01684nas a2200277   4500008004100000022001400041245016300055210006900218260010600287300001400393490000700407520057500414653002400989653003101013653002801044653003101072653002101103100002101124700002001145700001901165700001801184700002301202700002601225700002601251856012901277       2007                        eng d  a0968-089600aSynthesis and evaluation of antifungal properties of a series of the novel 2-amino-5-oxo-4-phenyl-5,6,7,8-tetrahydroquinoline-3-carbonitrile and its analogues0 aSynthesis and evaluation of antifungal properties of a series of  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcNOV  a6705-67150 v153 a<p>A series of 2-amino-5-oxo-4-phenyl-5,6,7,8-tetrahydroquinoline-3-carbonitrile and various analogues have been synthesized in excellent isolated yields starting from various arylidenemalononitrile and 3-amino-2-cyclohexen-1-one in 1-propanol as solvent at reflux temperature in the absence of any added catalyst. All the synthesized compounds were evaluated for their antifungal activity. The relationship between functional group variation and biological activity of the evaluated compounds is discussed in the article. (C) 2007 Elsevier Ltd. All rights reserved.</p>10aAntifungal activity10aantiproliferative activity10aarylidenemalononitriles10aarylquinoline carbonitrile10aMichael addition1 aGholap, Atul, R.1 aToti, Kiran, S.1 aShirazi, Fazal1 aKumari, Ratna1 aBhat, Manoj, Kumar1 aDeshpande, Mukund, V.1 aSrinivasan, Kumar, V.  uhttps://library.ncl.res.in/content/synthesis-and-evaluation-antifungal-properties-series-novel-2-amino-5-oxo-4-phenyl-5678-001714nas a2200265   4500008004100000022001400041245016400055210006900219260010600288300001600394490000700410520067400417653002601091653002401117653001701141653001401158653001601172653002001188100002101208700002001229700001901249700002601268700002601294856012801320       2008                        eng d  a0040-402000aEfficient synthesis of antifungal pyrimidines via palladium catalyzed Suzuki/Sonogashira cross-coupling reaction from Biginelli 3,4-dihydropyrimidin-2(1H)-ones0 aEfficient synthesis of antifungal pyrimidines via palladium cata  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcOCT  a10214-102230 v643 a<p>An efficient regioselective approach to the synthesis of tetrasubstituted pyrimidines was developed by sequential functionalization of easily available Biginelli 3,4-dihydropyrimidine-2(1H)-ones via dehydrogenation, chlorination followed by palladium catalyzed C-C Suzuki/Sonogashira coupling reaction. All the synthesized compounds were evaluated in vitro for their antifungal activities against Candida albicans, Cryptococcus neoformans, Benjaminiella poitrasii, Yarrowia lipolytica, and Fusarium oxysporum, and antibacterial activities against Gram-negative Escherichia coli and Gram-positive Staphylococcus aureus. (c) 2008 Elsevier Ltd. All rights reserved.</p>10aAntifungal activities10aBiginelli compounds10achlorination10aOxidation10aPyrimidines10aSuzuki coupling1 aGholap, Atul, R.1 aToti, Kiran, S.1 aShirazi, Fazal1 aDeshpande, Mukund, V.1 aSrinivasan, Kumar, V.  uhttps://library.ncl.res.in/content/efficient-synthesis-antifungal-pyrimidines-palladium-catalyzed-suzukisonogashira-cross-001337nas a2200205   4500008004100000022001400041245009700055210006900152260010600221300001400327490000700341520051900348100002500867700002100892700002200913700001900935700002400954700002600978856012701004       2008                        eng d  a0960-894X00aSynthesis and antimicrobial activity of beta-lactam-bile acid conjugates linked via triazole0 aSynthesis and antimicrobial activity of betalactambile acid conj  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcMAR  a2043-20470 v183 a<p>Synthesis of novel 1,2,3-triazole-linked beta-lactam-bile acid conjugates 17-24 using 1,3-dipolar cycloaddition reaction of azido beta-lactam and terminal alkyne of bile acids in the presence of Cu( I) catalyst ( click chemistry) have been realized. These molecules were evaluated in vitro for their antifungal and antibacterial activities. Most of the compounds exhibited significant antifungal and moderate antibacterial activity against all the tested strains. (c) 2008 Elsevier Ltd. All rights reserved.</p>1 aVatmurge, Namdev, S.1 aHazra, Braja, G.1 aPore, Vandana, S.1 aShirazi, Fazal1 aChavan, Pradnya, S.1 aDeshpande, Mukund, V.  uhttps://library.ncl.res.in/content/synthesis-and-antimicrobial-activity-beta-lactam-bile-acid-conjugates-linked-triazole-001609nas 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-002379nas a2200385   4500008004100000022001400041245010600055210006900161260010600230300001400336490000700350520105700357653000601414653000601420653002801426653001501454653002201469653002101491653002501512653002901537653001901566653002401585100002601609700002401635700001901659700002201678700001901700700002701719700002401746700002401770700002101794700002601815700002601841856012601867       2009                        eng d  a0968-089600aExploration of click reaction for the synthesis of modified nucleosides as chitin synthase inhibitors0 aExploration of click reaction for the synthesis of modified nucl  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcMAR  a2433-24400 v173 a<p>Click reaction approach toward the synthesis of two sets of novel 1,2,3-triazolyl linked uridine derivatives 19a-19g and 21a-21g was achieved by Cu(I)-catalyzed 1,3-dipolar cycloaddition of 5'-azido-5'-deoxy-2',3'-O-(1-methylethylidene) uridine (17) with propargylated ether of phenols 18a-18g and propargylated esters 20a-20g. Structure of one of the representative compound 19d was unambiguously confirmed by X-ray crystallography. Chitin synthase inhibition study of all these compounds 19a-19g and 21a-21g was carried out to develop antifungal strategy. Compounds 19d, 19e, 19f, and 21f were identified as potent chitin synthase inhibitors by comparing with nikkomycin. Compounds 19a, 19b, 19c, 19d, 21a, and 21b showed good antifungal activity against human and plant pathogens. Compounds 19a, 19b, 19f, 21c, 21f, and 21g were identified as lead chitin synthase inhibitors for further modi. cations by comparing results of inhibition of growth, % germ tube formation and chitin synthase activity. (C) 2009 Elsevier Ltd. All rights reserved.</p>10a110a210a3-dipolar cycloaddition10a3-Triazole10a4-Disubstituted-110a5 `-Azidouridine10aAntifungal compounds10aChitin synthase activity10aClick reaction10aUridine nucleosides1 aChaudhary, Preeti, M.1 aChavan, Sayalee, R.1 aShirazi, Fazal1 aRazdan, Meenakshi1 aNimkar, Prachi1 aMaybhate, Shailaja, P.1 aLikhite, Anjali, P.1 aGonnade, Rajesh, G.1 aHazra, Braja, G.1 aDeshpande, Mukund, V.1 aDeshpande, Sunita, R.  uhttps://library.ncl.res.in/content/exploration-click-reaction-synthesis-modified-nucleosides-chitin-synthase-inhibitors-001503nas a2200265   4500008004100000022001400041245012700055210006900182260010300251300001400354490000700368520047800375653002700853653002400880653002200904653002300926653002200949100002600971700002200997700002401019700002201043700001901065700002601084856012701110       2011                        eng d  a0223-523400aStereoselective synthesis and antimicrobial activity of steroidal C-20 tertiary alcohols with thiazole/pyridine side chain0 aStereoselective synthesis and antimicrobial activity of steroida  a23 RUE LINOIS, 75724 PARIS, FRANCEbELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIERcSEP  a3681-36890 v463 a<p>Stereoselective synthesis of novel steroidal C-20 tertiary alcohols with thiazole and pyridine side chain using Grignard reaction of steroidal ketones and thiazole/pyridine magnesium bromide have been realized. These molecules were evaluated in vitro for their antifungal and antibacterial activities. Most of the compounds exhibited significant antifungal and antibacterial activity against all the tested strains. (C) 2011 Elsevier Masson SAS. All rights reserved.</p>10aantibacterial activity10aAntifungal activity10aGrignard reaction10aSteroid side chain10aSteroidal ketones1 aShingate, Bapurao, B.1 aLiazra, Braja, G.1 aSalunke, Deepak, B.1 aPore, Vandana, S.1 aShirazi, Fazal1 aDeshpande, Mukund, V.  uhttps://library.ncl.res.in/content/stereoselective-synthesis-and-antimicrobial-activity-steroidal-c-20-tertiary-alcohols-001309nas a2200265   4500008004100000022001400041245007700055210006900132260010600201300001600307490000700323520035200330653002200682653002700704653002400731653002000755653002400775100002600799700002100825700002400846700002200870700001900892700002600911856010600937       2013                        eng d  a0040-402000aSynthesis and antimicrobial activity of novel oxysterols from lanosterol0 aSynthesis and antimicrobial activity of novel oxysterols from la  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcDEC  a11155-111630 v693 a<p>Chemically diverse oxysterols and their synthetic manipulations were carried out from variety of Delta(8(9)_) lanosterol derivatives and evaluated for their in vitro antimicrobial activities. Most of the synthesized oxysterols exhibited significant antifungal activity against the tested strains. (C) 2013 Elsevier Ltd. All rights reserved.</p>10aAllylic oxidation10aantibacterial activity10aAntifungal activity10aDihydroxylation10aOxygenated steroids1 aShingate, Bapurao, B.1 aHazra, Braja, G.1 aSalunke, Deepak, B.1 aPore, Vandana, S.1 aShirazi, Fazal1 aDeshpande, Mukund, V.  uhttps://library.ncl.res.in/content/synthesis-and-antimicrobial-activity-novel-oxysterols-lanosterol-0