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FR290581, a novel sordarin derivative: synthesis and antifungal activity

Sordarin is a unique natural product antifungal agent that is an inhibitor of elongation factor 2. To improve biological activity, we synthesized various compounds by novel modification of the aglycone, sordaricin. As a result, we have discovered the novel sordarin derivativeFR290581. This compound exhibited superior activity and a good pharmacokinetic profile, and also displayed good in vivo activity against Candida albicans.
Source: The Aspergillus Website - updates - Category: Respiratory Medicine Authors: Source Type: news

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Novelmacrocyclic amidinourea derivatives 11, 18, and 25 were synthesized and evaluated as antifungal agentsagainstwild-type and fluconazoleresistantCandidaspecies.
Source: The Aspergillus Website - updates - Category: Respiratory Medicine Authors: Source Type: news
MK-3118 is as an orally active new antifungal in the early stage of clinical development that inhibits the biosynthesis of β-(1,3)-glucan. We evaluated the invitro activity of this compound against wild-type and echinocandin-resistant (ER) isolates containing mutations in the FKS gene(s) of Candida spp. and Aspergillus spp.MK-3118 demonstrated enhanced efficacy for most C. albicans and C.
Source: The Aspergillus Website - updates - Category: Respiratory Medicine Authors: Source Type: news
Abstract Amniotic membrane (AM) is frequently used in ophthalmologic surgery for rapid ocular surface reconstruction. Sometimes it may create a major problem with associated infections after biofilm formation over the membrane. To overcome this problem, AM was coated with the antimicrobial peptide clavanin A. The antifungal activity of clavanin A in the native and self-assembled form was determined against the common ocular surface pathogens Candida albicans, Aspergillus fumigatus, Alternaria sp. and Fusarium sp. Biofilm formation over the coated surface was significantly reduced in comparison with the uncoated me...
Source: Biofouling - Category: Molecular Biology Authors: Tags: Biofouling Source Type: research
Publication date: 15 February 2018 Source:Journal of Molecular Structure, Volume 1154 Author(s): Raghavendra P. Bakale, Ganesh N. Naik, Shrinath S. Machakanur, Chandrashekhar V. Mangannavar, Iranna S. Muchchandi, Kalagouda B. Gudasi A hydrazone ligand has been synthesized by the condensation of 2-nitrobenzaldehyde and hydralazine, and its Co(II), Ni(II), Cu(II) and Zn(II) complexes have been reported. Structural characterization of the ligand and its metal complexes has been performed by various spectroscopic [IR, NMR, UV–Vis, Mass], thermal and other physicochemical methods. The structure of the ligand and its Ni(I...
Source: Journal of Molecular Structure - Category: Molecular Biology Source Type: research
CONCLUSION: The Cu (II) complexes exhibit square planar geometry. A comparative study of inhibition values of the individual metals and their complexes indicate that the complexes exhibit higher antimicrobial activity than the individual metals. Superoxide dismutase and reducing power activities of the copper complexes have also been studied. Depending on the molecular structure, the Cu (II) NHC complex possess promising SOD mimetic activities. Further we are trying to explore more biological properties of Cu (II) NHC complexes in vitro and in vivo. PMID: 29022998 [PubMed - in process]
Source: Pakistan Journal of Biological Sciences: PJBS - Category: Biomedical Science Authors: Tags: Pak J Biol Sci Source Type: research
The cholesterol-lowering agents known as statins have in vitro activities against human pathogenic fungi, such as Candida species, Cryptococcus neoformans, and Zygomycetes. Synergy between statins and azoles against these fungi has also been reported. We evaluated the in vitro activities of two statins, lovastatin andsimvastatin, alone and in combination with azoles and amphotericin B, against clinical isolates ofAspergillus spp.
Source: The Aspergillus Website - updates - Category: Respiratory Medicine Authors: Source Type: news
Statins are a class of drugs widely used for lowering high cholesterol levels through their action on 3-hydroxy-3-methylglutaryl-CoA reductase, a key enzyme in the synthesis of cholesterol. We studied the effects of two major statins,simvastatin and atorvastatin, on five Candida species andAspergillus fumigatus. The statins strongly inhibited the growth of all species, except Candida krusei. Supplementation of Candida albicans and A.
Source: The Aspergillus Website - updates - Category: Respiratory Medicine Authors: Source Type: news
Ilicicolin H is a polyketide-nonribosomal peptide synthase (NRPS)-natural product isolated from Gliocadium roseum, which exhibits potent and broad spectrum antifungal activity, with sub- μg/mL MICs against Candida spp., Aspergillus fumigatus, and Cryptococcus spp. It showed a novel mode of action, potent inhibition (IC50 = 2-3 ng/mL) of the mitochondrial cytochrome bc1 reductase, and over 1000-fold selectivity relative to rat liver cytochrome bc1 reductase.
Source: The Aspergillus Website - updates - Category: Respiratory Medicine Authors: Source Type: news
The activities ofR-135853, a novel sordarin derivative that possesses a 1,4-oxazepane ring moiety, were evaluated in vitro and in vivo.R-135853 exhibited potent in vitro activities against Candida albicans (fluconazole-susceptible strains), Candida glabrata, Candida tropicalis, and Cryptococcus neoformans, with MICs at which 90% of isolates were inhibited of 0.03, 1, 0.5, and 0.5 microg/ml, respectively.
Source: The Aspergillus Website - updates - Category: Respiratory Medicine Authors: Source Type: news
Candida is the most common fungal pathogen of humans worldwide and has become a major clinical problem because of the growing number of immunocompromised patients, who are susceptible to infection. Moreover, the number of available antifungals is limited, and antifungal-resistantCandida strains are emerging. New and effective antifungals are therefore urgently needed. Here, we discovered a small molecule with activity againstCandida spp. bothin vitro andin vivo.
Source: The Aspergillus Website - updates - Category: Respiratory Medicine Authors: Source Type: news
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