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2012 Jiva April Cover 220 GSM Art Card Glossy ... - Jivaonline.net

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een designed to inhibit the activity of EPs whichincludesa. PAN and their derivatives - Renau et al.(2003) showed that Phe-Arg--naphthylamine(PAN) effectively inhibits the effluxmechanism of quinolones. The modification ofthis chemical series by Yoshida et al. (2006)through the addition of various hydrophilic chainshas yielded pyridopyrimidine compounds. Amongthese an ammonium acetic acid analogue hadpotent efficacy, high solubility, and a good safetyprofile in acute toxicity assay in animal model ofP. aeruginosa infection.b. Quinoline derivatives- Alkoxy- andthioalkoxy-quinolines increased the susceptibilityof E. aerogenes MDR strains to chloramphenicol(Mahamoud et al., 2006). More studies arenecessary to determine the therapeutic propertiesof these compounds.c. Arylpiperidines and arypiperazines -Schumacher et al. (2006) demonstrated EPIacitivity of anthryl piperazines and naphthylpiperazines. However, due to “serotonin agonist”properties of arylpiperazines, they are likely to betoxic in man and animals (Kern et al., 2006)Table 1. Drugs having EPI activityd. Amide derivatives- 5,9-dimethyl-deca-2,4,8-trienoic acid amides and 9-formyl-5methyldeca-2,4,8-trienoic acid amides enhance theactivity of ciprofloxacin by blocking EP in S.aureus.e. Substituted polyamines- Gill et al. (1999)showed the EPI ability of N-benzylatedpolyazaalkanes, N-benzylated polyaminoalkanesin H. influenzaeOther synthetic compounds having EPI activityare given in table 3.CONCLUSIONNargotra et al. (2009) pointed out theapplication of quantitative structure-activityrelationship (QSAR) analysis to identify thepharmacophoric groups involved in theinhibition of EP. This can be applied for designingnew EPIs. Currently, no EPIs has been licensed fortherapeutic use in human or veterinary practice.But one program involving co-administration ofan EPI (aerosolized formulation of a PANderivative)with ciprofloxacin has reached phaseII human clinical trials for the treatment ofpulmonary exacerbations in cystic fibrosis due toMDR Gram-negative bacterial pathogens by MpexPharmaceuticals.Drug EP Bacteria ReferencesReserpine Bmr B. subtilis Neyfakh et al., 1991tetK MRSA Gibbons and Udo, 2000Verapamil LmrA L. lactis VanVeen et al., 199611 pyrroloquinaxolinederivatives of Omeprazole NorA G+ve bacteria Vidaillac et al., 2007Phenothiazines MFS S. aureusAnti-tubercular drugs M. tuberculosis Chan et al., 2007BpeAB-OprB,AmrAB-OprA B. pseudomallei Chan et al., 2005RNDE. coli, P. aeruginosa,S. Typhimurium Martins et al., 2008P-SSRI MFS and RND G+ve and G-ve bacteria Wei et al., 2004GENERAL ARTICLEJIVA Vol. 10 Issue 1 <strong>April</strong> <strong>2012</strong>71

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