- From far west to east: Joining the molecular architecture of imidazole-like ligands in ho-1 complexes
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HO-1 overexpression has been reported in several cases/types of human malignancies. Unfortunately, poor clinical outcomes are reported in most of these cases, and the inhibition of HO-1 is considered a valuable and proven anticancer approach. To identify
- Fallica, Antonino Nicolò,Floresta, Giuseppe,Greish, Khaled,Patamia, Vincenzo,Pittalà, Valeria,Rescifina, Antonio,Sorrenti, Valeria
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- 2-ARYLCARBOXAMIDE-NITROGENEOUS HETEROCYCLE COMPOUND
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A compound represented bv the formula [I]: [wherein R1 and R2 are the same or different and each represents C1-6 alkyl, C3-8 cycloalkyl, et al; R3a, R3b, and R4 are the same or different and each represents hydrogen, C1-6 alkyl, et al; X represents -N-, -CH-, et al; Y1 represents a single bond, C1-3 alkylene, et al; Y2 represents C1-4 alkylene, oxy(C1-4 alkylene), et al; Ar1 represents a monocyclic aromatic carbocyclic group, monocyclic aromatic heterocyclic group, et al; and Ar2 represents a 5- or 6-membered aromatic carbocyclic group, aromatic heterocyclic group, et al]. This compound functions as a melanin-concentrating hormone receptor antagonist and is useful as, e.g., a therapeutic agent for obesity, et al.
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(2008/06/13)
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- Benzo-fused heterocyclic compounds having a 5-membered ring processes for their preparation their use as medicaments their use as diagnostic agents and medicaments containing them
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Benzo-fused heterocyclic compounds having a 5-membered ring, processes for their preperation, their use as medicaments, their use as diagnostic agents and medicaments containing them. Benzo-fused heterocyclic compounds having a 5-membered ring, of the formula I STR1 where X is N or CR(6); Y is oxygen, S or NR(7); A and B together are a bond or are both hydrogen, if, at the same time, X is CR(6) and Y is NR(7), one of the substituents R(1) to R(6) is a --CO--N=C(NH2)2 group; the other respective substituents R(1) to R(6) are H, Hal or alkyl; up to two of the other substituents R(1) to R(6) are CN, NO2, N3, (C1 -C4)-alkoxy, CF3 ; up to one of the other substituents is R(8)--Cn H2n --Z-- or phenyl; R(7) is H, alk(en)yl or R(8)--Cn H2n --, and pharmaceutically tolerated salts there of, are described. A process f or the preparation of the compounds I which comprises reacting a compound of the formula II STR2 in which one of the substituents R(1)' to R(5)' is a --CO--L group and L is a leaving group which can easily be replaced nucleophilically, with guanidine, and, if appropriate, converting the product into the pharmacologically tolerated salt, furthermore is also described.
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- Acetylenic and allenic derivatives of 2-(5-benzyloxyindolyl) and 2-(5-hydroxyindolyl)methylamines: synthesis and in vitro evaluation as monoamine oxidase inhibitors
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We report the synthesis and in vitro studies as MAO inhibitors of 2 series of new acetylenic and allenic derivatives of 2-(5-benzyloxyindolyl)- and 2-(5-hydroxyindolyl)methylamines and their indolylmethylamine precursors.All compounds were MAO inhibitors and either did not show selectivity (the benzyloxy compounds 5) or were selective for MAO-A (most of the hydroxy compounds 7).Three of the studied compounds, 7d, 7g and 7i, were found to be slightly more selective for MAO-A than clorgyline.
- Cruces, MA,Elorriaga, C,Fernandez-Alvarez, E
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