First report of canine protothecosis caused by Prototheca wickerhamii in Argentina. Brief literature review.

Protothecosis is an infectious disease caused by microalgae of the genus Prototheca. Prototheca can be found in soil and water and transiently colonize animals. Cutaneous protothecosis can involve not only the skin but also the underlying subcutaneous tissue and lymph nodes.

Synthesis of Novel Triazine-Based Chalcones and 8,9-dihydro-7-pyrimido[4,5-][1,4]diazepines as Potential Leads in the Search of Anticancer, Antibacterial and Antifungal Agents.

This study presents the synthesis of four series of novel hybrid chalcones ()- and ()- and six series of 1,3,5-triazine-based pyrimido[4,5-][1,4]diazepines (-)- and the evaluation of their anticancer, antibacterial, antifungal, and cytotoxic properties. Chalcones ,, ,, ,-, - and the pyrimido[4,5-][1,4]diazepines ,, , ,,-, ,,- exhibited outstanding anticancer activity against a panel of 60 cancer cell lines with GI values between 0.01 and 100 μM and LC values in the range of 4.

Scedosporium boydii finding in an immunocompromised patient and review of the literature.

Background: Scedosporiasis is an emerging mycosis that has gained importance in recent years due to its worldwide prevalence. It is caused by species of the Scedosporium apiospermum complex. These species can cause opportunistic infections in immunocompromised patients and, occasionally, in immunocompetent patients as well.

Extracts of Trichocline sinuata (Asteraceae) as natural sensitizers in the photodynamic inactivation of Candida albicans.

Despite significant progress in the development of phototherapy drugs, it is widely recognized that natural products remain the primary source of new photoactive compounds. Exploring uncharted flora in the east-central region of Argentina may offer a vast array of opportunities to isolate new photoactive molecules or plant extracts with high potential for use in antimicrobial photodynamic therapy (aPDT) against Candida albicans. To assess the photofungicidal potential of T.

Miconazole Nitrate Microparticles in Lidocaine Loaded Films as a Treatment for Oropharyngeal Candidiasis.

Oral candidiasis is an opportunistic infection that affects mainly individuals with weakened immune system. Devices used in the oral area to treat this condition include buccal films, which present advantages over both oral tablets and gels. Since candidiasis causes pain, burning, and itching, the purpose of this work was to develop buccal films loaded with both lidocaine (anesthetic) and miconazole nitrate (MN, antifungal) to treat this pathology topically.

First total synthesis of chromanone A, preparation of related compounds and evaluation of their antifungal activity against , a biofilm forming agent.

A straightforward and convenient approach for the first total syntheses of chromanone A and a related 7-OMe substituted natural product is reported. These unique C-3 substituted 2-hydroxymethyl chromones were recently isolated as fungal metabolites. Chromanone A was synthesized in 25.

Evaluation of the antifungal photodynamic activity of Thymophylla pentachaeta extracts against Candida albicans and its virulence factors.

Background: Candida albicans is one of the most common causative of opportunistic infections. Treatment of candidiasis is challenging considering the few antifungal drugs available and the increase in resistance. Antimicrobial photodynamic therapy (aPDT) is a recently developed therapeutic option that combines a non-toxic photosensitizer (PS) and light to kill the microbial pathogens.

ROS-generating rare-earth coordination networks for photodynamic inactivation of .

Water-ethanol suspensions of 2D coordination network (CN) based on rare earth elements and mixed ligands were evaluated as reactive oxygen species (ROS) generators under UV light irradiation, in contact with a biomimetic substrate (tryptophan) or an O2(1Δg) quencher (1,3-diphenylisobenzofuran; 1,3-DPBF). A combination of bottom-up and top-down strategies was implemented in order to obtain nano-sized CN particles and the subsequent colloidal suspensions were also tested towards photodynamic inactivation of Candida albicans (C. albicans).

[Optimization of variables in photodynamic antifungal assays against Candida species].

Oral infections due to yeasts of the genus Candida are very common in patients with predisposing factors, such as physiological conditions or certain underlying diseases. Moreover, oral candidiasis can also evolve into disseminated forms. In this work, strains of the genus Candida were studied to establish the optimal radiation conditions for photosensitizing compounds, in a photodynamic antifungal therapy protocol.

Water Extract from Inflorescences of Industrial Hemp Futura 75 Variety as a Source of Anti-Inflammatory, Anti-Proliferative and Antimycotic Agents: Results from In Silico, In Vitro and Ex Vivo Studies.

Industrial hemp () is traditionally cultivated as a valuable source of fibers and nutrients. Multiple studies also demonstrated antimicrobial, anti-proliferative, phytotoxic and insecticide effects of the essential oil from hemp female inflorescences. On the other side, only a few studies explored the potential pharmacological application of polar extracts from inflorescences.

New thiazolyl-pyrazoline derivatives bearing nitrogen mustard as potential antimicrobial and antiprotozoal agents.

A new series of N-substituted pyrazoline derivatives 6a-g, 7a-g, 8a-g, and 9a-g was synthetized by reaction of hydrazine derivatives and chalcone-thiazole hybrids bearing nitrogen mustard 5a-g. The chalcones 5a-g were obtained by Claisen-Schmidt condensation of thiazole-2-nitrogen mustard 3 and selected acetophenones 4a-g. These new compounds 6/7/8/9a-g were screened for their antifungal activity against Cryptococcus neoformans, with IC values of 3.

Photodynamic activity of Tagetes minuta extracts against superficial fungal infections.

Candida and dermatophyte species are the most common causes of superficial mycoses because their treatment can be difficult due to limitations of current antifungal drugs in terms of toxicity, bioavailability, interactions, narrow-spectrum activity, and development of resistance. Photodynamic therapy (PDT) involves the topical administration of a photosensitizer in combination with light of an appropriate wavelength and molecular oxygen that produces reactive oxygen species (ROS), which promote damage to several vital components of the microorganism. Tagetes species are known as a source of thiophenes, biologically active compounds whose antifungal activity is enhanced by irradiation with UVA.

Mechanistic studies of Candida albicans photodynamic inactivation with Porophyllum obscurum hexanic extract and its isolated thiophenic compounds.

Porophyllum obscurum (Spreng) DC (Asteraceae) hexanic extract (PoHex) from aerial parts has demonstrated antifungal activity under UVA irradiation against Candida spp. isolates from patients with oropharyngeal candidiasis and four thiophenes were isolated as responsible of the activity. In the present work, we studied the photomechanisms whereby PoHex and their thiophenes produce photoinactivation of C.

On the effect of intramolecular H-bonding in the configurational assessment of polyhydroxylated compounds with computational methods. The hyacinthacines case.

Hyacinthacines are important members of the pyrrolizidine family, with several compounds having ambiguous, revised or unverified structures. Herein we thoroughly explored the performance DP4 and DP4+ for the in silico stereoassignment of hyacinthacines A1, A2 and five synthetic isomers. The results suggested that the quality of the predictions strongly depended on the conformational landscape provided by DFT energies, with five compounds correctly assigned.

Approaches to the mechanism of antifungal activity of Zuccagnia punctata-Larrea nitida bi-herbal combination.

Background: In our previous study the synergism of four combinations of Zuccagnia punctata (ZpE) and Larrea nitida (LnE) exudates with the reliable statistical-based MixLow method was assessed, and the markers of the most anti-C. albicans synergistic ZpE-LnE bi-herbal combination were quantified according to European Medicines Agency (EMA).

Purpose: To study the mechanisms of action as well as the cytotoxic properties of the ZpE-LnE most synergistic combination found in the previous work.

General Quantum-Based NMR Method for the Assignment of Absolute Configuration by Single or Double Derivatization: Scope and Limitations.

The determination of the absolute configuration of chiral alcohols and amines is typically carried out with modified Mosher methods involving a double-derivatization strategy. On the other hand, the number of robust and reliable methods to accomplish that goal using a single derivatization approach is much less abundant and mainly limited to secondary alcohols or primary amines. Herein, we report a conceptually novel strategy to settle the most likely absolute configuration of a wide variety of substrates and chiral derivatizing agents following a single-derivatization experiment coupled with quantum calculations of NMR shifts and DP4+ analysis.

Synthesis and DFT Calculations of Novel Vanillin-Chalcones and Their 3-Aryl-5-(4-(2-(dimethylamino)-ethoxy)-3-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbaldehyde Derivatives as Antifungal Agents.

Novel ()-1-(aryl)-3-(4-(2-(dimethylamino)ethoxy)-3-methoxyphenyl) prop-2-en-1-ones were synthesized by a Claisen-Schmidt reaction of 4-(2-(dimethylamino)ethoxy)-3-methoxy-benzaldehyde () with several acetophenone derivatives . Subsequently, cyclocondensation reactions of chalcones with hydrazine hydrate afforded the new racemic 3-aryl-5-(4-(2-(dimethylamino)ethoxy)-3-methoxyphenyl)-4,5-dihydro-1-pyrazole-1-carbaldehydes when the reaction was carried out in formic acid. The antifungal activity of both series of compounds against eight fungal species was determined.

Plant phenolics and terpenoids as adjuvants of antibacterial and antifungal drugs.

Background: The intensive use of antibacterial and antifungal drugs has dramatically increased the microbial resistance and has led to a higher number of difficult-to-eradicate infections. Combination therapy with two or more antimicrobial drugs has emerged some years ago to overcome the issue, but it has proven to be not completely effective. Natural secondary metabolites of MW ≤ 500 represent promising adjuvants for antimicrobials and have been the object of several researches that have increased in the last two decades.

Antifungal photosensitive activity of Porophyllum obscurum (Spreng.) DC.: Correlation of the chemical composition of the hexane extract with the bioactivity.

We report Porophyllum obscurum as a source of new photosensitizers with potential use in Photodynamic Therapy as an alternative for oropharyngeal candidiasis treatment. The antifungal photosensitive activity of different extracts from P. obscurum was evaluated by using microdilution and bioautographic assays.

Antifungal toxicity of linear geranylphenol. Influence of oxigenate substituents.

Twenty four linear geranylphenols were evaluated for their antifungal properties against ATCC and clinical isolates of Candida albicans and Cryptococcus neoformans. For the analysis of their antifungal behavior the compounds were grouped into two series: (i) compounds with only one geranyl substituent on the benzene ring and (ii) compounds with two geranyl moieties on the benzene ring. Results showed that compounds of series (i) present better antifungal activities than those of series (ii).

Hybrid Molecules Containing a 7-Chloro-4-aminoquinoline Nucleus and a Substituted 2-Pyrazoline with Antiproliferative and Antifungal Activity.

Twenty-four new hybrid analogues (15-38) containing 7-chloro-4-aminoquinoline and 2-pyrazoline N-heterocyclic fragments were synthesized. Twelve of the new compounds were evaluated against 58 human cancer cell lines by the U.S.

Antifungal drugs combinations: a patent review 2000-2015.

Introduction: Combination therapy has emerged as an approach to improve the efficacy of antifungal drugs. Its main objective is to achieve synergistic interaction with higher antifungal properties and lower toxic effects than each substance alone.

Areas Covered: Twenty-four patents disclosed in the period of 2000-2015 were covered in this review.

Photodynamic inactivation of oropharyngeal Candida strains.

Oropharyngeal candidiasis (OPC) is an infection frequent in immunocompromised patients. Photodynamic therapy is an alternative to conventional treatments, based on the utilization of compounds that inhibit or kill microorganisms only under the effect of light, process known as Photodynamic Inactivation (PDI). In the present study, PDI of Candida spp.

Efficient synthesis of novel 3-aryl-5-(4-chloro-2-morpholinothiazol-5-yl)-4,5-dihydro-1H-pyrazoles and their antifungal activity alone and in combination with commercial antifungal agents.

The α,β-unsaturated carbonyl compounds 5a-f were prepared by reaction between 2-chloro-4-morpholinothiazol-5-carbaldehyde 3 and substituted acetophenones 4a-f. Treatment of compounds 5a-f with hydrazine hydrate employing mild reaction conditions led to the formation of 4,5-dihydro-1H-pyrazoles 6a-f. Then the treatment with acetic anhydride or formic acid afforded the expected 4,5-dihydro-1H-pyrazoles 7a-f and 8a-f.