01609nas a2200229   4500008004100000022001400041245010700055210006900162260011000231300001400341490000600355520070600361100002501067700002101092700002201113700001901135700002601154700002301180700002501203700002401228856012701252       2008                        eng d  a1477-052000aSynthesis and biological evaluation of bile acid dimers linked with 1,2,3-triazole and bis-beta-lactam0 aSynthesis and biological evaluation of bile acid dimers linked w  aTHOMAS GRAHAM HOUSE, SCIENCE PARK, MILTON RD, CAMBRIDGE CB4 0WF, CAMBS, ENGLANDbROYAL SOC CHEMISTRYcOCT  a3823-38300 v63 a<p>We report herein the synthesis and biological evaluation of bile acid dimers 11-18 linked through 1,2,3-triazole and bis-beta-lactam. The dimers 11-18 were synthesized using 1,3-dipolar cycloaddition reaction of diazido bis-beta-lactams 3, 4 and terminal alkynes 7-10 derived from cholic acid/deoxycholic acid in the presence of Cu(I) catalyst (click chemistry). These novel molecules were evaluated in vitro for their antifungal and antibacterial activity. Most of the compounds exhibited significant antifungal as well as antibacterial activity against all the tested fungal and bacterial strains. Moreover, their in vitro cytotoxicities towards HEK-293 and MCF-7 cells were also established.</p>1 aVatmurge, Namdev, S.1 aHazra, Braja, G.1 aPore, Vandana, S.1 aShirazi, Fazal1 aDeshpande, Mukund, V.1 aKadreppa, Sreenath1 aChattopadhyay, Samit1 aGonnade, Rajesh, G.  uhttps://library.ncl.res.in/content/synthesis-and-biological-evaluation-bile-acid-dimers-linked-123-triazole-and-bis-beta-002034nas a2200313   4500008004100000022001400041245010000055210006900155260010600224300001400330490000700344520092600351653002701277653001601304653001701320653001401337653001701351100002401368700002401392700002101416700002201437700002101459700002101480700001901501700002601520700002301546700002501569856012601594       2008                        eng d  a0960-894X00aSynthesis of chimeric tetrapeptide-linked cholic acid derivatives: impending synergistic agents0 aSynthesis of chimeric tetrapeptidelinked cholic acid derivatives  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcOCT  a5512-55170 v183 a<p>Tetrapeptides derived from glycine and beta-alanine were hooked at the C-3 beta position of the modified cholic acid to realize novel linear tetrapeptide-linked cholic acid derivatives. All the synthesized compounds were tested against a wide variety of microorganisms (Gram-negative bacteria, Gram-positive bacteria and fungi) and their cytotoxicity was evaluated against human embryonic kidney (HEK293) and human mammary adenocarcinoma (MCF-7) cell lines. While relatively inactive by themselves, these compounds interact synergistically with antibiotics such as fluconazole and erythromycin to inhibit growth of fungi and bacteria, respectively, at 1-24 mu g/mL. The synergistic effect shown by our novel compounds is due to their inherent amphiphilicity. The fractional inhibitory concentrations reported are comparable to those reported for Polymyxin B derivatives. (c) 2008 Elsevier Ltd. All rights reserved.</p>10aAntimicrobial activity10aCholic acid10aCytotoxicity10aSynergism10aTetrapeptide1 aBavikar, Sudhir, N.1 aSalunke, Deepak, B.1 aHazra, Braja, G.1 aPore, Vandana, S.1 aDodd, Robert, H.1 aThierry, Josiane1 aShirazi, Fazal1 aDeshpande, Mukund, V.1 aKadreppa, Sreenath1 aChattopadhyay, Samit  uhttps://library.ncl.res.in/content/synthesis-chimeric-tetrapeptide-linked-cholic-acid-derivatives-impending-synergistic-0