Leishmanicidal activity of some aliphatic diamines and amino-alcohols.
A number of aliphatic diamines and amino-alcohols and several of their alkyl, acyl and carbamoyl derivatives, have been synthesised and evaluated in vitro on cultures of Leishmania spp. In general, diamine derivatives resulted to be more potent than their amino-alcohol or amino-ether analogues. Two diamine derivatives (8b and 9d) and one amino-alcohol (6a) showed a fair inhibition of parasite growth, at concentrations below 10 microg/mL, with potencies close to that of the reference drug, amphotericin B. Some SAR considerations have been deduced.
del Olmo
Esther
E
Departamento de Quijmica Farmaceutica, Facultad de Farmacia, Univ. de Salamanca, 37007, Salamanca, Spain. olmo@usal.es
Alves
Mario
M
López
José L
JL
Inchaustti
Alba
A
Yaluff
Gloria
G
Rojas de Arias
Antonieta
A
San Feliciano
Arturo
A
D000605:Amino Alcohols / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D003959:Diamines / Q000138:chemical synthesis / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D007891:Leishmania / Q000187:drug effects* / Q000254:growth & development; D021261:Parasitic Sensitivity Tests; D013329:Structure-Activity Relationship
D000605:Amino Alcohols; D000981:Antiprotozoal Agents; D003959:Diamines