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Items: 1 to 50 of 155

1.

Bioisosteric ferrocenyl aminoquinoline-benzimidazole hybrids: Antimicrobial evaluation and mechanistic insights.

Baartzes N, Stringer T, Seldon R, Warner DF, Taylor D, Wittlin S, Chibale K, Smith GS.

Eur J Med Chem. 2019 Jun 26;180:121-133. doi: 10.1016/j.ejmech.2019.06.069. [Epub ahead of print]

PMID:
31301563
2.

Author Correction: Arylmethylamino steroids as antiparasitic agents.

Krieg R, Jortzik E, Goetz AA, Blandin S, Wittlin S, Elhabiri M, Rahbari M, Nuryyeva S, Voigt K, Dahse HM, Brakhage A, Beckmann S, Quack T, Grevelding CG, Pinkerton AB, Schönecker B, Burrows J, Davioud-Charvet E, Rahlfs S, Becker K.

Nat Commun. 2019 Jul 8;10(1):2997. doi: 10.1038/s41467-019-11018-x.

3.

Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles.

Attram HD, Wittlin S, Chibale K.

Medchemcomm. 2019 Feb 19;10(3):450-455. doi: 10.1039/c8md00608c. eCollection 2019 Mar 1.

PMID:
31015908
4.

Cell Penetration, Herbicidal Activity, and in-vivo-Toxicity of Oligo-Arginine Derivatives and of Novel Guanidinium-Rich Compounds Derived from the Biopolymer Cyanophycin.

Grogg M, Hilvert D, Ebert MO, Beck AK, Seebach D, Kurth F, Dittrich PS, Sparr C, Wittlin S, Rottmann M, Mäser P.

Helv Chim Acta. 2018 Oct;101(10). pii: e1800112. doi: 10.1002/hlca.201800112.

5.

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

Hooft van Huijsduijnen R, Wells T, Tanner M, Wittlin S.

Malar J. 2019 Mar 22;18(1):94. doi: 10.1186/s12936-019-2728-8.

6.

Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis.

Baragaña B, Forte B, Choi R, Nakazawa Hewitt S, Bueren-Calabuig JA, Pisco JP, Peet C, Dranow DM, Robinson DA, Jansen C, Norcross NR, Vinayak S, Anderson M, Brooks CF, Cooper CA, Damerow S, Delves M, Dowers K, Duffy J, Edwards TE, Hallyburton I, Horst BG, Hulverson MA, Ferguson L, Jiménez-Díaz MB, Jumani RS, Lorimer DD, Love MS, Maher S, Matthews H, McNamara CW, Miller P, O'Neill S, Ojo KK, Osuna-Cabello M, Pinto E, Post J, Riley J, Rottmann M, Sanz LM, Scullion P, Sharma A, Shepherd SM, Shishikura Y, Simeons FRC, Stebbins EE, Stojanovski L, Straschil U, Tamaki FK, Tamjar J, Torrie LS, Vantaux A, Witkowski B, Wittlin S, Yogavel M, Zuccotto F, Angulo-Barturen I, Sinden R, Baum J, Gamo FJ, Mäser P, Kyle DE, Winzeler EA, Myler PJ, Wyatt PG, Floyd D, Matthews D, Sharma A, Striepen B, Huston CD, Gray DW, Fairlamb AH, Pisliakov AV, Walpole C, Read KD, Van Voorhis WC, Gilbert IH.

Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):7015-7020. doi: 10.1073/pnas.1814685116. Epub 2019 Mar 20.

7.

Antimalarial Pyrido[1,2- a]benzimidazole Derivatives with Mannich Base Side Chains: Synthesis, Pharmacological Evaluation, and Reactive Metabolite Trapping Studies.

Okombo J, Brunschwig C, Singh K, Dziwornu GA, Barnard L, Njoroge M, Wittlin S, Chibale K.

ACS Infect Dis. 2019 Mar 8;5(3):372-384. doi: 10.1021/acsinfecdis.8b00279. Epub 2019 Jan 17.

PMID:
30608648
8.

Structure-Activity Relationship Studies and Plasmodium Life Cycle Profiling Identifies Pan-Active N-Aryl-3-trifluoromethyl Pyrido[1,2- a]benzimidazoles Which Are Efficacious in an in Vivo Mouse Model of Malaria.

Mayoka G, Njoroge M, Okombo J, Gibhard L, Sanches-Vaz M, Fontinha D, Birkholtz LM, Reader J, van der Watt M, Coetzer TL, Lauterbach S, Churchyard A, Bezuidenhout B, Egan TJ, Yeates C, Wittlin S, Prudêncio M, Chibale K.

J Med Chem. 2019 Jan 24;62(2):1022-1035. doi: 10.1021/acs.jmedchem.8b01769. Epub 2018 Dec 24.

PMID:
30562027
9.

Evaluation of 4-Amino 2-Anilinoquinazolines against Plasmodium and Other Apicomplexan Parasites In Vitro and in a P. falciparum Humanized NOD-scid IL2Rγnull Mouse Model of Malaria.

Gilson PR, Nguyen W, Poole WA, Teixeira JE, Thompson JK, Guo K, Stewart RJ, Ashton TD, White KL, Sanz LM, Gamo FJ, Charman SA, Wittlin S, Duffy J, Tonkin CJ, Tham WH, Crabb BS, Cooke BM, Huston CD, Cowman AF, Sleebs BE.

Antimicrob Agents Chemother. 2019 Feb 26;63(3). pii: e01804-18. doi: 10.1128/AAC.01804-18. Print 2019 Mar.

10.

Multistage Antiplasmodium Activity of Astemizole Analogues and Inhibition of Hemozoin Formation as a Contributor to Their Mode of Action.

Kumar M, Okombo J, Mambwe D, Taylor D, Lawrence N, Reader J, van der Watt M, Fontinha D, Sanches-Vaz M, Bezuidenhout BC, Lauterbach SB, Liebenberg D, Birkholtz LM, Coetzer TL, Prudêncio M, Egan TJ, Wittlin S, Chibale K.

ACS Infect Dis. 2019 Feb 8;5(2):303-315. doi: 10.1021/acsinfecdis.8b00272. Epub 2019 Jan 7.

PMID:
30525439
11.

Antiplasmodial imidazopyridazines: structure-activity relationship studies lead to the identification of analogues with improved solubility and hERG profiles.

Cheuka PM, Lawrence N, Taylor D, Wittlin S, Chibale K.

Medchemcomm. 2018 Sep 6;9(10):1733-1745. doi: 10.1039/c8md00382c. eCollection 2018 Oct 1.

12.

Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria".

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Gonzàlez Cabrera D, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01941-18. doi: 10.1128/AAC.01941-18. Print 2018 Nov. No abstract available.

13.

Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains.

Le Manach C, Paquet T, Wicht K, Nchinda AT, Brunschwig C, Njoroge M, Gibhard L, Taylor D, Lawrence N, Wittlin S, Eyermann CJ, Basarab GS, Duffy J, Fish PV, Street LJ, Chibale K.

J Med Chem. 2018 Oct 25;61(20):9371-9385. doi: 10.1021/acs.jmedchem.8b01333. Epub 2018 Oct 16.

PMID:
30256636
14.

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

Gibhard L, Njoroge M, Paquet T, Brunschwig C, Taylor D, Lawrence N, Abay E, Wittlin S, Wiesner L, Street LJ, Chibale K, Basarab GS.

Antimicrob Agents Chemother. 2018 Nov 26;62(12). pii: e00261-18. doi: 10.1128/AAC.00261-18. Print 2018 Dec.

15.

3D-QSAR Modeling and Synthesis of New Fusidic Acid Derivatives as Antiplasmodial Agents.

Kaur G, Pavadai E, Wittlin S, Chibale K.

J Chem Inf Model. 2018 Aug 27;58(8):1553-1560. doi: 10.1021/acs.jcim.8b00105. Epub 2018 Aug 7.

PMID:
30040885
16.

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria.

Brunschwig C, Lawrence N, Taylor D, Abay E, Njoroge M, Basarab GS, Le Manach C, Paquet T, Cabrera DG, Nchinda AT, de Kock C, Wiesner L, Denti P, Waterson D, Blasco B, Leroy D, Witty MJ, Donini C, Duffy J, Wittlin S, White KL, Charman SA, Jiménez-Díaz MB, Angulo-Barturen I, Herreros E, Gamo FJ, Rochford R, Mancama D, Coetzer TL, van der Watt ME, Reader J, Birkholtz LM, Marsh KC, Solapure SM, Burke JE, McPhail JA, Vanaerschot M, Fidock DA, Fish PV, Siegl P, Smith DA, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Silue KD, Street LJ, Chibale K.

Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: e00012-18. doi: 10.1128/AAC.00012-18. Print 2018 Sep. Erratum in: Antimicrob Agents Chemother. 2018 Oct 24;62(11):.

17.

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

Nchinda AT, Le Manach C, Paquet T, Gonzàlez Cabrera D, Wicht KJ, Brunschwig C, Njoroge M, Abay E, Taylor D, Lawrence N, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Lafuente-Monasterio MJ, Duffy J, Burrows J, Street LJ, Chibale K.

J Med Chem. 2018 May 10;61(9):4213-4227. doi: 10.1021/acs.jmedchem.8b00382. Epub 2018 Apr 27.

PMID:
29665687
18.

Correction to: Chronomedicine and type 2 diabetes: shining some light on melatonin.

Forrestel AC, Miedlich SU, Yurcheshen M, Wittlin SD, Sellix MT.

Diabetologia. 2018 May;61(5):1237. doi: 10.1007/s00125-018-4577-3.

PMID:
29470590
19.

Refining risk in diabetes and CAD with SPECT MPI: New insights and future challenges.

Naqvi SY, Wittlin SD, Schwartz RG.

J Nucl Cardiol. 2019 Aug;26(4):1103-1106. doi: 10.1007/s12350-017-1177-4. Epub 2018 Feb 5. No abstract available.

PMID:
29404896
20.

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

Abla N, Bashyam S, Charman SA, Greco B, Hewitt P, Jiménez-Díaz MB, Katneni K, Kubas H, Picard D, Sambandan Y, Sanz L, Smith D, Wang T, Willis P, Wittlin S, Spangenberg T.

ACS Med Chem Lett. 2017 Nov 28;8(12):1304-1308. doi: 10.1021/acsmedchemlett.7b00391. eCollection 2017 Dec 14.

21.

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

Leven M, Knaab TC, Held J, Duffy S, Meister S, Fischli C, Meitzner D, Lehmann U, Lungerich B, Kuna K, Stahlke P, Delves MJ, Buchholz M, Winzeler EA, Avery VM, Mordmüller B, Wittlin S, Kurz T.

J Med Chem. 2017 Jul 27;60(14):6036-6044. doi: 10.1021/acs.jmedchem.7b00140. Epub 2017 Jul 17.

PMID:
28653845
22.

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase.

Paquet T, Le Manach C, Cabrera DG, Younis Y, Henrich PP, Abraham TS, Lee MCS, Basak R, Ghidelli-Disse S, Lafuente-Monasterio MJ, Bantscheff M, Ruecker A, Blagborough AM, Zakutansky SE, Zeeman AM, White KL, Shackleford DM, Mannila J, Morizzi J, Scheurer C, Angulo-Barturen I, Martínez MS, Ferrer S, Sanz LM, Gamo FJ, Reader J, Botha M, Dechering KJ, Sauerwein RW, Tungtaeng A, Vanachayangkul P, Lim CS, Burrows J, Witty MJ, Marsh KC, Bodenreider C, Rochford R, Solapure SM, Jiménez-Díaz MB, Wittlin S, Charman SA, Donini C, Campo B, Birkholtz LM, Hanson KK, Drewes G, Kocken CHM, Delves MJ, Leroy D, Fidock DA, Waterson D, Street LJ, Chibale K.

Sci Transl Med. 2017 Apr 26;9(387). pii: eaad9735. doi: 10.1126/scitranslmed.aad9735.

23.

Identification of steroid-like natural products as antiplasmodial agents by 2D and 3D similarity-based virtual screening.

Pavadai E, Kaur G, Wittlin S, Chibale K.

Medchemcomm. 2017 Mar 22;8(6):1152-1157. doi: 10.1039/c7md00063d. eCollection 2017 Jun 1.

24.

Arylmethylamino steroids as antiparasitic agents.

Krieg R, Jortzik E, Goetz AA, Blandin S, Wittlin S, Elhabiri M, Rahbari M, Nuryyeva S, Voigt K, Dahse HM, Brakhage A, Beckmann S, Quack T, Grevelding CG, Pinkerton AB, Schönecker B, Burrows J, Davioud-Charvet E, Rahlfs S, Becker K.

Nat Commun. 2017 Feb 17;8:14478. doi: 10.1038/ncomms14478. Erratum in: Nat Commun. 2019 Jul 8;10(1):2997.

25.

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

Baumgärtner F, Jourdan J, Scheurer C, Blasco B, Campo B, Mäser P, Wittlin S.

Malar J. 2017 Jan 25;16(1):45. doi: 10.1186/s12936-017-1696-0.

26.

Antimalarial Pyrido[1,2-a]benzimidazoles: Lead Optimization, Parasite Life Cycle Stage Profile, Mechanistic Evaluation, Killing Kinetics, and in Vivo Oral Efficacy in a Mouse Model.

Singh K, Okombo J, Brunschwig C, Ndubi F, Barnard L, Wilkinson C, Njogu PM, Njoroge M, Laing L, Machado M, Prudêncio M, Reader J, Botha M, Nondaba S, Birkholtz LM, Lauterbach S, Churchyard A, Coetzer TL, Burrows JN, Yeates C, Denti P, Wiesner L, Egan TJ, Wittlin S, Chibale K.

J Med Chem. 2017 Feb 23;60(4):1432-1448. doi: 10.1021/acs.jmedchem.6b01641. Epub 2017 Feb 7.

PMID:
28094524
27.

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

Dong Y, Wang X, Kamaraj S, Bulbule VJ, Chiu FC, Chollet J, Dhanasekaran M, Hein CD, Papastogiannidis P, Morizzi J, Shackleford DM, Barker H, Ryan E, Scheurer C, Tang Y, Zhao Q, Zhou L, White KL, Urwyler H, Charman WN, Matile H, Wittlin S, Charman SA, Vennerstrom JL.

J Med Chem. 2017 Apr 13;60(7):2654-2668. doi: 10.1021/acs.jmedchem.6b01586. Epub 2017 Jan 18.

PMID:
28052200
28.

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

Espinoza-Moraga M, Singh K, Njoroge M, Kaur G, Okombo J, De Kock C, Smith PJ, Wittlin S, Chibale K.

Bioorg Med Chem Lett. 2017 Feb 1;27(3):658-661. doi: 10.1016/j.bmcl.2016.11.077. Epub 2016 Nov 25.

PMID:
28012840
29.

Probing the Peroxycarbenium [3+2] Cycloaddition Reactions with 1,2-Disubstituted Ethylenes: Results and Insights.

Xu ZJ, Wittlin S, Wu Y.

Chemistry. 2017 Feb 10;23(9):2031-2034. doi: 10.1002/chem.201605871. Epub 2017 Jan 20.

PMID:
28012253
30.

Chronomedicine and type 2 diabetes: shining some light on melatonin.

Forrestel AC, Miedlich SU, Yurcheshen M, Wittlin SD, Sellix MT.

Diabetologia. 2017 May;60(5):808-822. doi: 10.1007/s00125-016-4175-1. Epub 2016 Dec 16. Review. Erratum in: Diabetologia. 2018 Feb 22;:.

PMID:
27981356
31.

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

Williamson AE, Ylioja PM, Robertson MN, Antonova-Koch Y, Avery V, Baell JB, Batchu H, Batra S, Burrows JN, Bhattacharyya S, Calderon F, Charman SA, Clark J, Crespo B, Dean M, Debbert SL, Delves M, Dennis AS, Deroose F, Duffy S, Fletcher S, Giaever G, Hallyburton I, Gamo FJ, Gebbia M, Guy RK, Hungerford Z, Kirk K, Lafuente-Monasterio MJ, Lee A, Meister S, Nislow C, Overington JP, Papadatos G, Patiny L, Pham J, Ralph SA, Ruecker A, Ryan E, Southan C, Srivastava K, Swain C, Tarnowski MJ, Thomson P, Turner P, Wallace IM, Wells TN, White K, White L, Willis P, Winzeler EA, Wittlin S, Todd MH.

ACS Cent Sci. 2016 Oct 26;2(10):687-701. Epub 2016 Sep 14.

32.

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.

Le Manach C, Nchinda AT, Paquet T, Gonzàlez Cabrera D, Younis Y, Han Z, Bashyam S, Zabiulla M, Taylor D, Lawrence N, White KL, Charman SA, Waterson D, Witty MJ, Wittlin S, Botha ME, Nondaba SH, Reader J, Birkholtz LM, Jiménez-Díaz MB, Martínez MS, Ferrer S, Angulo-Barturen I, Meister S, Antonova-Koch Y, Winzeler EA, Street LJ, Chibale K.

J Med Chem. 2016 Nov 10;59(21):9890-9905. Epub 2016 Oct 26.

PMID:
27748596
33.

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

Le Bihan A, de Kanter R, Angulo-Barturen I, Binkert C, Boss C, Brun R, Brunner R, Buchmann S, Burrows J, Dechering KJ, Delves M, Ewerling S, Ferrer S, Fischli C, Gamo-Benito FJ, Gnädig NF, Heidmann B, Jiménez-Díaz MB, Leroy D, Martínez MS, Meyer S, Moehrle JJ, Ng CL, Noviyanti R, Ruecker A, Sanz LM, Sauerwein RW, Scheurer C, Schleiferboeck S, Sinden R, Snyder C, Straimer J, Wirjanata G, Marfurt J, Price RN, Weller T, Fischli W, Fidock DA, Clozel M, Wittlin S.

PLoS Med. 2016 Oct 4;13(10):e1002138. doi: 10.1371/journal.pmed.1002138. eCollection 2016 Oct.

34.

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

Baragaña B, Norcross NR, Wilson C, Porzelle A, Hallyburton I, Grimaldi R, Osuna-Cabello M, Norval S, Riley J, Stojanovski L, Simeons FR, Wyatt PG, Delves MJ, Meister S, Duffy S, Avery VM, Winzeler EA, Sinden RE, Wittlin S, Frearson JA, Gray DW, Fairlamb AH, Waterson D, Campbell SF, Willis P, Read KD, Gilbert IH.

J Med Chem. 2016 Nov 10;59(21):9672-9685. Epub 2016 Sep 10.

35.

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

Boss C, Aissaoui H, Amaral N, Bauer A, Bazire S, Binkert C, Brun R, Bürki C, Ciana CL, Corminboeuf O, Delahaye S, Dollinger C, Fischli C, Fischli W, Flock A, Frantz MC, Girault M, Grisostomi C, Friedli A, Heidmann B, Hinder C, Jacob G, Le Bihan A, Malrieu S, Mamzed S, Merot A, Meyer S, Peixoto S, Petit N, Siegrist R, Trollux J, Weller T, Wittlin S.

ChemMedChem. 2016 Sep 20;11(18):1995-2014. doi: 10.1002/cmdc.201600298. Epub 2016 Jul 29.

PMID:
27471138
36.

Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials.

Norcross NR, Baragaña B, Wilson C, Hallyburton I, Osuna-Cabello M, Norval S, Riley J, Stojanovski L, Simeons FR, Porzelle A, Grimaldi R, Wittlin S, Duffy S, Avery VM, Meister S, Sanz L, Jiménez-Díaz B, Angulo-Barturen I, Ferrer S, Martínez MS, Gamo FJ, Frearson JA, Gray DW, Fairlamb AH, Winzeler EA, Waterson D, Campbell SF, Willis P, Read KD, Gilbert IH.

J Med Chem. 2016 Jul 14;59(13):6101-20. doi: 10.1021/acs.jmedchem.6b00028. Epub 2016 Jun 17.

37.

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

Baragaña B, Hallyburton I, Lee MC, Norcross NR, Grimaldi R, Otto TD, Proto WR, Blagborough AM, Meister S, Wirjanata G, Ruecker A, Upton LM, Abraham TS, Almeida MJ, Pradhan A, Porzelle A, Martínez MS, Bolscher JM, Woodland A, Luksch T, Norval S, Zuccotto F, Thomas J, Simeons F, Stojanovski L, Osuna-Cabello M, Brock PM, Churcher TS, Sala KA, Zakutansky SE, Jiménez-Díaz MB, Sanz LM, Riley J, Basak R, Campbell M, Avery VM, Sauerwein RW, Dechering KJ, Noviyanti R, Campo B, Frearson JA, Angulo-Barturen I, Ferrer-Bazaga S, Gamo FJ, Wyatt PG, Leroy D, Siegl P, Delves MJ, Kyle DE, Wittlin S, Marfurt J, Price RN, Sinden RE, Winzeler EA, Charman SA, Bebrevska L, Gray DW, Campbell S, Fairlamb AH, Willis PA, Rayner JC, Fidock DA, Read KD, Gilbert IH.

Nature. 2016 Sep 1;537(7618):122. doi: 10.1038/nature18280. Epub 2016 May 25. No abstract available.

38.

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.

Ng CL, Siciliano G, Lee MC, de Almeida MJ, Corey VC, Bopp SE, Bertuccini L, Wittlin S, Kasdin RG, Le Bihan A, Clozel M, Winzeler EA, Alano P, Fidock DA.

Mol Microbiol. 2016 Aug;101(3):381-93. doi: 10.1111/mmi.13397. Epub 2016 May 7.

39.

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

Pavadai E, El Mazouni F, Wittlin S, de Kock C, Phillips MA, Chibale K.

J Chem Inf Model. 2016 Mar 28;56(3):548-62. doi: 10.1021/acs.jcim.5b00680. Epub 2016 Mar 8.

40.

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

Jourdan J, Matile H, Reift E, Biehlmaier O, Dong Y, Wang X, Mäser P, Vennerstrom JL, Wittlin S.

ACS Infect Dis. 2016 Jan 8;2(1):54-61. Epub 2015 Sep 28.

41.

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.

Le Manach C, Paquet T, Brunschwig C, Njoroge M, Han Z, Gonzàlez Cabrera D, Bashyam S, Dhinakaran R, Taylor D, Reader J, Botha M, Churchyard A, Lauterbach S, Coetzer TL, Birkholtz LM, Meister S, Winzeler EA, Waterson D, Witty MJ, Wittlin S, Jiménez-Díaz MB, Santos Martínez M, Ferrer S, Angulo-Barturen I, Street LJ, Chibale K.

J Med Chem. 2015 Nov 12;58(21):8713-22. doi: 10.1021/acs.jmedchem.5b01605. Epub 2015 Nov 2.

PMID:
26502160
42.

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

Jortzik E, Zocher K, Isernhagen A, Mailu BM, Rahlfs S, Viola G, Wittlin S, Hunt NH, Ihmels H, Becker K.

Antimicrob Agents Chemother. 2015 Oct 12;60(1):115-25. doi: 10.1128/AAC.01066-15. Print 2016 Jan.

43.

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

Gonzàlez Cabrera D, Douelle F, Le Manach C, Han Z, Paquet T, Taylor D, Njoroge M, Lawrence N, Wiesner L, Waterson D, Witty MJ, Wittlin S, Street LJ, Chibale K.

J Med Chem. 2015 Sep 24;58(18):7572-9. doi: 10.1021/acs.jmedchem.5b01156. Epub 2015 Sep 8.

PMID:
26322748
44.

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

Ongarora DS, Strydom N, Wicht K, Njoroge M, Wiesner L, Egan TJ, Wittlin S, Jurva U, Masimirembwa CM, Chibale K.

Bioorg Med Chem. 2015 Sep 1;23(17):5419-32. doi: 10.1016/j.bmc.2015.07.051. Epub 2015 Jul 30.

PMID:
26264839
45.

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

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