Optical molecular sensors for cytochrome p450 activity

Details Optical molecular sensors for cytochrome p450 activity Optical molecular sensors for cytochrome p450 activity

C - Chemistry, Metallurgy

07

D

C07D 311/16 (2006.01) C07D 265/38 (2006.01) C07D 311/82 (2006.01) C07D 493/10 (2006.01) C12Q 1/26 (2006.01)

Patent

CA 2352631

The invention provides a compound, useful as an optical probe or sensor of the activity of at least one cytochrome P450 enzyme, and methods of using the compound to screen candidate drugs, and candidate drugs identified by these methods. The optical probe of the invention is a compound having the generic structure Y-L-Q, wherein Y is selected from the group consisting of Q as herein defined, saturated C1-C20 alkyl, unsaturated C1-C20 alkenyl, unsaturated C1-C20 alkynyl, substituted saturated C1-C20 alkyl, substituted unsaturated C1-C20 alkenyl, substituted unsaturated C1-C20 alkynyl, C1-C20 cycloalkyl, C1-C20 cycloalkenyl, substituted saturated C1-C20 cycloalkyl, substituted unsaturated C1-C20 cycloalkenyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl; L is selected from the group of (- OCR2H)p-, wherein for each p, all R2 are separately selected from the group consisting of a hydrogen atom, saturated C1-C20 alkyl, unsaturated C1-C20 alkenyl, unsaturated C1-C20 alkynyl, substituted saturated C1-C20 alkyl, substituted unsaturated C1-C20 alkenyl, substituted unsaturated C1-C20 alkynyl, C1-C20 cycloalkyl, C1-C20 cycloalkenyl, substituted saturated C1-C20 cycloalkyl, substituted unsaturated C1-C20 cycloalkenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, and p is a positive integer no greater than twelve; and Q is a chemical moiety that gives rise to optical properties in its hydroxy or hydroxylate, phenol or phenoxide form that are different from the optical properties that arise from its ether form. Most preferably, p is one, R2 is hydrogen, and Q is the ether form of a phenoxide fluorophore.

L'invention concerne un composé, pouvant servir de sonde ou de capteur optique de l'activité d'au moins un enzyme cytochrome P450, ainsi que des procédés d'utilisation dudit composé pour analyser des médicaments candidats, et des médicaments candidats identifiés par lesdits procédés. La sonde optique est composé de structure générique Y-L-Q. Y est choisi dans le groupe constitué par Q, comme défini selon l'invention, C¿1?-C¿20? alkyle saturé, C¿1?-C¿20? alcényle insaturé, C¿1?-C¿20? alkynyle insaturé, C¿1?-C¿20? alkyle saturé substitué, C¿1?-C¿20? alcényle insaturé substitué, C¿1?-C¿20? alkynyle insaturé, C¿1?-C¿20? cycloalkyle, C¿1?-C¿20? cycloalcényle, C¿1?-C¿20? cycloalkyle saturé substitué, C¿1?-C¿20? cycloalcényle insaturé substitué, aryle, aryle substitué, hétéroaryle et hétéroaryle substitué. L est choisi dans le groupe constitué par un atome d'hydrogène, C¿1?-C¿20? alkyle saturé, C¿1?-C¿20? alcényle insaturé, C¿1?-C¿20? alkynyle insaturé, C¿1?-C¿20? alkyle saturé substitué, C¿1?-C¿20? alcényle insaturé substitué, C¿1?-C¿20? alkynyle insaturé substitué, C¿1?-C¿20? cycloalkyle, C¿1?-C¿20? cycloalcényle, C¿1?-C¿20? cycloalkyle saturé substitué, C¿1?-C¿20? cycloalcényle insaturé substitué, aryle, aryle substitué, hétéroaryle, hétéroaryle substitué, p étant un nombre entier positif n'excédant pas douze. Q est une fraction chimique qui permet d'obtenir des propriétés optiques, dans ses formes hydroxy ou hydroxylate, phénol ou phénoxyde, qui sont différentes des propriétés optiques qui découlent de l'une ou de l'autre de ses formes. Idéalement, p est un, R¿2? est l'hydrogène et Q est la forme éther d'un phénoxyde fluorophore.

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