Search Results - "Hutter, Sébastien"
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Structural simplification of the 3‐nitroimidazo[1,2‐ a ]pyridine antileishmanial pharmacophore: Design, synthesis, and antileishmanial activity of novel 2,4-disubstituted 5-nitroimidazoles
Published in Heterocyclic Communications (05-08-2024)“…As part of our ongoing antileishmanial structure–activity relationship study, a structural simplification of the 3‐nitroimidazo[1,2‐ a ]pyridine ring to a…”
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A New Thienopyrimidinone Chemotype Shows Multistage Activity against Plasmodium falciparum, Including Artemisinin-Resistant Parasites
Published in Microbiology spectrum (31-10-2021)“…Human malaria infection begins with a one-time asymptomatic liver stage followed by a cyclic symptomatic blood stage. For decades, the research for novel…”
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Nongenotoxic 3‑Nitroimidazo[1,2‑a]pyridines Are NTR1 Substrates That Display Potent in Vitro Antileishmanial Activity
Published in ACS medicinal chemistry letters (10-01-2019)“…Twenty nine original 3-nitroimidazo[1,2-a]pyridine derivatives, bearing a phenylthio (or benzylthio) moiety at position 8 of the scaffold, were synthesized…”
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4
Design, synthesis and biological evaluation of novel 4-alkapolyenylpyrrolo[1,2-a]quinoxalines as antileishmanial agents – Part III
Published in European journal of medicinal chemistry (23-06-2014)“…A series of new 4-alkapolyenylpyrrolo[1,2-a]quinoxaline derivatives, original and structural analogues of alkaloid chimanine B and of previously described…”
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Antimalarial artemisinin-based combination therapies (ACT) and COVID-19 in Africa: In vitro inhibition of SARS-CoV-2 replication by mefloquine-artesunate
Published in International journal of infectious diseases (01-10-2020)“…At the end of November 2019, a novel coronavirus responsible for respiratory tract infections (COVID-19) emerged in China. Despite drastic containment…”
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In Vitro Antiviral Activity of Doxycycline against SARS-CoV-2
Published in Molecules (Basel, Switzerland) (31-10-2020)“…In December 2019, a new severe acute respiratory syndrome coronavirus (SARS-CoV-2), causing coronavirus disease 2019 (COVID-19), emerged in Wuhan, China…”
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Antimalarial drugs inhibit the replication of SARS-CoV-2: An in vitro evaluation
Published in Travel medicine and infectious disease (01-09-2020)“…In December 2019, a new severe acute respiratory syndrome coronavirus (SARS-CoV-2) causing coronavirus diseases 2019 (COVID-19) emerged in Wuhan, China…”
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Methylene blue inhibits replication of SARS-CoV-2 in vitro
Published in International journal of antimicrobial agents (01-12-2020)“…•Methylene blue (MB) has a 50% cytotoxic concentration (CC50) >100 μM in Vero E6 cells.•MB inhibited SARS-CoV-2 replication in Vero E6 cells (EC50 = 0.30 ±…”
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Synthesis and Antiplasmodial Evaluation of 4-Carboxamido- and 4-Alkoxy-2-Trichloromethyl Quinazolines
Published in Molecules (Basel, Switzerland) (27-08-2020)“…From three previously identified antiplasmodial hit compounds ( - ) and inactive series ( ), all based on a 2-trichloromethylquinazoline scaffold, we conducted…”
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10
Treating leishmaniasis in Amazonia, part 2: Multi-target evaluation of widely used plants to understand medicinal practices
Published in Journal of ethnopharmacology (10-05-2022)“…Leishmaniasis are widely distributed among tropical and subtropical countries, and remains a crucial health issue in Amazonia. Indigenous groups across…”
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Synthesis of Nitrostyrylthiazolidine-2,4-dione Derivatives Displaying Antileishmanial Potential
Published in Pharmaceuticals (Basel, Switzerland) (03-07-2024)“…A series of 61 thiazolidine-2,4-diones bearing a styryl group at position 5 was synthesized in 2-5 steps and their structure was proved by elemental and…”
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12
Looking for new antiplasmodial quinazolines: DMAP-catalyzed synthesis of 4-benzyloxy- and 4-aryloxy-2-trichloromethylquinazolines and their in vitro evaluation toward Plasmodium falciparum
Published in European journal of medicinal chemistry (25-08-2016)“…A DMAP catalyzed synthesis of new 4-benzyloxy- and 4-aryloxy-2-trichloromethylquinazolines was studied, in a view to react 4-chloroquinazolines with poorly…”
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Pd-catalyzed C-C and C-N cross-coupling reactions in 2-aminothieno[3,2-]pyrimidin-4(3)-one series for antiplasmodial pharmacomodulation
Published in RSC advances (06-07-2022)“…In 2015, we identified gamhepathiopine (M1), a 2- tert -butylaminothieno[3,2- d ]pyrimidin-4(3 H )-one antiplasmodial hit targeting all development stages of…”
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New antiplasmodial 4-amino-thieno[3,2-d]pyrimidines with improved intestinal permeability and microsomal stability
Published in European journal of medicinal chemistry (05-03-2023)“…The increasing number of Plasmodium falciparum strains resistant to current treatments justifies the urgent need to discover new compounds active on several…”
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4-Substituted Thieno[3,2-d]pyrimidines as Dual-Stage Antiplasmodial Derivatives
Published in Pharmaceuticals (Basel, Switzerland) (01-07-2022)“…Malaria remains one of the major health problems worldwide. The increasing resistance of Plasmodium to approved antimalarial drugs requires the development of…”
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Discovery of new hit-molecules targeting Plasmodium falciparum through a global SAR study of the 4-substituted-2-trichloromethylquinazoline antiplasmodial scaffold
Published in European journal of medicinal chemistry (05-01-2017)“…From 4 antiplasmodial hit-molecules identified in 2-trichloromethylquinazoline series, we conducted a global Structure-Activity relationship (SAR) study…”
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Novel thienopyrimidones targeting hepatic and erythrocytic stages of Plasmodium parasites with increased microsomal stability
Published in European journal of medicinal chemistry (05-12-2023)“…Based on the structure of a previously identified hit, Gamhepathiopine 1, which showed promising antiplasmodial activity, but poor microsomal stability,…”
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Synthesis of antiplasmodial 2-aminothieno[3,2-d]pyrimidin-4(3H)-one analogues using the scaffold hopping strategy
Published in European journal of medicinal chemistry (05-11-2022)“…Gamhepathiopine (also known as M1), is a multi-stage acting antiplasmodial 2-tert-butylaminothieno[3,2-d]pyrimidin-4(3H)-one hydrochloride that was first…”
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Antiviral Activity of Repurposing Ivermectin against a Panel of 30 Clinical SARS-CoV-2 Strains Belonging to 14 Variants
Published in Pharmaceuticals (Basel, Switzerland) (02-04-2022)“…Over the past two years, several variants of SARS-CoV-2 have emerged and spread all over the world. However, infectivity, clinical severity, re-infection,…”
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Synthesis and antiplasmodial activity of new 4-aryl-2-trichloromethylquinazolines
Published in Bioorganic & medicinal chemistry (2008)“…A series of original 4-aryl-substituted 2-trichloromethylquinazoline derivatives was synthesized using a microwave-assisted Suzuki-Miyaura cross-coupling…”
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