Synthesis and potent antiprotozoal activity of mono/di amidino 2-anilinobenzimidazoles versus Plasmodium falciparum and Trypanosoma brucei rhodesiense
Bioorganic and Medicinal Chemistry, cilt.24, sa.18, ss.4038-4044, 2016 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 24 Sayı: 18
- Basım Tarihi: 2016
- Doi Numarası: 10.1016/j.bmc.2016.06.047
- Dergi Adı: Bioorganic and Medicinal Chemistry
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.4038-4044
- Anahtar Kelimeler: Anilinobenzimidazoles, Carboxamidines, Antiparasitic agents, Plasmodium falciparum, Trypanosoma brucei rhodesiense
- Sağlık Bilimleri Üniversitesi Adresli: Hayır
Özet
A series of mono and dicationic new 2-anilinobenzimidazole carboxamidines were prepared in a four step process starting from 4-amino-3-nitrobenzonitrile and corresponding o-phenylenediamines. Their antiparasitic activity against Plasmodium falciparum (P. falciparum) and Trypanosoma brucei rhodesiense (T.b. rhodesiense) were evaluated in vitro. Some of the dicationic compounds (10,12,14) showed equal or very close activity against T.b. rhodesiense with melarsoprol and also showed promising activity against P. falciparum as compared to chloroquine. Among the monocationic derivatives compound 21 exhibited best inhibitory activity against P. falciparum.