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Items: 1 to 50 of 114

1.

Pharmacokinetics and Pharmacodynamics of the Nitroimidazole DNDI-0690 in Mouse Models of Cutaneous Leishmaniasis.

Wijnant GJ, Croft SL, de la Flor R, Alavijeh M, Yardley V, Braillard S, Mowbray C, Van Bocxlaer K.

Antimicrob Agents Chemother. 2019 Aug 23;63(9). pii: e00829-19. doi: 10.1128/AAC.00829-19. Print 2019 Sep.

2.

Novel benzoxaborole, nitroimidazole and aminopyrazoles with activity against experimental cutaneous leishmaniasis.

Van Bocxlaer K, Caridha D, Black C, Vesely B, Leed S, Sciotti RJ, Wijnant GJ, Yardley V, Braillard S, Mowbray CE, Ioset JR, Croft SL.

Int J Parasitol Drugs Drug Resist. 2019 Feb 26. pii: S2211-3207(18)30185-4. doi: 10.1016/j.ijpddr.2019.02.002. [Epub ahead of print]

3.

Synthesis, Profiling, and in Vivo Evaluation of Cyclopeptides Containing N-Methyl Amino Acids as Antiplasmodial Agents.

Fagundez C, Sellanes D, Peña S, Scarone L, Aguiar ACC, de Souza JO, Guido RVC, Stewart L, Yardley V, Ottilie S, Winzeler EA, Gamo FJ, Sanz LM, Serra GL.

ACS Med Chem Lett. 2018 Dec 26;10(1):137-141. doi: 10.1021/acsmedchemlett.8b00543. eCollection 2019 Jan 10.

PMID:
30655961
4.

Local Skin Inflammation in Cutaneous Leishmaniasis as a Source of Variable Pharmacokinetics and Therapeutic Efficacy of Liposomal Amphotericin B.

Wijnant GJ, Van Bocxlaer K, Fortes Francisco A, Yardley V, Harris A, Alavijeh M, Murdan S, Croft SL.

Antimicrob Agents Chemother. 2018 Sep 24;62(10). pii: e00631-18. doi: 10.1128/AAC.00631-18. Print 2018 Oct.

5.

Investigating Permeation Behavior of Flufenamic Acid Cocrystals Using a Dissolution and Permeation System.

Guo M, Wang K, Qiao N, Yardley V, Li M.

Mol Pharm. 2018 Sep 4;15(9):4257-4272. doi: 10.1021/acs.molpharmaceut.8b00670. Epub 2018 Aug 20.

6.

Comparative efficacy, toxicity and biodistribution of the liposomal amphotericin B formulations Fungisome® and AmBisome® in murine cutaneous leishmaniasis.

Wijnant GJ, Van Bocxlaer K, Yardley V, Harris A, Alavijeh M, Silva-Pedrosa R, Antunes S, Mauricio I, Murdan S, Croft SL.

Int J Parasitol Drugs Drug Resist. 2018 Aug;8(2):223-228. doi: 10.1016/j.ijpddr.2018.04.001. Epub 2018 Apr 12.

7.

Topical Treatment for Cutaneous Leishmaniasis: Dermato-Pharmacokinetic Lead Optimization of Benzoxaboroles.

Van Bocxlaer K, Gaukel E, Hauser D, Park SH, Schock S, Yardley V, Randolph R, Plattner JJ, Merchant T, Croft SL, Jacobs RT, Wring SA.

Antimicrob Agents Chemother. 2018 Apr 26;62(5). pii: e02419-17. doi: 10.1128/AAC.02419-17. Print 2018 May.

8.

Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis.

Thompson AM, O'Connor PD, Marshall AJ, Blaser A, Yardley V, Maes L, Gupta S, Launay D, Braillard S, Chatelain E, Wan B, Franzblau SG, Ma Z, Cooper CB, Denny WA.

J Med Chem. 2018 Mar 22;61(6):2329-2352. doi: 10.1021/acs.jmedchem.7b01581. Epub 2018 Mar 6.

9.

Relation between Skin Pharmacokinetics and Efficacy in AmBisome Treatment of Murine Cutaneous Leishmaniasis.

Wijnant GJ, Van Bocxlaer K, Yardley V, Harris A, Murdan S, Croft SL.

Antimicrob Agents Chemother. 2018 Feb 23;62(3). pii: e02009-17. doi: 10.1128/AAC.02009-17. Print 2018 Mar.

10.

In Vivo and In Vitro Activities and ADME-Tox Profile of a Quinolizidine-Modified 4-Aminoquinoline: A Potent Anti-P. falciparum and Anti-P. vivax Blood-Stage Antimalarial.

Basilico N, Parapini S, Sparatore A, Romeo S, Misiano P, Vivas L, Yardley V, Croft SL, Habluetzel A, Lucantoni L, Renia L, Russell B, Suwanarusk R, Nosten F, Dondio G, Bigogno C, Jabes D, Taramelli D.

Molecules. 2017 Dec 1;22(12). pii: E2102. doi: 10.3390/molecules22122102.

11.

Efficacy of Paromomycin-Chloroquine Combination Therapy in Experimental Cutaneous Leishmaniasis.

Wijnant GJ, Van Bocxlaer K, Yardley V, Murdan S, Croft SL.

Antimicrob Agents Chemother. 2017 Jul 25;61(8). pii: e00358-17. doi: 10.1128/AAC.00358-17. Print 2017 Aug.

12.

7-Substituted 2-Nitro-5,6-dihydroimidazo[2,1-b][1,3]oxazines: Novel Antitubercular Agents Lead to a New Preclinical Candidate for Visceral Leishmaniasis.

Thompson AM, O'Connor PD, Marshall AJ, Yardley V, Maes L, Gupta S, Launay D, Braillard S, Chatelain E, Franzblau SG, Wan B, Wang Y, Ma Z, Cooper CB, Denny WA.

J Med Chem. 2017 May 25;60(10):4212-4233. doi: 10.1021/acs.jmedchem.7b00034. Epub 2017 May 11.

13.

Synthesis and antitrypanosomal activities of novel pyridylchalcones.

Bhambra AS, Ruparelia KC, Tan HL, Tasdemir D, Burrell-Saward H, Yardley V, Beresford KJM, Arroo RRJ.

Eur J Med Chem. 2017 Mar 10;128:213-218. doi: 10.1016/j.ejmech.2017.01.027. Epub 2017 Jan 23.

14.

Antiprotozoal glutathione derivatives with flagellar membrane binding activity against T. brucei rhodesiense.

Daunes S, Yardley V, Croft SL, D'Silva C.

Bioorg Med Chem. 2017 Feb 15;25(4):1329-1340. doi: 10.1016/j.bmc.2016.12.016. Epub 2016 Dec 18.

15.

Visceral Leishmaniasis Patients Display Altered Composition and Maturity of Neutrophils as well as Impaired Neutrophil Effector Functions.

Yizengaw E, Getahun M, Tajebe F, Cruz Cervera E, Adem E, Mesfin G, Hailu A, Van der Auwera G, Yardley V, Lemma M, Skhedy Z, Diro E, Yeshanew A, Melkamu R, Mengesha B, Modolell M, Munder M, Müller I, Takele Y, Kropf P.

Front Immunol. 2016 Nov 29;7:517. eCollection 2016.

16.

Cutaneous Leishmaniasis in Khyber Pakhtunkhwa Province of Pakistan: Clinical Diversity and Species-Level Diagnosis.

Khan NH, Bari AU, Hashim R, Khan I, Muneer A, Shah A, Wahid S, Yardley V, O'Neil B, Sutherland CJ.

Am J Trop Med Hyg. 2016 Nov 2;95(5):1106-1114. doi: 10.4269/ajtmh.16-0343. Epub 2016 Sep 6.

17.

Topical formulations of miltefosine for cutaneous leishmaniasis in a BALB/c mouse model.

Van Bocxlaer K, Yardley V, Murdan S, Croft SL.

J Pharm Pharmacol. 2016 Jul;68(7):862-72. doi: 10.1111/jphp.12548. Epub 2016 May 27.

18.

A Replicative In Vitro Assay for Drug Discovery against Leishmania donovani.

Tegazzini D, Díaz R, Aguilar F, Peña I, Presa JL, Yardley V, Martin JJ, Coteron JM, Croft SL, Cantizani J.

Antimicrob Agents Chemother. 2016 May 23;60(6):3524-32. doi: 10.1128/AAC.01781-15. Print 2016 Jun.

19.

Drug permeation and barrier damage in Leishmania-infected mouse skin.

Van Bocxlaer K, Yardley V, Murdan S, Croft SL.

J Antimicrob Chemother. 2016 Jun;71(6):1578-85. doi: 10.1093/jac/dkw012. Epub 2016 Feb 21.

PMID:
26903275
20.

Repositioning Antitubercular 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]oxazoles for Neglected Tropical Diseases: Structure-Activity Studies on a Preclinical Candidate for Visceral Leishmaniasis.

Thompson AM, O'Connor PD, Blaser A, Yardley V, Maes L, Gupta S, Launay D, Martin D, Franzblau SG, Wan B, Wang Y, Ma Z, Denny WA.

J Med Chem. 2016 Mar 24;59(6):2530-50. doi: 10.1021/acs.jmedchem.5b01699. Epub 2016 Mar 8.

21.

Design, synthesis and antitrypanosomal activities of 2,6-disubstituted-4,5,7-trifluorobenzothiophenes.

Bhambra AS, Edgar M, Elsegood MRJ, Li Y, Weaver GW, Arroo RRJ, Yardley V, Burrell-Saward H, Krystof V.

Eur J Med Chem. 2016 Jan 27;108:347-353. doi: 10.1016/j.ejmech.2015.11.043. Epub 2015 Nov 30.

PMID:
26698538
22.

The Oral Antimalarial Drug Tafenoquine Shows Activity against Trypanosoma brucei.

Carvalho L, Martínez-García M, Pérez-Victoria I, Manzano JI, Yardley V, Gamarro F, Pérez-Victoria JM.

Antimicrob Agents Chemother. 2015 Oct;59(10):6151-60. doi: 10.1128/AAC.00879-15. Epub 2015 Jul 20.

23.

Protein energy malnutrition increases arginase activity in monocytes and macrophages.

Corware K, Yardley V, Mack C, Schuster S, Al-Hassi H, Herath S, Bergin P, Modolell M, Munder M, Müller I, Kropf P.

Nutr Metab (Lond). 2014 Oct 24;11(1):51. doi: 10.1186/1743-7075-11-51. eCollection 2014.

24.

Nitroimidazo-oxazole compound DNDI-VL-2098: an orally effective preclinical drug candidate for the treatment of visceral leishmaniasis.

Gupta S, Yardley V, Vishwakarma P, Shivahare R, Sharma B, Launay D, Martin D, Puri SK.

J Antimicrob Chemother. 2015 Feb;70(2):518-27. doi: 10.1093/jac/dku422. Epub 2014 Nov 10.

PMID:
25389223
25.

Activity of anti-cancer protein kinase inhibitors against Leishmania spp.

Sanderson L, Yardley V, Croft SL.

J Antimicrob Chemother. 2014 Jul;69(7):1888-91. doi: 10.1093/jac/dku069. Epub 2014 Mar 25.

PMID:
24668412
26.

Antileishmanial activity, uptake, and biodistribution of an amphotericin B and poly(α-Glutamic Acid) complex.

Mohamed-Ahmed AH, Seifert K, Yardley V, Burrell-Saward H, Brocchini S, Croft SL.

Antimicrob Agents Chemother. 2013 Oct;57(10):4608-14. doi: 10.1128/AAC.02343-12. Epub 2013 Jun 24.

27.

Inhibition of Leishmania infantum trypanothione reductase by azole-based compounds: a comparative analysis with its physiological substrate by X-ray crystallography.

Baiocco P, Poce G, Alfonso S, Cocozza M, Porretta GC, Colotti G, Biava M, Moraca F, Botta M, Yardley V, Fiorillo A, Lantella A, Malatesta F, Ilari A.

ChemMedChem. 2013 Jul;8(7):1175-83. doi: 10.1002/cmdc.201300176. Epub 2013 Jun 3.

PMID:
23733388
28.

Efficacy and tolerability of oleylphosphocholine (OlPC) in a laboratory model of visceral leishmaniasis.

Fortin A, Hendrickx S, Yardley V, Cos P, Jansen H, Maes L.

J Antimicrob Chemother. 2012 Nov;67(11):2707-12. doi: 10.1093/jac/dks273. Epub 2012 Jul 10.

PMID:
22782488
29.

Synthesis of a Microcystis aeruginosa predicted metabolite with antimalarial activity.

Peña S, Scarone L, Manta E, Stewart L, Yardley V, Croft S, Serra G.

Bioorg Med Chem Lett. 2012 Aug 1;22(15):4994-7. doi: 10.1016/j.bmcl.2012.06.028. Epub 2012 Jun 16.

PMID:
22765903
30.

Synthesis of aminoquinoline-based aminoalcohols and oxazolidinones and their antiplasmodial activity.

Kobarfard F, Yardley V, Little S, Daryaee F, Chibale K.

Chem Biol Drug Des. 2012 Mar;79(3):326-31. doi: 10.1111/j.1747-0285.2011.01278.x. Epub 2012 Jan 11.

PMID:
22129095
31.

Glutathione reductase-catalyzed cascade of redox reactions to bioactivate potent antimalarial 1,4-naphthoquinones--a new strategy to combat malarial parasites.

Müller T, Johann L, Jannack B, Brückner M, Lanfranchi DA, Bauer H, Sanchez C, Yardley V, Deregnaucourt C, Schrével J, Lanzer M, Schirmer RH, Davioud-Charvet E.

J Am Chem Soc. 2011 Aug 3;133(30):11557-71. doi: 10.1021/ja201729z. Epub 2011 Jul 12.

PMID:
21682307
32.

Antileishmanial and antitrypanosomal activities of the 8-aminoquinoline tafenoquine.

Yardley V, Gamarro F, Croft SL.

Antimicrob Agents Chemother. 2010 Dec;54(12):5356-8. doi: 10.1128/AAC.00985-10. Epub 2010 Sep 13. Erratum in: Antimicrob Agents Chemother. 2011 Jan;55(1):458.

33.

Antimalarial versus cytotoxic properties of dual drugs derived from 4-aminoquinolines and Mannich bases: interaction with DNA.

Wenzel NI, Chavain N, Wang Y, Friebolin W, Maes L, Pradines B, Lanzer M, Yardley V, Brun R, Herold-Mende C, Biot C, Tóth K, Davioud-Charvet E.

J Med Chem. 2010 Apr 22;53(8):3214-26. doi: 10.1021/jm9018383.

PMID:
20329733
34.

Therapeutic glucocorticoid-induced TNF receptor-mediated amplification of CD4+ T cell responses enhances antiparasitic immunity.

Haque A, Stanley AC, Amante FH, Rivera Fde L, Zhou Y, Kuns RD, Yardley V, Sakaguchi S, Hill GR, Engwerda CR.

J Immunol. 2010 Mar 1;184(5):2583-92. doi: 10.4049/jimmunol.0903080. Epub 2010 Feb 5.

35.

Synthesis and evaluation of phenylequine for antimalarial activity in vitro and in vivo.

Blackie MA, Yardley V, Chibale K.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1078-80. doi: 10.1016/j.bmcl.2009.12.030. Epub 2009 Dec 11.

PMID:
20034790
36.

Fluorinated rhodacyanine (SJL-01) possessing high efficacy for visceral leishmaniasis (VL).

Yang M, Arai C, Bakar Md A, Lu J, Ge JF, Pudhom K, Takasu K, Kasai K, Kaiser M, Brun R, Yardley V, Itoh I, Ihara M.

J Med Chem. 2010 Jan 14;53(1):368-73. doi: 10.1021/jm9013086.

PMID:
19894726
37.

A new series of amodiaquine analogues modified in the basic side chain with in vitro antileishmanial and antiplasmodial activity.

Guglielmo S, Bertinaria M, Rolando B, Crosetti M, Fruttero R, Yardley V, Croft SL, Gasco A.

Eur J Med Chem. 2009 Dec;44(12):5071-9. doi: 10.1016/j.ejmech.2009.09.012. Epub 2009 Sep 15.

38.

Combining 4-aminoquinoline- and clotrimazole-based pharmacophores toward innovative and potent hybrid antimalarials.

Gemma S, Campiani G, Butini S, Joshi BP, Kukreja G, Coccone SS, Bernetti M, Persico M, Nacci V, Fiorini I, Novellino E, Taramelli D, Basilico N, Parapini S, Yardley V, Croft S, Keller-Maerki S, Rottmann M, Brun R, Coletta M, Marini S, Guiso G, Caccia S, Fattorusso C.

J Med Chem. 2009 Jan 22;52(2):502-13. doi: 10.1021/jm801352s.

PMID:
19113955
39.

Antiplasmodial, beta-haematin inhibition, antitrypanosomal and cytotoxic activity in vitro of novel 4-aminoquinoline 2-imidazolines.

Musonda CC, Yardley V, de Souza RC, Ncokazi K, Egan TJ, Chibale K.

Org Biomol Chem. 2008 Dec 7;6(23):4446-51. doi: 10.1039/b813007h. Epub 2008 Oct 24.

PMID:
19005606
40.

Reversed chloroquines based on the 3,4-dihydropyrimidin-2(1H)-one scaffold: synthesis and evaluation for antimalarial, beta-haematin inhibition, and cytotoxic activity.

October N, Watermeyer ND, Yardley V, Egan TJ, Ncokazi K, Chibale K.

ChemMedChem. 2008 Nov;3(11):1649-53. doi: 10.1002/cmdc.200800172. No abstract available.

PMID:
18846586
41.

Synthesis and antiprotozoal evaluation of new N4-(benzyl)spermidyl-linked bis(1,3,5-thiadiazinane-2-thiones).

Coro J, Little S, Yardley V, Suárez M, Rodríguez H, Martín N, Perez-Pineiro R.

Arch Pharm (Weinheim). 2008 Nov;341(11):708-13. doi: 10.1002/ardp.200800011.

PMID:
18720341
42.

Antiparasitic activities and toxicities of individual enantiomers of the 8-aminoquinoline 8-[(4-amino-1-methylbutyl)amino]-6-methoxy-4-methyl-5-[3,4-dichlorophenoxy]quinoline succinate.

Nanayakkara NP, Ager AL Jr, Bartlett MS, Yardley V, Croft SL, Khan IA, McChesney JD, Walker LA.

Antimicrob Agents Chemother. 2008 Jun;52(6):2130-7. doi: 10.1128/AAC.00645-07. Epub 2008 Mar 31.

43.

Clotrimazole scaffold as an innovative pharmacophore towards potent antimalarial agents: design, synthesis, and biological and structure-activity relationship studies.

Gemma S, Campiani G, Butini S, Kukreja G, Coccone SS, Joshi BP, Persico M, Nacci V, Fiorini I, Novellino E, Fattorusso E, Taglialatela-Scafati O, Savini L, Taramelli D, Basilico N, Parapini S, Morace G, Yardley V, Croft S, Coletta M, Marini S, Fattorusso C.

J Med Chem. 2008 Mar 13;51(5):1278-94. doi: 10.1021/jm701247k. Epub 2008 Feb 16.

PMID:
18278860
44.

Design, synthesis, and structure-activity relationship studies of 4-quinolinyl- and 9-acrydinylhydrazones as potent antimalarial agents.

Fattorusso C, Campiani G, Kukreja G, Persico M, Butini S, Romano MP, Altarelli M, Ros S, Brindisi M, Savini L, Novellino E, Nacci V, Fattorusso E, Parapini S, Basilico N, Taramelli D, Yardley V, Croft S, Borriello M, Gemma S.

J Med Chem. 2008 Mar 13;51(5):1333-43. doi: 10.1021/jm7012375. Epub 2008 Feb 16.

PMID:
18278859
45.

Antimalarial dual drugs based on potent inhibitors of glutathione reductase from Plasmodium falciparum.

Friebolin W, Jannack B, Wenzel N, Furrer J, Oeser T, Sanchez CP, Lanzer M, Yardley V, Becker K, Davioud-Charvet E.

J Med Chem. 2008 Mar 13;51(5):1260-77. doi: 10.1021/jm7009292. Epub 2008 Feb 9.

PMID:
18260613
46.

Gene expression profiling of Leishmania (Leishmania) donovani: overcoming technical variation and exploiting biological variation.

Decuypere S, Vanaerschot M, Rijal S, Yardley V, Maes L, de Doncker S, Chappuis F, Dujardin JC.

Parasitology. 2008 Feb;135(2):183-94. Epub 2007 Oct 12.

47.

Synthesis and in vitro protozoocidal evaluation of novel diazabicyclic tropolone derivatives.

Khrizman A, Slack RD, Remsing RC, Little S, Yardley V, Moyna G.

Arch Pharm (Weinheim). 2007 Nov;340(11):569-76.

PMID:
17924365
48.

Application of multicomponent reactions to antimalarial drug discovery. Part 3: discovery of aminoxazole 4-aminoquinolines with potent antiplasmodial activity in vitro.

Musonda CC, Little S, Yardley V, Chibale K.

Bioorg Med Chem Lett. 2007 Sep 1;17(17):4733-6. Epub 2007 Jun 27.

PMID:
17644333
49.

Anti-malarial activity of N6-modified purine analogues.

Too K, Brown DM, Bongard E, Yardley V, Vivas L, Loakes D.

Bioorg Med Chem. 2007 Aug 15;15(16):5551-62. Epub 2007 May 18.

PMID:
17548196
50.

Synthesis and in vitro protozoocidal activity of diazabicyclic benzotropolone derivatives.

Khrizman A, Moulthrop JS, Little S, Wharton H, Yardley V, Moyna G.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4183-6. Epub 2007 May 18.

PMID:
17532634

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