Biochemical and pharmacologic properties of 2614W94, a reversible, competitive inhibitor of monoamine oxidase-A

Interactions of Nitrogen-Containing Xenobiotics with Monoamine Oxidase (MAO) Isozymes A and B: SAR Studies on MAO Substrates and Inhibitors

“…On the basis of its overall pharmacological profile, 109 was advanced into clinical trials as an antidepressant/anxiolytic agent. Hepatotoxic side-effects in man, however, caused it to be withdrawn from further consideration ( , ).…”

Recent Advances in Malaria Chemotherapy

“…In fact, the as so ci a tion of two antimalarial mol e cules should al low to im prove the treat ment ef fi cacy and to avoid the emer gence of re sis tant strains. 66 If one par a site is re sis tant to a drug A in a pop u la tion of 10 9 par a sites, and one par a site re sis tant to a drug B in a pop u la tion of 10 9 par a site, only one in a pop u la tion of 10 18 par a sites will be re sis tant to both drugs A and B. Each ill per son be ing car rier of 10 8 to 10 12 par a sites, the prob a bil ity of si mul ta neous re sis tance to two drugs act ing with dif fer ent modes is close to zero.…”

“…Keeping in mind that heme lib er ated in the par a site food vac u ole is a tar get of spe cial in ter est, there are good argu ments for com bin ing an artemisinin de riv a tive to all newly in tro duced antimalarial drug to de lay or even pre vent the devel op ment of re sis tance. 66 We adopt this ther apy ap proach by pre par ing new chi me ric mol e cules by co va lently at tach ing a trioxane moi ety to a 4-aminoquinoline en tity. 82 These mol ecules, named trioxaquines (Fig.…”