A series of alkylamido- (1) and alkylaminobiphenyl (2) derivatives were synthesized as possible bioisosters of the reported ACAT inhibitors phenylpyridazine analogues (I). Both 1 and 2 were tested on the human ACAT-1 and ACAT-2 isoforms. The amino derivatives 2 were found to be inactive, contrary to the related pyridazine derivatives. By contrast, the ortho-substituted amides la and Id showed an interesting activity. These results support the essential role of the pyridazine nucleus. Modeling studies were also performed.

Gelain, A., Barlocco, D., Kwon Byoung, M., Jeong Tae, S., Im Kyung, R., Legnani, L., et al. (2008). Biphenyl versus Phenylpyridazine Derivatives: The Role of the Heterocycle in a Series of Acyl-CoA:Cholesterol Acyl Transferase Inhibitors. JOURNAL OF MEDICINAL CHEMISTRY, 51(5), 1474-1477 [10.1021/jm701474c].

Biphenyl versus Phenylpyridazine Derivatives: The Role of the Heterocycle in a Series of Acyl-CoA:Cholesterol Acyl Transferase Inhibitors

LEGNANI, LAURA;
2008

Abstract

A series of alkylamido- (1) and alkylaminobiphenyl (2) derivatives were synthesized as possible bioisosters of the reported ACAT inhibitors phenylpyridazine analogues (I). Both 1 and 2 were tested on the human ACAT-1 and ACAT-2 isoforms. The amino derivatives 2 were found to be inactive, contrary to the related pyridazine derivatives. By contrast, the ortho-substituted amides la and Id showed an interesting activity. These results support the essential role of the pyridazine nucleus. Modeling studies were also performed.
Articolo in rivista - Articolo scientifico
Acat inhibitors; Molecular modeling; DFT calculations;
English
1474
1477
4
Gelain, A., Barlocco, D., Kwon Byoung, M., Jeong Tae, S., Im Kyung, R., Legnani, L., et al. (2008). Biphenyl versus Phenylpyridazine Derivatives: The Role of the Heterocycle in a Series of Acyl-CoA:Cholesterol Acyl Transferase Inhibitors. JOURNAL OF MEDICINAL CHEMISTRY, 51(5), 1474-1477 [10.1021/jm701474c].
Gelain, A; Barlocco, D; Kwon Byoung, M; Jeong Tae, S; Im Kyung, R; Legnani, L; Toma, L
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/351884
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