01358nas a2200217   4500008004100000022001400041245010700055210006900162260011000231300001200341490000600353520049100359100002200850700002400872700002400896700002400920700002600944700001800970700002400988856012801012       2012                        eng d  a2040-250300aSynthesis and antifungal activity of 1,5-disubstituted-1,2,3-triazole containing fluconazole analogues0 aSynthesis and antifungal activity of 15disubstituted123triazole   aTHOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLANDbROYAL SOC CHEMISTRYcAPR  a484-4880 v33 a<p>Fluconazole based novel mimics containing 1,5-disubstituted 1,2,3-triazoles were synthesized by using Ru catalysed 1,3 dipolar cycloaddition. All the newly synthesized compounds and pure enantiomers were more potent than fluconazole against Candida albicans. Docking of 9A and 9B showed different conformation in the active site of Cyp51 of Candida albicans. The more active compounds 2 and 2A did not exhibit any toxicity up to 3.12 mu g mL(-1) against mammalian cell line L929.</p>1 aPore, Vandana, S.1 aJagtap, Manisha, A.1 aAgalave, Sandip, G.1 aPandey, Atindra, K.1 aSiddiqi, Mohammad, I.1 aKumar, Vikash1 aShukla, Praveen, K.  uhttps://library.ncl.res.in/content/synthesis-and-antifungal-activity-15-disubstituted-123-triazole-containing-fluconazole-001413nas a2200205   4500008004100000022001400041245005400055210005400109260011000163300001400273490000700287520069000294100002200984700002401006700002101030700002401051700001801075700002601093856008801119       2015                        eng d  a1477-052000aDesign and synthesis of new fluconazole analogues0 aDesign and synthesis of new fluconazole analogues  aTHOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLANDbROYAL SOC CHEMISTRYcMAY  a6551-65610 v133 a<p>We have synthesized new fluconazole analogues containing two different 1,2,3-triazole units in the side chain. The synthesis of new amide analogues using a variety of acids is also described. All the compounds showed very good antifungal activity. A hemolysis study of the most active compounds 6e and 13j showed that both compounds did not cause any hemolysis at the dilutions tested. These compounds did not exhibit any toxicity to L929 cells at MIC and lower concentrations. In the docking study, the overall binding mode of 6e and 13j appeared to be reasonable and provided a good insight into the structural basis of inhibition of Candida albicans Cyp51 by these compounds.</p>1 aPore, Vandana, S.1 aAgalave, Sandip, G.1 aSingh, Pratiksha1 aShukla, Praveen, K.1 aKumar, Vikash1 aSiddiqi, Mohammad, I.  uhttps://library.ncl.res.in/content/design-and-synthesis-new-fluconazole-analogues-0