Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines.
The synthesis of 2-(5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)hydrazone-derivatives (BTPs) and their in vitro evaluation against Trypanosoma cruzi trypomastigotes, Mycobacterium tuberculosis, Leishmania amazonensis axenic amastigotes, and six human cancer cell lines is described. The in vivo activity of the most active and least toxic compounds against T. cruzi and L. amazonensis was also studied. BTPs constitute a new family of drug leads with potential activity against infectious diseases. Due to their drug-like properties, this series of compounds can potentially serve as templates for future drug-optimization and drug-development efforts for use as therapeutic agents in developing countries.
Aponte
José C
JC
Department of Chemistry, University of Louisville, Louisville, KY 40292, USA.
Vaisberg
Abraham J
AJ
Castillo
Denis
D
Gonzalez
German
G
Estevez
Yannick
Y
Arevalo
Jorge
J
Quiliano
Miguel
M
Zimic
Mirko
M
Verástegui
Manuela
M
Málaga
Edith
E
Gilman
Robert H
RH
Bustamante
Juan M
JM
Tarleton
Rick L
RL
Wang
Yuehong
Y
Franzblau
Scott G
SG
Pauli
Guido F
GF
Sauvain
Michel
M
Hammond
Gerald B
GB
D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000633:toxicity; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D045744:Cell Line, Tumor; D006801:Humans; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D021261:Parasitic Sensitivity Tests; D011743:Pyrimidines / Q000737:chemistry* / Q000633:toxicity; D014349:Trypanosoma cruzi / Q000187:drug effects
D000981:Antiprotozoal Agents; D000995:Antitubercular Agents; D011743:Pyrimidines