01721nas a2200229 4500008004100000022001400041245003600055210003500091260009000126300001200216490000700228520101400235653002201249653000901271653002001280653001701300653002001317100002601337700002901363700002701392856007201419 2010 eng d a1354-377600aAntifungal agents, WO20090257330 aAntifungal agents WO2009025733 aTELEPHONE HOUSE, 69-77 PAUL STREET, LONDON EC2A 4LQ, ENGLANDbINFORMA HEALTHCAREcJAN a137-1430 v203 a

Background: The incidence and prevalence of serious mycoses continues to be a public health problem. These infections are an important cause of morbidity and mortality, especially in immunocompromised patients. The present patent deals with isolation and characterization of a `pure' mixture of two novel isoxazolidinone-containing natural products from two new fungal strains. They have the partial structure of secalonic acid and show very good antifungal activity in mammals and plants and also synergism with other active ingredients. Objective: To analyze the activity of the isoxazolidinone-containing compounds in the present patent. Methods: To review the discovery and development of antifungal compounds in general and secalonic acid related compounds in particular. Conclusion: The research of Parish and collaborators at Merck and Co. has isolated novel antifungal compounds with a new mode of action. These molecules may be considered potential antifungal leads for further clinical study.

10aAntifungal agents10aCaFT10aisoxazolidinone10aparnafungins10asecalonic acids1 aSudhir, Pore, Vandana1 aRanan, Deshpande, Sunita1 aGanpat, Aher, Nilkanth uhttps://library.ncl.res.in/content/antifungal-agents-wo2009025733-002326nas 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

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.

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

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.

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-002318nas a2200253 4500008004100000022001400041245009700055210006900152260000900221490000700230520148500237653000601722653001301728653002201741653002601763653002301789653001501812100002101827700001801848700001901866700002601885700002801911856012501939 2023 eng d a1860-717900aDesign and synthesis of 1,3-diynes as potent antifungal agents against aspergillus fumigatus0 aDesign and synthesis of 13diynes as potent antifungal agents aga cMAY 0 v183 a

Eugenol and isoeugenol, secondary metabolites isolated from the plant Myristica fragrans have displayed antifungal activities against Aspergillus fumigatus (IC50 1900 mu M). Compounds having conjugated unsaturation have been of great use as antifungals i. e. amphotericin B, nystatin and terbinafine etc. Hence, in the present study, we have designed and synthesised 1,3-diynes by utilizing Glaser-Hay and Cadiot-Chodkiewicz coupling reactions to furnish possible antifungal agents. Synthesis of 1,6-diphenoxyhexa-2,4-diyne derivatives was achieved by Cu(I) catalysed coupling of propargylated eugenol, isoeugenol, guaiacol, vanillin and dihydrogenated eugenol or eugenol in good to excellent yields. All the synthesized compounds were evaluated against pathogenic fungus A. fumigatus. Among all the synthesized compounds, one of the compounds was found to be exhibiting promising antifungal activity with IC50 value of 7.75 mu M thereby suggesting that this type of scaffold could pave the way for developing new antifungal agents. The most active compound was found to be low cytotoxic when assayed against L-132 cancer cell line. Effect of the most active compound on ergosterol biosynthesis has also been studied. Also, the most active compound exhibited significant anti-biofilm activity although the concentration was found to be higher than its anti-fungal activity. Morphological changes in the biofilm were remarkable under confocal laser scanning microscopy.

10a110a3-Diynes10aAntifungal agents10aAspergillus fumigatus10aCadiot-Chodkiewicz10aGlaser-Hay1 aGoswami, Lakshmi1 aGupta, Lovely1 aPaul, Sayantan1 aVijayaraghavan, Pooja1 aBhattacharya, Asish, K. uhttps://library.ncl.res.in/content/design-and-synthesis-13-diynes-potent-antifungal-agents-against-aspergillus-fumigatus