Aromatic amides as potentiators of bioefficacy of anti-infective drugs

摘要

The present invention relates to an aromatic substituted pentadienoic acid amides and there use in combination of specific amounts of aromatic amides i.e. 4-alkyl-5-(substituted phenyl)-2 (E),4(E)-pentadienoic acid amides, its geometrical isomers or their dihydro or tetrahydro derivatives and an anti-infective drug useful in potentiating the bioefficacy of antiinfective drug. The combination of the present invention is useful in the treatment of certain infections and disease at lower concentration of anti-infectives necessary to inhibit the growth of microbial strains and may also find applications in reducing the resistance in microorganisms.

主权项

1. A method for inhibiting growth of a bacterial cell that employs an efflux pump resistance mechanism, comprising administering to a subject in need thereof a pharmaceutical composition comprising an effective amount of a potentiating compound of general formula 1 a-c including geometrical isomers and/or salts thereof:wherein R represents normal or branched chain C1 to C10 alkyl group and R1, R2 and R3 independently represent hydrogen, methoxyl, hydroxyl, halogen, or nitro; or where R2 and R3 together (R2+R3) represent —OCH2O—, —OCH2CH2O—, —CH2CH2CH2O—, or —CH2CH2C(CH3)2O—; R4 represents hydrogen or methoxyl; R5 represents hydrogen, normal or branched chain C1 to C8 alkyl, phenyl or benzyl; and R6 represents hydrogen, or C1 to C8 normal or branched chain alkyl group; or where NR5R6 together (R5+R6) represent an amino acid radical or a heterocyclic amine radical; and where dotted lines indicate the presence of double and/or single bonds.