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Items: 1 to 20 of 23

1.

Structural Insights into the Development of Cycloguanil Derivatives as Trypanosoma brucei Pteridine-Reductase-1 Inhibitors.

Landi G, Linciano P, Borsari C, Bertolacini CP, Moraes CB, Cordeiro-da-Silva A, Gul S, Witt G, Kuzikov M, Costi MP, Pozzi C, Mangani S.

ACS Infect Dis. 2019 May 1. doi: 10.1021/acsinfecdis.8b00358. [Epub ahead of print]

PMID:
31012301
2.

Enhancement of Benzothiazoles as Pteridine Reductase-1 Inhibitors for the Treatment of Trypanosomatidic Infections.

Linciano P, Pozzi C, Iacono LD, di Pisa F, Landi G, Bonucci A, Gul S, Kuzikov M, Ellinger B, Witt G, Santarem N, Baptista C, Franco C, Moraes CB, Müller W, Wittig U, Luciani R, Sesenna A, Quotadamo A, Ferrari S, Pöhner I, Cordeiro-da-Silva A, Mangani S, Costantino L, Costi MP.

J Med Chem. 2019 Apr 25;62(8):3989-4012. doi: 10.1021/acs.jmedchem.8b02021. Epub 2019 Apr 9.

PMID:
30908048
3.

Accelerating Drug Discovery Efforts for Trypanosomatidic Infections Using an Integrated Transnational Academic Drug Discovery Platform.

Moraes CB, Witt G, Kuzikov M, Ellinger B, Calogeropoulou T, Prousis KC, Mangani S, Di Pisa F, Landi G, Iacono LD, Pozzi C, Freitas-Junior LH, Dos Santos Pascoalino B, Bertolacini CP, Behrens B, Keminer O, Leu J, Wolf M, Reinshagen J, Cordeiro-da-Silva A, Santarem N, Venturelli A, Wrigley S, Karunakaran D, Kebede B, Pöhner I, Müller W, Panecka-Hofman J, Wade RC, Fenske M, Clos J, Alunda JM, Corral MJ, Uliassi E, Bolognesi ML, Linciano P, Quotadamo A, Ferrari S, Santucci M, Borsari C, Costi MP, Gul S.

SLAS Discov. 2019 Mar;24(3):346-361. doi: 10.1177/2472555218823171.

PMID:
30784368
4.

Discovery of new potent hits against intracellular Trypanosoma cruzi by QSAR-based virtual screening.

Melo-Filho CC, Braga RC, Muratov EN, Franco CH, Moraes CB, Freitas-Junior LH, Andrade CH.

Eur J Med Chem. 2019 Feb 1;163:649-659. doi: 10.1016/j.ejmech.2018.11.062. Epub 2018 Nov 29.

PMID:
30562700
5.

Development of a Focused Library of Triazole-Linked Privileged-Structure-Based Conjugates Leading to the Discovery of Novel Phenotypic Hits against Protozoan Parasitic Infections.

Uliassi E, Piazzi L, Belluti F, Mazzanti A, Kaiser M, Brun R, Moraes CB, Freitas-Junior LH, Gul S, Kuzikov M, Ellinger B, Borsari C, Costi MP, Bolognesi ML.

ChemMedChem. 2018 Apr 6;13(7):678-683. doi: 10.1002/cmdc.201700786. Epub 2018 Feb 16.

PMID:
29451361
6.

Aryl thiosemicarbazones for the treatment of trypanosomatidic infections.

Linciano P, Moraes CB, Alcantara LM, Franco CH, Pascoalino B, Freitas-Junior LH, Macedo S, Santarem N, Cordeiro-da-Silva A, Gul S, Witt G, Kuzikov M, Ellinger B, Ferrari S, Luciani R, Quotadamo A, Costantino L, Costi MP.

Eur J Med Chem. 2018 Feb 25;146:423-434. doi: 10.1016/j.ejmech.2018.01.043. Epub 2018 Jan 31.

PMID:
29407968
7.

Crassiflorone derivatives that inhibit Trypanosoma brucei glyceraldehyde-3-phosphate dehydrogenase (TbGAPDH) and Trypanosoma cruzi trypanothione reductase (TcTR) and display trypanocidal activity.

Uliassi E, Fiorani G, Krauth-Siegel RL, Bergamini C, Fato R, Bianchini G, Carlos Menéndez J, Molina MT, López-Montero E, Falchi F, Cavalli A, Gul S, Kuzikov M, Ellinger B, Witt G, Moraes CB, Freitas-Junior LH, Borsari C, Costi MP, Bolognesi ML.

Eur J Med Chem. 2017 Dec 1;141:138-148. doi: 10.1016/j.ejmech.2017.10.005. Epub 2017 Oct 3.

PMID:
29031061
8.

Exploiting the 2-Amino-1,3,4-thiadiazole Scaffold To Inhibit Trypanosoma brucei Pteridine Reductase in Support of Early-Stage Drug Discovery.

Linciano P, Dawson A, Pöhner I, Costa DM, Sá MS, Cordeiro-da-Silva A, Luciani R, Gul S, Witt G, Ellinger B, Kuzikov M, Gribbon P, Reinshagen J, Wolf M, Behrens B, Hannaert V, Michels PAM, Nerini E, Pozzi C, di Pisa F, Landi G, Santarem N, Ferrari S, Saxena P, Lazzari S, Cannazza G, Freitas-Junior LH, Moraes CB, Pascoalino BS, Alcântara LM, Bertolacini CP, Fontana V, Wittig U, Müller W, Wade RC, Hunter WN, Mangani S, Costantino L, Costi MP.

ACS Omega. 2017 Sep 30;2(9):5666-5683. doi: 10.1021/acsomega.7b00473. Epub 2017 Sep 11.

9.

Computer-aided discovery of two novel chalcone-like compounds active and selective against Leishmania infantum.

Gomes MN, Alcântara LM, Neves BJ, Melo-Filho CC, Freitas-Junior LH, Moraes CB, Ma R, Franzblau SG, Muratov E, Andrade CH.

Bioorg Med Chem Lett. 2017 Jun 1;27(11):2459-2464. doi: 10.1016/j.bmcl.2017.04.010. Epub 2017 Apr 4.

10.

Chroman-4-One Derivatives Targeting Pteridine Reductase 1 and Showing Anti-Parasitic Activity.

Di Pisa F, Landi G, Dello Iacono L, Pozzi C, Borsari C, Ferrari S, Santucci M, Santarem N, Cordeiro-da-Silva A, Moraes CB, Alcantara LM, Fontana V, Freitas-Junior LH, Gul S, Kuzikov M, Behrens B, Pöhner I, Wade RC, Costi MP, Mangani S.

Molecules. 2017 Mar 8;22(3). pii: E426. doi: 10.3390/molecules22030426.

11.

Synthesis and trypanocidal activity of a library of 4-substituted 2-(1H-pyrrolo[3,2-c]pyridin-2-yl)propan-2-ols.

Balfour MN, Franco CH, Moraes CB, Freitas-Junior LH, Stefani HA.

Eur J Med Chem. 2017 Mar 10;128:202-212. doi: 10.1016/j.ejmech.2017.01.040. Epub 2017 Feb 3.

PMID:
28189084
12.

Methoxylated 2'-hydroxychalcones as antiparasitic hit compounds.

Borsari C, Santarem N, Torrado J, Olías AI, Corral MJ, Baptista C, Gul S, Wolf M, Kuzikov M, Ellinger B, Witt G, Gribbon P, Reinshagen J, Linciano P, Tait A, Costantino L, Freitas-Junior LH, Moraes CB, Bruno Dos Santos P, Alcântara LM, Franco CH, Bertolacini CD, Fontana V, Tejera Nevado P, Clos J, Alunda JM, Cordeiro-da-Silva A, Ferrari S, Costi MP.

Eur J Med Chem. 2017 Jan 27;126:1129-1135. doi: 10.1016/j.ejmech.2016.12.017. Epub 2016 Dec 9.

PMID:
28064141
13.

Design, synthesis and antitrypanosomal activity of some nitrofurazone 1,2,4-triazolic bioisosteric analogues.

Silva FT, Franco CH, Favaro DC, Freitas-Junior LH, Moraes CB, Ferreira EI.

Eur J Med Chem. 2016 Oct 4;121:553-560. doi: 10.1016/j.ejmech.2016.04.065. Epub 2016 Jun 1.

PMID:
27318979
14.

Novel drug discovery for Chagas disease.

Moraes CB, Franco CH.

Expert Opin Drug Discov. 2016;11(5):447-55. doi: 10.1517/17460441.2016.1160883. Epub 2016 Apr 1. Review.

PMID:
26967915
15.

Current and Future Chemotherapy for Chagas Disease.

Gaspar L, Moraes CB, Freitas-Junior LH, Ferrari S, Costantino L, Costi MP, Coron RP, Smith TK, Siqueira-Neto JL, McKerrow JH, Cordeiro-da-Silva A.

Curr Med Chem. 2015;22(37):4293-312. Review.

PMID:
26477622
16.

Enantiomers of nifurtimox do not exhibit stereoselective anti-Trypanosoma cruzi activity, toxicity, or pharmacokinetic properties.

Moraes CB, White KL, Braillard S, Perez C, Goo J, Gaspar L, Shackleford DM, Cordeiro-da-Silva A, Thompson RC, Freitas-Junior L, Charman SA, Chatelain E.

Antimicrob Agents Chemother. 2015;59(6):3645-7. doi: 10.1128/AAC.05139-14. Epub 2015 Apr 6.

17.

Drug discovery for human African trypanosomiasis: identification of novel scaffolds by the newly developed HTS SYBR Green assay for Trypanosoma brucei.

Faria J, Moraes CB, Song R, Pascoalino BS, Lee N, Siqueira-Neto JL, Cruz DJ, Parkinson T, Ioset JR, Cordeiro-da-Silva A, Freitas-Junior LH.

J Biomol Screen. 2015 Jan;20(1):70-81. doi: 10.1177/1087057114556236. Epub 2014 Oct 23.

PMID:
25342146
18.

Drug discovery for Chagas disease should consider Trypanosoma cruzi strain diversity.

Zingales B, Miles MA, Moraes CB, Luquetti A, Guhl F, Schijman AG, Ribeiro I; Drugs for Neglected Disease Initiative; Chagas Clinical Research Platform Meeting.

Mem Inst Oswaldo Cruz. 2014 Sep;109(6):828-33. Epub 2014 Aug 22.

19.

Nitroheterocyclic compounds are more efficacious than CYP51 inhibitors against Trypanosoma cruzi: implications for Chagas disease drug discovery and development.

Moraes CB, Giardini MA, Kim H, Franco CH, Araujo-Junior AM, Schenkman S, Chatelain E, Freitas-Junior LH.

Sci Rep. 2014 Apr 16;4:4703. doi: 10.1038/srep04703.

20.

Chemosensitization potential of P-glycoprotein inhibitors in malaria parasites.

Alcantara LM, Kim J, Moraes CB, Franco CH, Franzoi KD, Lee S, Freitas-Junior LH, Ayong LS.

Exp Parasitol. 2013 Jun;134(2):235-43. doi: 10.1016/j.exppara.2013.03.022. Epub 2013 Mar 28.

PMID:
23541983

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