Results 11 to 20 of about 2,263 (168)

Scalable Access to N‑Acylindole Linkages: Enabling the Synthesis of Antitrypanosomal Noncanonical Cyclic Peptides for Chagas Disease. [PDF]

Angew Chem Int Ed Engl
A gram‐scale supply of bulbiferamide A, which features a rare N‐acylindole linkage and possesses potent inhibitory activity against Trypanosoma cruzi epimastigotes (IC50 = 4.1 µM)—the causative parasite of Chagas disease—was successfully achieved. Moreover, the cyclization strategy developed in this study facilitated the synthesis of noncanonical ...
Zhang J, Nakamura H.
europepmc   +3 more sources

African Trypanosomiasis Research at a Crossroads: Bibliometric and Systematic Insights for the Future. [PDF]

J Parasitol Res
Aim Despite a reduction in the overall incidence and prevalence in the last two decades, trypanosomiasis continues to be a public health concern in Africa. This study was designed to comprehensively evaluate current trends in trypanosomiasis research using bibliometric approaches to uncover emerging topics and knowledge gaps, thereby guiding future ...
Ogra IO, Adaji JZ, Jonathan EU, Nwajiani BK, Usman S, Kurovsky A, Sossou K, Balogun EO.   +7 more
europepmc   +2 more sources

Exploring Novel Nitrofuryl‐1,3,4‐Thiadiazole‐Based Derivatives: Design, Synthesis, and Evaluation of In Vitro Leishmanicidal and Trypanocidal Activity [PDF]

Arch Pharm (Weinheim)
In a series of substituted 1‐[5‐(5‐nitrofuran‐2‐yl)‐1,3,4‐thiadiazol‐2‐yl]piperidine‐4‐carboxamides evaluated for in vitro antileishmanial and antitrypanosomal activity, compound 18 emerged as the most promising derivative, showing submicromolar anti‐parasitic effects targeting diverse Leishmania and Trypanosoma species and acceptable selectivity ...
Mousavi A, Slapničková M, Norouzbahari M, D'Alessandro S, Foroumadi P, Peytam F, Perego F, Doleželová E, Emamgholipour Z, Tehrani M, Sadat‐Ebrahimi S, Hosseinzadeh E, Ahadi E, Firoozpour L, Bijanzadeh H, Basilico N, Zíková A, Foroumadi A.   +17 more
europepmc   +2 more sources

Cymantrenyl-Nucleobases: Synthesis, Anticancer, Antitrypanosomal and Antimicrobial Activity Studies

Molecules, 2017
The synthesis of four cymantrene-5-fluorouracil derivatives (1–4) and two cymantrene-adenine derivatives (5 and 6) is reported. All of the compounds were characterized by spectroscopic methods and the crystal structure of two derivatives (1 and 6 ...
Artur Jabłoński, Karolina Matczak, Aneta Koceva-Chyła, Kamil Durka, Dietmar Steverding, Katarzyna Jakubiec-Krześniak, Jolanta Solecka, Damian Trzybiński, Krzysztof Woźniak, Vanesa Andreu, Gracia Mendoza, Manuel Arruebo, Krzysztof Kochel, Barbara Krawczyk, Dominik Szczukocki, Konrad Kowalski   +15 more
doaj   +3 more sources

Antitrypanosomal Activity of Fluoroquinolones [PDF]

Antimicrobial Agents and Chemotherapy, 1999
ABSTRACT Six fluoroquinolones presently in clinical use and four investigational tetracyclic fluoroquinolones were tested for in vitro activity against bloodstream-form Trypanosoma brucei brucei . All compounds had measurable activity, but the tetracyclic analogs were most potent, with 50% effective ...
E, Nenortas, C, Burri, T A, Shapiro
openaire   +2 more sources

Synthesis and antitrypanosomal activities of novel pyridylchalcones [PDF]

European Journal of Medicinal Chemistry, 2017
A library of novel pyridylchalcones were synthesised and screened against Trypanosoma brucei rhodesiense. Eight were shown to have good activity with the most potent 8 having an IC50 value of 0.29 μM. Cytotoxicity testing with human KB cells showed a good selectivity profile for this compound with a selectivity index of 47.
Bhambra, Avninder S., Ruparelia, K. C., Tan, Hoon Leong, Tasdemir, D., Burrell-Saward, H., Yardley, Vanessa, Beresford, Kenneth J. M., Arroo, R. R. J.   +7 more
openaire   +4 more sources

Sesquiterpene Lactones from Vernonia cinerascens Sch. Bip. and Their in Vitro Antitrypanosomal Activity. [PDF]

Molecules, 2018
Kimani NM, Matasyoh JC, Kaiser M, Brun R, Schmidt TJ.   +4 more
europepmc   +2 more sources

Antitrypanosomal Activities of Tryptanthrins [PDF]

Antimicrobial Agents and Chemotherapy, 2002
ABSTRACT New drugs and molecular targets are needed against Trypanosoma brucei , the protozoan that causes African sleeping sickness. Tryptanthrin (indolo[2,1-b]quinazoline-6,12-dione), a traditional antifungal agent, and 11 analogs were tested against T. brucei in vitro.
John, Scovill, Elizabeth, Blank, Michael, Konnick, Elizabeth, Nenortas, Theresa, Shapiro   +4 more
openaire   +2 more sources

Synthesis, characterization and in vitro antitrypanosomal activities of new carboxamides bearing quinoline moiety. [PDF]

PLoS ONE, 2018
The reported toxicities of current antitrypanosomal drugs and the emergence of drug resistant trypanosomes underscore the need for the development of new antitrypanosomal agents.
David Izuchukwu Ugwu, Uchechukwu Chris Okoro, Narendra Kumar Mishra   +2 more
doaj   +1 more source

Antitrypanosomal Activities of Proteasome Inhibitors [PDF]

Antimicrobial Agents and Chemotherapy, 2002
ABSTRACT Seven peptidyl proteasome inhibitors were tested for in vitro activity against Trypanosoma brucei bloodstream forms. Two compounds showed activity in the low nanomolar range. In general, trypanosomes were more susceptible to the compounds than were human HL-60 cells.
Njinkeng Joseph, Nkemngu, Joseph, Nkemgu-Njinkeng, Vera, Rosenkranz, Michael, Wink, Dietmar, Steverding   +4 more
openaire   +4 more sources