@article { ISI:000273942600008, title = {Antifungal agents, WO2009025733}, journal = {Expert Opinion on Therapeutic Patents}, volume = {20}, number = {1}, year = {2010}, month = {JAN}, pages = {137-143}, publisher = {INFORMA HEALTHCARE}, address = {TELEPHONE HOUSE, 69-77 PAUL STREET, LONDON EC2A 4LQ, ENGLAND}, abstract = {

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 {\textquoteleft}pure{\textquoteright} 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.

}, keywords = {Antifungal agents, CaFT, isoxazolidinone, parnafungins, secalonic acids}, issn = {1354-3776}, doi = {10.1517/13543770903338768}, author = {Sudhir, Pore Vandana and Ranan, Deshpande Sunita and Ganpat, Aher Nilkanth} } @article { ISI:000308046400038, title = {Hybrid molecules of carvacrol and benzoyl urea/thiourea with potential applications in agriculture and medicine}, journal = {Bioorganic \& Medicinal Chemistry Letters}, volume = {22}, number = {17}, year = {2012}, month = {SEP}, pages = {5550-5554}, publisher = {PERGAMON-ELSEVIER SCIENCE LTD}, address = {THE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLAND}, abstract = {

Benzoyl phenyl urea, a class of insect growth regulator{\textquoteright}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.

}, keywords = {Antifungal agents, Benzoyl carvacryl urea, Benzoyl phenyl urea, Crop protection agents, Insect growth regulators}, issn = {0960-894X}, doi = {10.1016/j.bmcl.2012.07.017}, author = {Pete, Umesh D. and Zade, Chetan M. and Bhosale, Jitendra D. and Tupe, Santosh G. and Chaudhary, Preeti M. and Dikundwar, Amol G. and Bendre, Ratnamala S.} } @article { ISI:000317204600005, title = {Chitin synthase inhibitors as antifungal agents}, journal = {Mini-Reviews in Medicinal Chemistry}, volume = {13}, number = {2}, year = {2013}, month = {FEB}, pages = {222-236}, publisher = {BENTHAM SCIENCE PUBL LTD}, address = {EXECUTIVE STE Y-2, PO BOX 7917, SAIF ZONE, 1200 BR SHARJAH, U ARAB EMIRATES}, abstract = {

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.

}, keywords = {Antifungal agents, Chitin synthase, Chitin synthase inhibitors, Nikkomycin, Peptidyl nucleoside antibiotics, Polyoxin}, issn = {1389-5575}, author = {Chaudhary, Preeti M. and Tupe, Santosh G. and Deshpande, Mukund V.} } @article {48300, title = {Design and synthesis of 1,3-diynes as potent antifungal agents against aspergillus fumigatus}, journal = {ChemMedChem}, volume = {18}, year = {2023}, month = {MAY }, type = {Article}, abstract = {

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.

}, keywords = {1, 3-Diynes, Antifungal agents, Aspergillus fumigatus, Cadiot-Chodkiewicz, Glaser-Hay}, issn = {1860-7179}, doi = {10.1002/cmdc.202300013}, author = {Goswami, Lakshmi and Gupta, Lovely and Paul, Sayantan and Vijayaraghavan, Pooja and Bhattacharya, Asish K.} }