Philippe M. Loiseau
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View article: Are hydrophilic deep eutectic solvents a potential vehicle for topical delivery of Amphotericin B against cutaneous leishmaniasis? An investigation of physicochemical properties, tolerability and antileishmanial efficacy
Are hydrophilic deep eutectic solvents a potential vehicle for topical delivery of Amphotericin B against cutaneous leishmaniasis? An investigation of physicochemical properties, tolerability and antileishmanial efficacy Open
Deep eutectic solvents (DES) are homogenous, low-melting mixtures that are liquid at ambient temperature. Recently, DES have attracted interest as novel alternatives to traditional solvents in cutaneous formulations. The aim of this work w…
View article: Resistance to Antileishmanial Drug Candidates: A Flowchart for an Early Phenotypic Evaluation of Risk
Resistance to Antileishmanial Drug Candidates: A Flowchart for an Early Phenotypic Evaluation of Risk Open
Background: Drug development for leishmaniases treatment follows a very selective process in order to propose drug candidates that possess all the qualities that meet the strict specifications of the pharmaceutical industry. Drug resistanc…
View article: Re-sensitization of antimony-resistant Leishmania by highly potent SbV-porphyrin through the involvement of ERG6-coding gene
Re-sensitization of antimony-resistant Leishmania by highly potent SbV-porphyrin through the involvement of ERG6-coding gene Open
Leishmaniasis chemotherapy faces significant challenges, including high costs, severe side effects, and the emergence of drug-resistant parasites, demanding global efforts to identify novel antileishmanial agents. Pentavalent antimony (SbV…
View article: Chemical analysis by molecular networking methods on extracts of Saba senegalensis (A.DC.) Pichon (Apocynaceae) and its anthelmintic activity on Caenorhabditis elegans
Chemical analysis by molecular networking methods on extracts of Saba senegalensis (A.DC.) Pichon (Apocynaceae) and its anthelmintic activity on Caenorhabditis elegans Open
International audience
View article: Dioecy impacts the chemical profile and biological activities of essential oils from leaves of <i>Pistacia lentiscus</i> L.
Dioecy impacts the chemical profile and biological activities of essential oils from leaves of <i>Pistacia lentiscus</i> L. Open
peer reviewed
View article: Pharmacophore-guided optimization of the hit compound CTN1122 in the design of promising imidazo[1,2-<i>a</i>]pyrazine derivatives targeting the casein kinase 1 for antileishmanial therapy
Pharmacophore-guided optimization of the hit compound CTN1122 in the design of promising imidazo[1,2-<i>a</i>]pyrazine derivatives targeting the casein kinase 1 for antileishmanial therapy Open
Docking studies revealed key pharmacophores for L-CK1.2 inhibition. 14 analogs were synthesized; compound 30 showed the best antileishmanial activity and submicromolar L-CK1.2 inhibition without significant cytotoxicity.
View article: Effect of Phlebotomus papatasi on the fitness, infectivity and antimony-resistance phenotype of antimony-resistant Leishmania major Mon-25
Effect of Phlebotomus papatasi on the fitness, infectivity and antimony-resistance phenotype of antimony-resistant Leishmania major Mon-25 Open
Leishmania major is responsible for zoonotic cutaneous leishmaniasis. Therapy is mainly based on the use of antimony-based drugs; however, treatment failures and illness relapses were reported. Although studies were developed to understand…
View article: In silico and in vitro activity of thio-linked pyrimidine-based compounds against Leishmania donovani
In silico and in vitro activity of thio-linked pyrimidine-based compounds against Leishmania donovani Open
International audience
View article: The Synthesis of 2′-Hydroxychalcones under Ball Mill Conditions and Their Biological Activities
The Synthesis of 2′-Hydroxychalcones under Ball Mill Conditions and Their Biological Activities Open
Chalcones are polyphenols that belong to the flavonoids family, known for their broad pharmacological properties. They have thus attracted the attention of chemists for their obtention and potential activities. In our study, a library of c…
View article: Chemoselective Synthesis and Anti-Kinetoplastidal Properties of 2,6-Diaryl-4H-tetrahydro-thiopyran-4-one S-Oxides: Their Interplay in a Cascade of Redox Reactions from Diarylideneacetones
Chemoselective Synthesis and Anti-Kinetoplastidal Properties of 2,6-Diaryl-4H-tetrahydro-thiopyran-4-one S-Oxides: Their Interplay in a Cascade of Redox Reactions from Diarylideneacetones Open
2,6-Diaryl-4H-tetrahydro-thiopyran-4-ones and corresponding sulfoxide and sulfone derivatives were designed to lower the major toxicity of their parent anti-kinetoplatidal diarylideneacetones through a prodrug effect. Novel diastereoselect…
View article: Deciphering the mechanism of action of VP343, an antileishmanial drug candidate, in Leishmania infantum
Deciphering the mechanism of action of VP343, an antileishmanial drug candidate, in Leishmania infantum Open
Antileishmanial chemotherapy is currently limited due to severe toxic side effects and drug resistance. Hence, new antileishmanial compounds based on alternative approaches, mainly to avoid the emergence of drug resistance, are needed. The…
View article: Inhibition of the macrophage demethylase LSD1 reverses <i>Leishmania amazonensis</i> -induced transcriptomic changes and causes a decrease in parasite load
Inhibition of the macrophage demethylase LSD1 reverses <i>Leishmania amazonensis</i> -induced transcriptomic changes and causes a decrease in parasite load Open
Intracellular pathogens exploit host cell functions to favor their own survival. In recent years, the subversion of epigenetic regulation has emerged as a key microbial strategy to modify host cell gene expression and evade antimicrobial i…
View article: CCDC 2258486: Experimental Crystal Structure Determination
CCDC 2258486: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2258488: Experimental Crystal Structure Determination
CCDC 2258488: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2258490: Experimental Crystal Structure Determination
CCDC 2258490: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2258487: Experimental Crystal Structure Determination
CCDC 2258487: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2258489: Experimental Crystal Structure Determination
CCDC 2258489: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Mechanochemical Studies on Coupling of Hydrazines and Hydrazine Amides with Phenolic and Furanyl Aldehydes—Hydrazones with Antileishmanial and Antibacterial Activities
Mechanochemical Studies on Coupling of Hydrazines and Hydrazine Amides with Phenolic and Furanyl Aldehydes—Hydrazones with Antileishmanial and Antibacterial Activities Open
Hydrazone compounds represent an important area of research that includes, among others, synthetic approaches and biological studies. A series of 17 hydrazones have been synthesized by mechanochemical means. The fragments chosen were pheno…
View article: Supramolecular assemblies from antimony(V) complexes for the treatment of leishmaniasis
Supramolecular assemblies from antimony(V) complexes for the treatment of leishmaniasis Open
The pentavalent meglumine antimoniate (MA) is still a first-line drug in the treatment of leishmaniasis in several countries. As an attempt to elucidate its mechanism of action and develop new antimonial drugs with improved therapeutic pro…
View article: Optimization of a highly-efficient hydro-CO2 piston for commercial refrigeration
Optimization of a highly-efficient hydro-CO2 piston for commercial refrigeration Open
International audience
View article: Design of Anti-infectious Agents from Lawsone in a Three-Component Reaction with Aldehydes and Isocyanides
Design of Anti-infectious Agents from Lawsone in a Three-Component Reaction with Aldehydes and Isocyanides Open
The first effective synthetic approach to naphthofuroquinones via a reaction involving lawsone, various aldehydes, and three isocyanides under microwave irradiation afforded derivatives in moderate to good yields. In addition, for less-rea…
View article: Stimulation of Acanthamoeba castellanii excystment by enzyme treatment and consequences on trophozoite growth
Stimulation of Acanthamoeba castellanii excystment by enzyme treatment and consequences on trophozoite growth Open
Acanthamoeba castellanii is a widespread Free-Living Amoeba (FLA) that can cause severe ocular or cerebral infections in immunocompetent and immunocompromised patients, respectively, besides its capacity to transport diverse pathogens. Dur…
View article: Nanoassemblies from Amphiphilic Sb Complexes Target Infection Sites in Models of Visceral and Cutaneous Leishmaniases
Nanoassemblies from Amphiphilic Sb Complexes Target Infection Sites in Models of Visceral and Cutaneous Leishmaniases Open
This work aims to evaluate whether nanoassemblies (NanoSb) made from antimony(V) complexes with octanoyl-N-methylglucamide (SbL8) or decanoyl-N-methylglucamide (SbL10) would effectively target the infection sites in visceral and cutaneous …
View article: Formulation of Amphotericin B in PEGylated Liposomes for Improved Treatment of Cutaneous Leishmaniasis by Parenteral and Oral Routes
Formulation of Amphotericin B in PEGylated Liposomes for Improved Treatment of Cutaneous Leishmaniasis by Parenteral and Oral Routes Open
Liposomal amphotericin B (AmB) or AmBisome® is the most effective and safe therapeutic agent for visceral leishmaniasis (VL), but its clinical efficacy is limited in cutaneous leishmaniasis (CL) and HIV/VL co-infection. The aim of this wor…
View article: The Potential of 2-Substituted Quinolines as Antileishmanial Drug Candidates
The Potential of 2-Substituted Quinolines as Antileishmanial Drug Candidates Open
There is a need for new, cost-effective drugs to treat leishmaniasis. A strategy based on traditional medicine practiced in Bolivia led to the discovery of the 2-substituted quinoline series as a source of molecules with antileishmanial ac…
View article: Targeting chalcone binding sites in living Leishmania using a reversible fluorogenic benzochalcone probe
Targeting chalcone binding sites in living Leishmania using a reversible fluorogenic benzochalcone probe Open
Chalcones (1,3-diphenyl-2-propen-1-ones) either natural or synthetic have a plethora of biological properties including antileishmanial activities, but their development as drugs is hampered by their largely unknown mechanisms of action. W…
View article: Minor Impact of A258D Mutation on Biochemical and Enzymatic Properties of Leishmania infantum GDP-Mannose Pyrophosphorylase
Minor Impact of A258D Mutation on Biochemical and Enzymatic Properties of Leishmania infantum GDP-Mannose Pyrophosphorylase Open
Background: Leishmaniasis, a vector-borne disease caused by the protozoan parasite from the genus Leishmania, is endemic to tropical and subtropical areas. Few treatments are available against leishmaniasis, with all presenting issues of t…
View article: Synthesis and Biological Profiles of Some Benzimidazolyl-chalcones as Anti-leishmanial and Trypanocidal Agents
Synthesis and Biological Profiles of Some Benzimidazolyl-chalcones as Anti-leishmanial and Trypanocidal Agents Open
Background: Benzimidazole constitutes a starting point for the development of new antiprotozoal agents since this nucleus exists in several pharmacologically significant molecules, in particular possessing antifungal, antiviral, antibacter…