01580nas a2200241   4500008004100000022001400041245008200055210006900137260010600206300001400312490000700326520070500333653001801038653002401056653001401080653001201094100002301106700002201129700002601151700002401177700002401201856011301225       2009                        eng d  a0960-894X00aDesign and synthesis of bile acid-based amino sterols as antimicrobial agents0 aDesign and synthesis of bile acidbased amino sterols as antimicr  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcSEP  a5411-54140 v193 a<p>New bile acid-based amino sterols were synthesized in good yields from C-3 beta-oxiranes as key intermediates. These derivatives were evaluated for their in vitro antimicrobial properties against human pathogens. These compounds showed better antibacterial activity as compared to antifungal activity. Compounds 21 and 22 showed comparable antibacterial activity to gentamicin against Staphylococcus aureus with IC(50) values of 5.14 and 4.46 mu g/mL. This is the first report for the synthesis of C-3 beta-oxiranes on the steroids having A/B cis ring junction and these oxiranes have been used for the synthesis of amino sterols 17, 18, 21, and 22. (C) 2009 Elsevier Ltd. All rights reserved.</p>10aAmino sterols10aAntibacterial agent10abile acid10aOxirane1 aAher, Nilkanth, G.1 aPore, Vandana, S.1 aMishra, Nripendra, N.1 aShukla, Praveen, K.1 aGonnade, Rajesh, G.  uhttps://library.ncl.res.in/content/design-and-synthesis-bile-acid-based-amino-sterols-antimicrobial-agents-001939nas a2200301   4500008004100000022001400041245008900055210006900144260010600213300001200319490000700331520093200338653000601270653000601276653001501282653002101297653001401318653001501332653001601347100002301363700002201386700002601408700001801434700002401452700002001476700002001496856012101516       2009                        eng d  a0960-894X00aSynthesis and antifungal activity of 1,2,3-triazole containing fluconazole analogues0 aSynthesis and antifungal activity of 123triazole containing fluc  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcFEB  a759-7630 v193 a<p>Fluconazole based novel mimics containing 1,2,3-triazole were designed and synthesized as antifungal agents. Their antifungal activities were evaluated in vitro by measuring the minimal inhibitory concentrations (MICs). Compounds 12, 15, and 16 were found to be more potent against Candida fungal pathogens than control drugs fluconazole and amphotericin B. The studies presented here provide structural modi. cation of fluconazole to give 1,2,3-trazole containing molecules. Furthermore, these molecules were evaluated in vivo against Candida albicans intravenous challenge in Swiss mice and antiproliferative activities were tested against human hepatocellular carcinoma Hep3B and human epithelial carcinoma A431. It was found that compound 12 resulted in 97.4% reduction in fungal load in mice and did not show any profound proliferative effect at lower dose (0.001 mg/ml). (C) 2008 Elsevier Ltd. All rights reserved.</p>10a110a210a3-Triazole10aAntifungal agent10abile acid10aConjugates10aFluconazole1 aAher, Nilkanth, G.1 aPore, Vandana, S.1 aMishra, Nripendra, N.1 aKumar, Awanit1 aShukla, Praveen, K.1 aSharma, Aanchal1 aBhat, Manoj, K.  uhttps://library.ncl.res.in/content/synthesis-and-antifungal-activity-123-triazole-containing-fluconazole-analogues-0