These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.
3. 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. Younis Y; Douelle F; González Cabrera D; Le Manach C; Nchinda AT; Paquet T; Street LJ; White KL; Zabiulla KM; Joseph JT; Bashyam S; Waterson D; Witty MJ; Wittlin S; Charman SA; Chibale K J Med Chem; 2013 Nov; 56(21):8860-71. PubMed ID: 24099149 [TBL] [Abstract][Full Text] [Related]
4. 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; 60(4):1432-1448. PubMed ID: 28094524 [TBL] [Abstract][Full Text] [Related]
5. Antimalarial pyrido[1,2-a]benzimidazoles. Ndakala AJ; Gessner RK; Gitari PW; October N; White KL; Hudson A; Fakorede F; Shackleford DM; Kaiser M; Yeates C; Charman SA; Chibale K J Med Chem; 2011 Jul; 54(13):4581-9. PubMed ID: 21644541 [TBL] [Abstract][Full Text] [Related]
7. 3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential. Younis Y; Douelle F; Feng TS; González Cabrera D; Le Manach C; Nchinda AT; Duffy S; White KL; Shackleford DM; Morizzi J; Mannila J; Katneni K; Bhamidipati R; Zabiulla KM; Joseph JT; Bashyam S; Waterson D; Witty MJ; Hardick D; Wittlin S; Avery V; Charman SA; Chibale K J Med Chem; 2012 Apr; 55(7):3479-87. PubMed ID: 22390538 [TBL] [Abstract][Full Text] [Related]
8. Structure-activity relationship studies of orally active antimalarial 3,5-substituted 2-aminopyridines. González Cabrera D; Douelle F; Younis Y; Feng TS; Le Manach C; Nchinda AT; Street LJ; Scheurer C; Kamber J; White KL; Montagnat OD; Ryan E; Katneni K; Zabiulla KM; Joseph JT; Bashyam S; Waterson D; Witty MJ; Charman SA; Wittlin S; Chibale K J Med Chem; 2012 Dec; 55(24):11022-30. PubMed ID: 23189922 [TBL] [Abstract][Full Text] [Related]
9. Histone methyltransferase inhibitors are orally bioavailable, fast-acting molecules with activity against different species causing malaria in humans. Malmquist NA; Sundriyal S; Caron J; Chen P; Witkowski B; Menard D; Suwanarusk R; Renia L; Nosten F; Jiménez-Díaz MB; Angulo-Barturen I; Santos Martínez M; Ferrer S; Sanz LM; Gamo FJ; Wittlin S; Duffy S; Avery VM; Ruecker A; Delves MJ; Sinden RE; Fuchter MJ; Scherf A Antimicrob Agents Chemother; 2015 Feb; 59(2):950-9. PubMed ID: 25421480 [TBL] [Abstract][Full Text] [Related]
10. 3,5-bis(benzylidene)-4-piperidones and related N-acyl analogs: a novel cluster of antimalarials targeting the liver stage of Plasmodium falciparum. Das U; Singh RS; Alcorn J; Hickman MR; Sciotti RJ; Leed SE; Lee PJ; Roncal N; Dimmock JR Bioorg Med Chem; 2013 Dec; 21(23):7250-6. PubMed ID: 24139941 [TBL] [Abstract][Full Text] [Related]
11. Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a SoftFocus kinase library: part 1. Le Manach C; Gonzàlez Cabrera D; Douelle F; Nchinda AT; Younis Y; Taylor D; Wiesner L; White KL; Ryan E; March C; Duffy S; Avery VM; Waterson D; Witty MJ; Wittlin S; Charman SA; Street LJ; Chibale K J Med Chem; 2014 Mar; 57(6):2789-98. PubMed ID: 24568587 [TBL] [Abstract][Full Text] [Related]
12. Antimalarial aminothiazoles and aminopyridines from phenotypic whole-cell screening of a SoftFocus(®) library. Paquet T; Gordon R; Waterson D; Witty MJ; Chibale K Future Med Chem; 2012 Dec; 4(18):2265-77. PubMed ID: 23234550 [TBL] [Abstract][Full Text] [Related]
13. Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate. Zhang YK; Plattner JJ; Easom EE; Jacobs RT; Guo D; Freund YR; Berry P; Ciaravino V; Erve JCL; Rosenthal PJ; Campo B; Gamo FJ; Sanz LM; Cao J J Med Chem; 2017 Jul; 60(13):5889-5908. PubMed ID: 28635296 [TBL] [Abstract][Full Text] [Related]
14. 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; 58(21):8713-22. PubMed ID: 26502160 [TBL] [Abstract][Full Text] [Related]
15. 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; 59(21):9890-9905. PubMed ID: 27748596 [TBL] [Abstract][Full Text] [Related]
16. Medicinal chemistry optimization of antiplasmodial imidazopyridazine hits from high throughput screening of a softfocus kinase library: part 2. Le Manach C; Paquet T; Gonzàlez Cabrera D; Younis Y; Taylor D; Wiesner L; Lawrence N; Schwager S; Waterson D; Witty MJ; Wittlin S; Street LJ; Chibale K J Med Chem; 2014 Nov; 57(21):8839-48. PubMed ID: 25313449 [TBL] [Abstract][Full Text] [Related]
17. Inhibitors of plasmodial serine hydroxymethyltransferase (SHMT): cocrystal structures of pyrazolopyrans with potent blood- and liver-stage activities. Witschel MC; Rottmann M; Schwab A; Leartsakulpanich U; Chitnumsub P; Seet M; Tonazzi S; Schwertz G; Stelzer F; Mietzner T; McNamara C; Thater F; Freymond C; Jaruwat A; Pinthong C; Riangrungroj P; Oufir M; Hamburger M; Mäser P; Sanz-Alonso LM; Charman S; Wittlin S; Yuthavong Y; Chaiyen P; Diederich F J Med Chem; 2015 Apr; 58(7):3117-30. PubMed ID: 25785478 [TBL] [Abstract][Full Text] [Related]
18. 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; 62(2):1022-1035. PubMed ID: 30562027 [TBL] [Abstract][Full Text] [Related]
19. Discovery and optimisation studies of antimalarial phenotypic hits. Mital A; Murugesan D; Kaiser M; Yeates C; Gilbert IH Eur J Med Chem; 2015 Oct; 103():530-8. PubMed ID: 26408453 [TBL] [Abstract][Full Text] [Related]
20. Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials. McConville M; Fernández J; Angulo-Barturen Í; Bahamontes-Rosa N; Ballell-Pages L; Castañeda P; de Cózar C; Crespo B; Guijarro L; Jiménez-Díaz MB; Martínez-Martínez MS; de Mercado J; Santos-Villarejo Á; Sanz LM; Frigerio M; Washbourn G; Ward SA; Nixon GL; Biagini GA; Berry NG; Blackman MJ; Calderón F; O'Neill PM J Med Chem; 2015 Aug; 58(16):6448-55. PubMed ID: 26222445 [TBL] [Abstract][Full Text] [Related] [Next] [New Search]