Substituted 2-alkyl-1-OXO-N-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides for antimalarial therapies

摘要

In one aspect, the invention relates to novel substituted 2-alkyl-1-oxo-N-phenyl-3-heteroaryl -1,2,3,4-tetrahydroisoquinoline-4-carboxamides; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating and/or preventing malaria. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

主权项

1. A compound having a structure represented by a formula: wherein Ar1 is selected from 3-pyridinyl, 4-isoxazolyl, N-methyl-4-pyrazolyl, 4-pyrazolyl, 4-isothiazolyl, 5-thiazolyl, 5-pyrimidinyl, or 4-pyridazinyl; R1 is selected from CF3, (CH3)2CH or cyclopropyl, R2 and R3 are independently selected from H, OCH3 or F; Ar2 has a structure represented by a formula: wherein R4a, R4b and R5 are independently selected from H, CN, F, Cl or OCF3, or a pharmaceutically acceptable salt, tautomer, geometrical isomer or optically active form thereof.