiarrhythmic activity. In particular, three of them (1b,c,e) were more active and potent than the reference drug, while exhibiting only modest or no negative inotropic and chronotropic effects and vasorelaxant activity, thus showing high selectivity of action. All compounds showed no cytotoxicity and 1b,c,d did not impair motor coordination. All in, these new analogues exhibit an interesting cardiovascular profile and deserve further investigation.
- Roselli, Mariagrazia,Carocci, Alessia,Budriesi, Roberta,Micucci, Matteo,Toma, Maddalena,Di Cesare Mannelli, Lorenzo,Lovece, Angelo,Catalano, Alessia,Cavalluzzi, Maria Maddalena,Bruno, Claudio,De Palma, Annalisa,Contino, Marialessandra,Perrone, Maria Grazia,Colabufo, Nicola Antonio,Chiarini, Alberto,Franchini, Carlo,Ghelardini, Carla,Habtemariam, Solomon,Lentini, Giovanni
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supporting information
p. 300 - 307
(2016/07/06)
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- Chemo- and Diastereoselective N-Heterocyclic Carbene-Catalyzed Cross-Benzoin Reactions Using N-Boc-α-amino Aldehydes
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N-Boc-α-amino aldehydes are shown to be excellent partners in cross-benzoin reactions with aliphatic or heteroaromatic aldehydes. The chemoselectivity of the reaction and the facial selectivity on the amino aldehyde allow cross-benzoin products to be obtained in good yields and good diastereomeric ratios. The developed method is utilized as the key step in a concise total synthesis of d-arabino-phytosphingosine.
- Haghshenas, Pouyan,Gravel, Michel
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supporting information
p. 4518 - 4521
(2016/09/28)
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- CYANOGUANIDINES AND THEIR USE AS ANTIVIRAL AGENTS
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This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit RSV infection and/or replication; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
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Page/Page column 150
(2014/01/17)
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- Synthesis of proline analogues as potent and selective cathepsin S inhibitors
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Cathepsin S is a potential target of autoimmune disease. A series of proline derived compounds were synthesized and evaluated as cathepsin S inhibitors. We discovered potent cathepsin S inhibitors through structure-activity relationship studies of proline analogues. In particular, compound 19-(S) showed promising in vitro/vivo pharmacological activities and properties as a selective cathepsin S inhibitor.
- Kim, Mira,Jeon, Jiyoung,Song, Jiyeon,Suh, Kwee Hyun,Kim, Young Hoon,Min, Kyung Hoon,Lee, Kwang-Ok
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p. 3140 - 3144
(2013/06/26)
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- An Air/water-stable tridentate N-heterocyclic carbene-palladium(II) Complex: Catalytic C-H activation of hydrocarbons via hydrogen/deuterium exchange process in deuterium oxide
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While developing novel catalysts for carbon-carbon or carbon-heteroatom coupling (nitrogen, oxygen, or fluorine), we were able to introduce tridentate N-heterocyclic carbene (NHC)-amidate-alkoxide palladium(II) complexes. In aqueous solution, these NHC-Pd(II) complexes showed high ability for C-H activation of various hydrocarbons (cyclohexane, cyclopentane, dimethyl ether, tetrahydrofuran, acetone, and toluene) under mild conditions.
- Lee, Joo Ho,Yoo, Kyung Soo,Park, Chan Pil,Olsen, Janet M.,Sakaguchi, Satoshi,Prakash, G. K. Surya,Mathew, Thomas,Jung, Kyung Woon
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scheme or table
p. 563 - 568
(2009/11/30)
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- A STEREOSELECTIVE SYNTHESIS OF N-BOC-α-AMINO ALCOHOLS AND α-AMINO ACIDS
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A sterteoselective synthesis of N-Boc-α-amino alcohols and α-amino acids via the addition of Grignard reagents to the chiral electrophilic glycine equivalent α-bromo-N-Boc-glycine(-)phenylmenthylester is described.
- Ermert, Philipp,Meyer, Jsabella,Stucki, Christoph,Schneebeli, Joerg,Obrecht, Jean-Pierre
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p. 1265 - 1268
(2007/10/02)
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