- Synthesis, SAR study, and biological evaluation of novel 2,3-dihydro-1H-imidazo[1,2-a]benzimidazole derivatives as phosphodiesterase 10A inhibitors
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Phosphodiesterase 10A (PDE10A) inhibitors were designed and synthesized based on the dihydro-imidazobenzimidazole scaffold. Compound 5a showed moderate inhibitory activity and good permeability, but unfavorable high P-glycoprotein (P-gp) liability for bra
- Chino, Ayaka,Honda, Shugo,Morita, Masataka,Yonezawa, Koichi,Hamaguchi, Wataru,Amano, Yasushi,Moriguchi, Hiroyuki,Yamazaki, Mayako,Aota, Masaki,Tomishima, Masaki,Masuda, Naoyuki
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p. 3692 - 3706
(2019/07/12)
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- Research in the field of imidazo[1,2-a]benzimidazole derivatives: XXVII. 1-acylmethyl-2-(ω-hydroxyalkylamino)-benzimidazoles and their transformation into derivatives of tricyclic systems
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1-Acylmethyl-2-(ω-hydroxyalkylamino)benzimidazoles were synthesized and their behavior under various conditions was investigated: at the thermolysis without solvent, at heating in DMF or in 2-aminoethanol, hydrohalic acids, and acetic anhydride, in the presence of chlorinating agents (SOCl2, POCl3). Depending on the reaction conditions derivatives were obtained of 1H-imidazo[1,2-a]-benzimidazole, 9H-2,3-dihydroimidazo[1,2-a] benzimidazole, and 10H-2,3,4,10-tetrahydropyrimido[1,2-a]-benzimidazole that were suitable synthons for the synthesis of functionally substituted derivatives of these tricyclic systems.
- Anisimova,Tolpygin,Borodkin
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experimental part
p. 275 - 285
(2010/08/19)
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- Benzimidazole compounds
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Compounds of the general formula (I): STR1 wherein A, B, C, D, n, R1, R2, R3, R4, X, Y and Z are as defined in the description, and their use as antidiabetics are disclosed.
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