Heterocyclic analogs of benzanilide derivatives as potassium channel activators. IX

European Journal of Medicinal Chemistry
Vincenzo CalderoneEnrica Martinotti

Abstract

On the basis of our previous works, addressed to synthesise new activators of BK potassium channels, and of many suggestions from the international literature, a simple pharmacophoric model, consisting of two suitably substituted phenyl rings bound to various kinds of linkers, was hypothesised. In particular, the effectiveness of the amidic linker was demonstrated, since several benzanilide derivatives showed interesting BK-opener properties. As a development of these benzanilides, in this work we introduced heterocyclic substituents, replacing the aryl ring on the acid side or on the basic one of the amide linker of the above pharmacophore. The pharmacological results indicated some relevant remarks about the structural requirements, needed for a satisfactory BK-opener activity. In particular, the presence of a phenolic function, with a possible H-bond donor role, has been confirmed. Furthermore, the presence of nitrogen heterocycles on the acid side of the amide linker seems to be a negative requirement, while furan and thiophene were well tolerated. On the contrary, the introduction of insaturated heterocyclic rings (pyridine and thiazole) on the basic side of the amide linker, led to satisfactory biological activity, while ...Continue Reading

Citations

Jan 1, 2008·Acta Crystallographica. Section E, Structure Reports Online·Aamer SaeedHiroyuki Ishida
Jan 1, 2008·Acta Crystallographica. Section E, Structure Reports Online·Aamer SaeedRoderick G Stanley
Jan 1, 2009·Acta Crystallographica. Section E, Structure Reports Online·Aamer SaeedMichael Bolte
Jan 1, 2009·Acta Crystallographica. Section E, Structure Reports Online·Aamer SaeedMasood Parvez
Jan 1, 2009·Acta Crystallographica. Section E, Structure Reports Online·Aamer SaeedRoderick G Stanley
Jan 1, 2009·Acta Crystallographica. Section E, Structure Reports Online·Aamer SaeedUlrich Flörke
Jan 1, 2009·Acta Crystallographica. Section E, Structure Reports Online·Aamer SaeedMasood Parvez
Jan 1, 2009·Acta Crystallographica. Section E, Structure Reports Online·Aamer SaeedMichael Bolte
Jan 1, 2010·Acta Crystallographica. Section E, Structure Reports Online·Aamer SaeedJim Simpson
Mar 9, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Sandeep Kumar Mishra, N Suryaprakash
Oct 13, 2006·European Journal of Medicinal Chemistry·Vincenzo CalderoneEnrica Martinotti
Sep 8, 2010·Physical Chemistry Chemical Physics : PCCP·G N Manjunatha ReddyN Suryaprakash
Jul 31, 2020·Biomolecules·Paulina PecynaMalgorzata Kucinska
Feb 13, 2016·Acta Crystallographica. Section E, Crystallographic Communications·Rodolfo Moreno-FuquenAlan R Kennedy

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