Design and synthesis of novel benzimidazole derivatives as phosphodiesterase 10A inhibitors with reduced CYP1A2 inhibition

Design and Microwave Assisted Synthesis of Coumarin Derivatives as PDE Inhibitors

“…The structural analogs viz., compounds VIII and X contain benzoxazole and benzimidazole attached to quinoline through oxygen as linker group. These have shown possess promising PDE inhibition as reported by Hamaguchi et al [ 23 ]. Also substitution of the pyrazole with simple alkyl groups retained potency while adding minimal molecular weight.…”

Structure activity relationship (SAR) study of benzimidazole scaffold for different biological activities: A mini-review

“…Among the series, compound 62 surfaced out as the potent PDE10A (phosphodiesterases) inhibiton with reduced CYP1A2 (cytochrome P450 1A2) inhibitory because of the introduction of an isopropyl group at the 2-position and a methoxy group at the 5-position of the benzimidazole ring as illustrated in Fig.43 [83].…”

Recyclization‐Isomerization in the Reduction of 1‐(2‐Nitro(het)aryl)benzimidazoles

“…It was shown that the activity of N‐phenylbenzimidazoles as inhibitors of the platelet derived growth factor receptor (PDGFR) was determined by a reaction of the N‐phenyl ring with the hydrophobic part of the enzyme's active center. It was found in other studies that the use of N‐hetaryl substituted benzimidazoles instead of N‐aryl analogues reduced the biological effect of compounds, while replacement of the aromatic moiety by a non‐aromatic one suppressed it completely . Moreover, N‐(aminophenyl)benzimidazoles can be used for synthesizing compounds of yet another important class of biologically active compounds, viz ., fused benzimidazole derivatives with a bridgehead nitrogen atom …”