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In vitro assays identified thiohydantoins with anti-trypanosomatid activity and molecular modelling studies indicated possible selective CYP51 inhibition. [PDF]
Camargo PG +9 more
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Synthesis and Biological Evaluation of 4‑(4-Nitrophenyl)‑1<i>H</i>‑1,2,3-triazole Derivatives as Antitrypanosomal Agents. [PDF]
Oliveira FC +8 more
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Expert Opinion on Investigational Drugs, 2005
Trypanosomes are the causative agents of Chagas' disease in Central and South America and sleeping sickness in sub-Saharan Africa. The current chemotherapy of the human trypanosomiases relies on only six drugs, five of which were developed > 30 years ago.
Steverding, Dietmar, Tyler, Kevin M.
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Trypanosomes are the causative agents of Chagas' disease in Central and South America and sleeping sickness in sub-Saharan Africa. The current chemotherapy of the human trypanosomiases relies on only six drugs, five of which were developed > 30 years ago.
Steverding, Dietmar, Tyler, Kevin M.
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Antitrypanosomal Activity of Phosphonylmethoxyalkylpurines
The Journal of Parasitology, 1994Phosphonylmethoxyalkylpurines and -pyrimidines exhibit potent activity against a broad spectrum of DNA viruses. We evaluated some of these nucleotide analogues for antitrypanosomal activity in vitro and in mice. The most active compounds were (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl) adenine (HPMPA) and (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)-2,6-
R, Kaminsky, E, Zweygarth, E, De Clercq
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Bistacrines as potential antitrypanosomal agents
Bioorganic & Medicinal Chemistry, 2017Human African Trypanosomiasis (HAT) is caused by two subspecies of the genus Trypanosoma, namely Trypanosoma brucei rhodesiense and Trypanosoma brucei gambiense. The disease is fatal if left untreated and therapy is limited due to only five non-adequate drugs currently available. In preliminary studies, dimeric tacrine derivatives were found to inhibit
Ines, Schmidt +10 more
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Antitrypanosomal Therapy for Chronic Chagas' Disease
New England Journal of Medicine, 2011A 42-year-old woman presents after donating blood and receiving a report that she is positive for Chagas' disease. Chagas' disease is caused by a parasite and is endemic in many parts of Latin America.
Facundo, Garcia-Bournissen +1 more
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Antileishmanial and antitrypanosomal drug identification
Emerging Topics in Life Sciences, 2017Although the treatments for human African trypanosomiasis (HAT), leishmaniasis and Chagas disease (CD) still rely on drugs developed several decades ago, there has been significant progress in the identification, development and use of novel drugs and formulations. Notably, there are now two drugs in clinical trial for HAT, fexinidazole and acoziborole;
Simon L, Croft +2 more
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Antitrypanosomal and Antileishmanial Activities
2018The so-called neglected tropical diseases, which are endemic in 149 tropical and subtropical countries, affect more than 1 billion people annually, including 875 million children in developing economies. These diseases are responsible for over 500,000 deaths per year and are characterized by long-term disability and severe pain.
Sanchez Alberti, Andrés +3 more
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