Neglected diseases due to the parasitic protozoa Leishmania and Trypanosoma (kinetoplastids)
affect millions of people worldwide, and the lack of suitable treatments has promoted an ongoing
drug discovery effort to identify novel nontoxic and cost-effective chemotherapies. Polyamines are
ubiquitous small organic molecules that play key roles in kinetoplastid parasites metabolism, redox homeostasis
and in the normal progression of cell cycles, which differ from those found in the mammalian
host. These features make polyamines attractive in terms of antiparasitic drug development. The present
work provides a comprehensive insight on the use of polyamine derivatives and related nitrogen compounds
in the chemotherapy of kinetoplastid diseases. The amount of literature on this subject is considerable,
and a classification considering drug targets and chemical structures were made. Polyamines,
aminoalcohols and basic heterocycles designed to target the relevant parasitic enzyme trypanothione
reductase are discussed in the first section, followed by compounds directed to less common targets, like
parasite SOD and the aminopurine P2 transporter. Finally, the third section comprises nitrogen compounds
structurally derived from antimalaric agents. References on the chemical synthesis of the selected
compounds are reported together with their in vivo and/or in vitro IC50 values, and structureactivity
relationships within each group are analyzed. Some favourable structural features were identified
from the SAR analyses comprising protonable sites, hydrophobic groups and optimum distances
between them. The importance of certain pharmacophoric groups or amino acid residues in the bioactivity
of polyamine derived compounds is also discussed.
An Alternate Cost-effective Medium for In Vitro Regeneration of Therapeutically Important Ocimum citriodorum Vis