01844nas a2200325   4500008004100000022001400041245011200055210006900167260009800236300001400334490000700348520076600355653001301121653001401134653001401148653000601162653000601168653001601174653000901190653000801199653001701207100002601224700002401250700001601274700002701290700002601317700002401343700002401367856012701391       2008                        eng d  a0749-158100aStructural elucidation of propargylated products of 3-substituted-1,2,4-triazole-5-thiols by NMR techniques0 aStructural elucidation of propargylated products of 3substituted  aTHE ATRIUM, SOUTHERN GATE, CHICHESTER PO19 8SQ, W SUSSEX, ENGLANDbJOHN WILEY & SONS LTDcDEC  a1168-11740 v463 a<p>Propargylation of 3-substituted-1,2,4-triazole-5-thiols, which predominantly exist as their thione tautomers, was carried out with the view to synthesize different heterocycles and study their biological activity. Three different products namely, a mono S-propargyl and two S,N-dipropargyl regioisomers, arising from N1/N2 substitution, were isolated and characterized. Unambiguous structural elucidation of the regioisomers of S,N-dipropargyl derivatives was achieved by means of (13)C-(1)H HMBC technique. The proportion of the regioisomers was found to vary with the substituent on the 1,2,4-triazole thiols. No product corresponding to N4 substitution was isolated from any of the reactions carried out. Copyright (C) 2008 John Wiley &amp; Sons, Ltd.</p>10a(1)H NMR10a(13)C NMR10a(15)N NMR10a110a210a4-triazoles10aHMBC10aNMR10aRegioisomers1 aChaudhary, Preeti, M.1 aChavan, Sayalee, R.1 aKavitha, M.1 aMaybhate, Shailaja, P.1 aDeshpande, Sunita, R.1 aLikhite, Anjali, P.1 aRajamohanan, P., R.  uhttps://library.ncl.res.in/content/structural-elucidation-propargylated-products-3-substituted-124-triazole-5-thiols-nmr-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-000945nas a2200229   4500008004100000022001400041245004900055210004800104260010300152300001200255490000700267520017800274653001900452653001500471653002900486653001400515100002600529700002700555700002400582700002600606856008300632       2010                        eng d  a0376-469900aFacile synthesis of N-substituted maleimides0 aFacile synthesis of Nsubstituted maleimides  aANUSANDHAN BHAWAN, 2 RAFI MARG, NEW DELHI, 110001, INDIAbCOUNCIL SCIENTIFIC & INDUSTRIAL REScAPR  a487-4880 v493 a<p>A simple and efficient method for the synthesis of N-substituted malemides from the corresponding maleamie acids under the phase transfer catalysis has been described</p>10aMaleamic acids10amaleimides10aphase transfer catalysis10asynthesis1 aDeshpande, Sunita, R.1 aMaybhate, Shailaja, P.1 aLikhite, Anjali, P.1 aChaudhary, Preeti, M.  uhttps://library.ncl.res.in/content/facile-synthesis-n-substituted-maleimides-002326nas a2200277   4500008004100000022001400041245011600055210006900171260010600240300001400346490000700360520125500367653002201622653002701644653002401671653002701695653002901722100002001751700002101771700002601792700002201818700002601840700002401866700002601890856013201916       2012                        eng d  a0960-894X00aHybrid molecules of carvacrol and benzoyl urea/thiourea with potential applications in agriculture and medicine0 aHybrid molecules of carvacrol and benzoyl ureathiourea with pote  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcSEP  a5550-55540 v223 a<p>Benzoyl phenyl urea, a class of insect growth regulator's acts by inhibiting chitin synthesis. Carvacrol, a naturally occurring monoterpenoid is an effective antifungal agent. We have structurally modified carvacrol (2-methyl-5-[1-methylethyl] phenol) by introducing benzoylphenyl urea linkage. Two series of benzoylcarvacryl thiourea (BCTU, 4a-f) and benzoylcarvacryl urea (BCU, 5a-f) derivatives were prepared and characterized by elemental analysis, IR, H-1 and C-13 NMR and Mass spectroscopy. Derivatives 4b, 4d, 4e, 4f and 5d, 5f showed comparable insecticidal activity with the standard BPU lufenuron against Dysdercus koenigii. BCTU derivatives 4c, 4e and BCU 5c showed good antifungal activity against phytopathogenic fungi viz. Magnaporthe grisae, Fusarium oxysporum, Dreschlera oryzae; food spoilage yeasts viz. Debaromyces hansenii, Pichia membranifaciens; and human pathogens viz. Candida albicans and Cryptococcus neoformans. Compounds 5d, 5e and 5f showed potent activity against human pathogens. Moderate and selective activity was observed for other compounds. All the synthesized compounds were non-haemolytic. These compounds have potential application in agriculture and medicine. (C) 2012 Elsevier Ltd. All rights reserved.</p>10aAntifungal agents10aBenzoyl carvacryl urea10aBenzoyl phenyl urea10aCrop protection agents10aInsect growth regulators1 aPete, Umesh, D.1 aZade, Chetan, M.1 aBhosale, Jitendra, D.1 aTupe, Santosh, G.1 aChaudhary, Preeti, M.1 aDikundwar, Amol, G.1 aBendre, Ratnamala, S.  uhttps://library.ncl.res.in/content/hybrid-molecules-carvacrol-and-benzoyl-ureathiourea-potential-applications-agriculture-and-001665nas a2200241   4500008004100000022001400041245005200055210005200107260011100159300001200270490000700282520083700289653002201126653002001148653003101168653001501199653003601214653001301250100002601263700002201289700002601311856008601337       2013                        eng d  a1389-557500aChitin synthase inhibitors as antifungal agents0 aChitin synthase inhibitors as antifungal agents  aEXECUTIVE STE Y-2, PO BOX 7917, SAIF ZONE, 1200 BR SHARJAH, U ARAB EMIRATESbBENTHAM SCIENCE PUBL LTDcFEB  a222-2360 v133 a<p>Increased risk of fungal diseases in immunocompromised patients, emerging fungal pathogens, limited repertoire of antifungal drugs and resistance development against the drugs demands for development of new and effective antifungal agents. With greater knowledge of fungal metabolism efforts are being made to inhibit specific enzymes involved in different biochemical pathways for the development of antifungal drugs. Chitin synthase is one such promising target as it is absent in plants and mammals. Nikkomycin Z, a chitin synthase inhibitor is under clinical development. Chitin synthesis in fungi, chitin synthase as a target for antifungal agent development, different chitin synthase inhibitors isolated from natural sources, randomly synthesized and modified from nikkomycin and polyoxin are discussed in this review.</p>10aAntifungal agents10aChitin synthase10aChitin synthase inhibitors10aNikkomycin10aPeptidyl nucleoside antibiotics10aPolyoxin1 aChaudhary, Preeti, M.1 aTupe, Santosh, G.1 aDeshpande, Mukund, V.  uhttps://library.ncl.res.in/content/chitin-synthase-inhibitors-antifungal-agents-002896nas a2200313   4500008004100000022001400041245011800055210006900173260010300242300001200345490000700357520176400364653000602128653000602134653002702140653003302167653001502200653001602215653003002231100002602261700002202287700002502309700002102334700002602355700002702381700002402408700002602432856012402458       2015                        eng d  a0376-469900aSynthesis and antifungal potential of 1,2,3-triazole and 1,2,4-triazole thiol substituted strobilurin derivatives0 aSynthesis and antifungal potential of 123triazole and 124triazol  aANUSANDHAN BHAWAN, 2 RAFI MARG, NEW DELHI, 110001, INDIAbCOUNCIL SCIENTIFIC & INDUSTRIAL REScJUL  a908-9170 v543 a<p>beta-Methoxyacrylate group is an important pharmacophore of commercially used strobilurin fungicides. In the present study, a total of seventeen 1,2,4-triazole thiols 8a-h and 1,2,3-triazole substituted 10a-i strobilurin derivatives have been synthesized. 1,2,4-Triazole thiol substituted strobilurin derivatives 8a-h have been found to inhibit the growth of plant pathogens such as Fusarium oxysporum, Magnaporthe grisea, Drechslera oryzae and human pathogens Aspergillus fumigatus and different strains of Cryptococcus neoformans, with MIC in the range of 16-256 mu g/mL. In case of Candida albicans tested strain, the MIC is &gt; 256 mu g/mL. p-Chlorophenyl substituted 1,2,4-triazole thiol strobiulrin derivative 8e is the most potent inhibitor with MIC of 16-64 mu g/mL against most of the tested pathogens. Antifungal action of the compounds is due to inhibition of mitochondrial respiration. In the resazurin reduction assay, EC50 for inhibition of RZ reduction in D. oryzae by azoxystrobin and 8e are 3.42 +/- 0.03 mu g/mL and 3.63 +/- 0.21 mu g/mL, respectively; while in case of C. neoformans, EC50,, of azoxystrobin and 8e are between 0.65-0.85 mu g/mL. In a non-pathogenic model Benjaminiella poitrasii, though the MIC for all the synthesized compounds 8a-h and 10a-i are &gt; 256 mu g/ml, yeast to hypha transition is inhibited in the range of 21-75% at 4 mu g/mL concentration while EC50 for inhibition of RZ reduction by azoxystrobin and 8e are 31.5 +/- 0.4 mu g/mL and 17.95 +/- 0.7 mu g/mL, respectively. The 50% germ tube formation inhibition in case of C. albicans is observed at 108.49 mu g/mL. 1,2,4-Triazole thiol substituted strobilurin derivatives hold promise for the control of pathogenic fungi in agriculture and health care.</p>10a110a210a3-triazole strobilurin10a4-triazole thiol strobilurin10aantifungal10aStrobilurin10aY-H transition inhibition1 aChaudhary, Preeti, M.1 aTupe, Santosh, G.1 aJorwekar, Shweta, U.1 aSant, Duhita, G.1 aDeshpande, Sunita, R.1 aMaybhate, Shailaja, P.1 aLikhite, Anjali, P.1 aDeshpande, Mukund, V.  uhttps://library.ncl.res.in/content/synthesis-and-antifungal-potential-123-triazole-and-124-triazole-thiol-substituted-0