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List of works by Sergio Wittlin

2,4-Diaminothienopyrimidines as orally active antimalarial agents

scientific article published on 28 January 2014

3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential

scientific article

3-Alkoxy-1,2-Dioxolanes: Synthesis and Evaluation as Potential Antimalarial Agents

scientific article published on April 14, 2011

3-Hydroxy-N'-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally

scientific article published on 27 June 2017

A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum-Infected Mouse Models from Structure-Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines

scientific article published on 26 October 2015

A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria

scientific article

A new double-antibody sandwich ELISA targeting Plasmodium falciparum aldolase to evaluate anti-malarial drug sensitivity

scientific article published on 12 October 2009

Aminoindoles, a novel scaffold with potent activity against Plasmodium falciparum

scientific article

Ancient Chinese methods are remarkably effective for the preparation of artemisinin-rich extracts of Qing Hao with potent antimalarial activity.

scientific article

Anti-malarial ozonides OZ439 and OZ609 tested at clinically relevant compound exposure parameters in a novel ring-stage survival assay

scientific article published on 18 December 2019

Antimalarial activity of N-alkyl amine, carboxamide, sulfonamide, and urea derivatives of a dispiro-1,2,4-trioxolane piperidine

scientific article published on 22 August 2006

Antimalarial activity of novel pyrrolizidinyl derivatives of 4-aminoquinoline

scientific article

Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies

scientific article

Antimalarial mannoxanes: hybrid antimalarial drugs with outstanding oral activity profiles and a potential dual mechanism of action

scientific article published on 20 June 2011

Antiparasitic agents: new drugs on the horizon

scientific article published on 29 May 2012

Antiprotozoal Selectivity of Diimidazoline N-Phenylbenzamides

scientific article published on 16 January 2015

Arylmethylamino steroids as antiparasitic agents

scientific article published on 17 February 2017

Benzo[b]quinolizinium Derivatives Have a Strong Antimalarial Activity and Inhibit Indoleamine Dioxygenase

scientific article published on 12 October 2015

Blood schizontocidal and gametocytocidal activity of 3-hydroxy-N'-arylidenepropanehydrazonamides: a new class of antiplasmodial compounds

scientific article published on 25 September 2014

CPAP is a novel stat5-interacting cofactor that augments stat5-mediated transcriptional activity

scientific article (publication date: September 2002)

CRISPR-Cas9-modified pfmdr1 protects Plasmodium falciparum asexual blood stages and gametocytes against a class of piperazine-containing compounds but potentiates artemisinin-based combination therapy partner drugs

scientific article

Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling

scientific article

Characterization of the two major CYP450 metabolites of ozonide (1,2,4-trioxolane) OZ277.

scientific article published on 30 January 2008

Comparative antimalarial activities of six pairs of 1,2,4,5-tetraoxanes (peroxide dimers) and 1,2,4,5,7,8-hexaoxonanes (peroxide trimers).

scientific article published on 7 May 2007

Comparative embryotoxicity of different antimalarial peroxides: in vitro study using the rat whole embryo culture model (WEC).

scientific article published on 11 August 2010

Comparative ex vivo activity of novel endoperoxides in multidrug-resistant plasmodium falciparum and P. vivax

scientific article

Comparison of SYBR Green I-, PicoGreen-, and [3H]-hypoxanthine-based assays for in vitro antimalarial screening of plants from Nigerian ethnomedicine

scientific article published on 18 February 2010

Compounds structurally related to ellagic acid show improved antiplasmodial activity

scientific article published on 17 November 2008

Corrigendum: A novel multiple-stage antimalarial agent that inhibits protein synthesis

scientific article published on 25 May 2016

Cysteine-Rich Protective Antigen (CyRPA) as promising blood-stage candidate protein for inclusion in a malaria subunit vaccine

scholarly article by Paola Favuzza et al published 2012 in Malaria Journal

Discovery and Characterization of ACT-451840: an Antimalarial Drug with a Novel Mechanism of Action

scientific article

Discovery of Novel Benzo[a]phenoxazine SSJ-183 as a Drug Candidate for Malaria

scientific article

Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy

scientific article published on 10 September 2016

Discovery of dual function acridones as a new antimalarial chemotype

scientific article

Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum

scientific article

First-in-man safety and pharmacokinetics of synthetic ozonide OZ439 demonstrates an improved exposure profile relative to other peroxide antimalarials

scientific article published on February 2013

Global metabolic responses of NMRI mice to an experimental Plasmodium berghei infection

scientific article published on 23 July 2008

Histone methyltransferase inhibitors are orally bioavailable, fast-acting molecules with activity against different species causing malaria in humans

scientific article

Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead Chemistry

scientific article

Identification and deconvolution of cross-resistance signals from antimalarial compounds using multidrug-resistant Plasmodium falciparum strains

scientific article

Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ null Mouse Model of Malaria

scientific article published on 17 April 2018

Identification of New Human Malaria Parasite Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors by Pharmacophore and Structure-Based Virtual Screening

scientific article published on 25 February 2016

Identification of Taxreb107 as a lactogenic hormone responsive gene in mammary epithelial cells

scientific article published on October 2003

Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle

scientific article published on 17 October 2016

Identification of a new chemical class of antimalarials

scientific article

Identification of an antimalarial synthetic trioxolane drug development candidate

scientific article

In vitro activity of anti-malarial ozonides against an artemisinin-resistant isolate

scientific article published on 25 January 2017

In vitro and in vivo activity of solithromycin (CEM-101) against Plasmodium species

scientific article published on 14 November 2011

In vitro and in vivo characterization of the antimalarial lead compound SSJ-183 in Plasmodium models

scientific article

In vitro and in vivo interaction of synthetic peroxide RBx11160 (OZ277) with piperaquine in Plasmodium models

scientific article published on 7 November 2006

In vitro assessment of the pharmacodynamic properties and the partitioning of OZ277/RBx-11160 in cultures of Plasmodium falciparum

scientific article published on 30 May 2006

In vitro assessment of the pharmacodynamic properties of DB75, piperaquine, OZ277 and OZ401 in cultures of Plasmodium falciparum

scientific article published on 30 July 2008

In vitro interaction of artemisinin derivatives or the fully synthetic peroxidic anti-malarial OZ277 with thapsigargin in Plasmodium falciparum strains

scientific article published on 31 January 2013

In vitro susceptibility of P. falciparum populations from Colombia and Tanzania to a new synthetic peroxide (OZ277).

scientific article published on June 2007

In vitroantiplasmodial activity and toxicity assessment of some plants from Nigerian ethnomedicine

scientific article published on August 26, 2010

Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT): cocrystal structures of pyrazolopyrans with potent blood- and liver-stage activities

scientific article

Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria.

scientific article published on 26 November 2018

Isothermal microcalorimetry, a new tool to monitor drug action against Trypanosoma brucei and Plasmodium falciparum

scientific article

Long-Lasting and Fast-Acting in Vivo Efficacious Antiplasmodial Azepanylcarbazole Amino Alcohol

scientific article published on 28 November 2017

Malaria-infected mice are cured by oral administration of new artemisinin derivatives

scientific article published on 31 January 2008

Mechanism of antimalarial action of the synthetic trioxolane RBX11160 (OZ277).

scientific article published on 4 December 2006

Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: part 1.

scientific article

Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a softfocus kinase library: part 2.

scientific article published on 23 October 2014

Methotrexate and aminopterin lack in vivo antimalarial activity against murine malaria species

scientific article published on 13 June 2009

Monoclonal Antibodies That Recognize the Alkylation Signature of Antimalarial Ozonides OZ277 (Arterolane) and OZ439 (Artefenomel).

scientific article

Novel Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase with Anti-malarial Activity in the Mouse Model

scientific article

Novel in vivo active anti-malarials based on a hydroxy-ethyl-amine scaffold

scientific article published on 11 December 2012

Novel orally active antimalarial thiazoles

scientific article

Novel synthetic route for antimalarial benzo[a]phenoxazine derivative SSJ-183 and two active metabolites

scientific article

Occurrence of sesquiterpene derivatives in Scleria striatonux de wild (Cyperaceae).

scientific article

Okundoperoxide, a bicyclic cyclofarnesylsesquiterpene endoperoxide from Scleria striatinux with antiplasmodial activity

scientific article published on February 2009

Open Source Drug Discovery: Highly Potent Antimalarial Compounds Derived from the Tres Cantos Arylpyrroles

scientific article published on 14 September 2016

Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of Malaria

scientific article published on 11 July 2011

Passive immunoprotection of Plasmodium falciparum-infected mice designates the CyRPA as candidate malaria vaccine antigen

scientific article (publication date: 15 June 2012)

Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).

scientific article published on 11 June 2007

Plasmodium vivax: in vitro susceptibility of blood stages to synthetic trioxolane compounds and the diamidine DB75.

scientific article published on 3 February 2006

Potent antimalarial 1,2,4-trioxanes through perhydrolysis of epoxides

scientific article published on 9 April 2013

Preclinical Evaluation of the Antifolate QN254, 5-Chloro- N'6'-(2,5-Dimethoxy-Benzyl)-Quinazoline-2,4,6-Triamine, as an Antimalarial Drug Candidate

scientific article

Probing the antimalarial mechanism of artemisinin and OZ277 (arterolane) with nonperoxidic isosteres and nitroxyl radicals

scientific article published on 22 December 2009

Prodrugs of reverse fosmidomycin analogues

scientific article published on 12 February 2015

Simple Analogues of Qinghaosu (Artemisinin)

scientific article published on May 15, 2012

Socs2 and elf5 mediate prolactin-induced mammary gland development

scientific journal article

Soudanones A-G: Antifungal Isochromanones from the Ascomycetous Fungus Cadophora sp. Isolated from an Iron Mine

scientific article published on 2 June 2015

Spiro and dispiro-1,2,4-trioxolanes as antimalarial peroxides: charting a workable structure-activity relationship using simple prototypes

scientific article published on July 2005

Spiro- and dispiro-1,2-dioxolanes: contribution of iron(II)-mediated one-electron vs two-electron reduction to the activity of antimalarial peroxides

scientific article published on 20 October 2007

Spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane pairs: relationship between peroxide bond iron(II) reactivity, heme alkylation efficiency, and antimalarial activity.

scientific article published on 9 July 2009

Structure-Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines

scientific article published on 31 August 2015

Structure-Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439).

scientific article

Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines

scientific article

Structure-activity relationships for ferriprotoporphyrin IX association and β-hematin inhibition by 4-aminoquinolines using experimental and ab initio methods

scientific article published on 23 April 2013

Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity

scientific article published on 29 October 2013

Synthesis and Biological Properties of a Rhodacyanine Derivatives, SSJ-127, Having High Efficacy against Malaria Protozoa

scholarly article by Masataka Ihara et al published 2009 in Heterocycles

Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents

scientific article published on 25 November 2016

Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a]phenoxazine derivatives

scientific article published on 5 August 2011

Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive 3,7-bis(dialkylamino)phenoxazin-5-ium derivatives

scientific article published on 14 May 2008

Synthesis and in vitro antiprotozoal activities of water-soluble, inexpensive phenothiazinium chlorides

Synthesis of cyanine dyes and investigation of their in vitro antiprotozoal activities

Synthesis of fusidic acid bioisosteres as antiplasmodial agents and molecular docking studies in the binding site of elongation factor-G

Synthesis, Structure−Activity Relationship, and Mode-of-Action Studies of Antimalarial Reversed Chloroquine Compounds

scientific article published on September 9, 2010

Synthetic ozonide drug candidate OZ439 offers new hope for a single-dose cure of uncomplicated malaria

scientific article

The activities of current antimalarial drugs on the life cycle stages of Plasmodium: a comparative study with human and rodent parasites

scientific article

The comparative antimalarial properties of weak base and neutral synthetic ozonides

scientific article published on 22 November 2009

The structure and antimalarial activity of dispiro-1,2,4,5-tetraoxanes derived from (+)-dihydrocarvone

scientific article published on September 29, 2010

The structure-activity relationship of the antimalarial ozonide arterolane (OZ277).

scientific article

Thiazolopyrimidine inhibitors of 2-methylerythritol 2,4-cyclodiphosphate synthase (IspF) from Mycobacterium tuberculosis and Plasmodium falciparum

scientific journal article

Triclosan is minimally effective in rodent malaria models

scientific article published in January 2011

Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials

scientific article published on 17 June 2016

Two promoters within the human LMO4 gene contribute to its overexpression in breast cancer cells

scientific article published on September 2003

Two successful decades of Swiss collaborations to develop new anti-malarials

article

UV-triggered affinity capture identifies interactions between the Plasmodium falciparum multidrug resistance protein 1 (PfMDR1) and antimalarial agents in live parasitized cells

scientific article published on 10 June 2013

Weak base dispiro-1,2,4-trioxolanes: Potent antimalarial ozonides

article