the resistance of plasmodium falciparum to 4-amioquinolines has been confirmed in parts of south america such as venezuela, colombia, brazil and panama since 1961. during 1968-1970, 147 p. falciparum cases in the kazeroon and bandar abbas areas were tested against 4-aminoquinolines, bases on 25 mg resochin /kg of body weight over a period of 3 days. twenty–foure, 48 , 72 and 96 hours after drug...

A diverse set of highly substituted 4-aminoquinolines was synthesized from ynamides, triflic anhydride, 2-chloropyridine, and readily accessible amides in a mild one-step procedure.

We developed a one-pot, two-stage synthetic route to substituted 4-aminoquinolines involving an imidoylative Sonogashira coupling followed by acid-mediated cyclization. This three-component reaction affords pharmaceutically valuable 4-aminoquinolines in a one-pot procedure from readily available starting materials. The reaction tolerates various substituents on the arene as well as the use of s...

Palladium-catalyzed oxidative coupling of 2-vinylanilines and isocyanides constitutes a direct, facile, and efficient approach to 2-aminoquinolines. The procedure, employing palladium acetate and silver carbonate, is attractive in terms of assembly efficiency, functional group tolerance, and operational simplicity. A variety of 2-aminoquinolines were prepared in good to excellent yields.

The occurrence, during the present decade, of resistance to the 4-aminoquinoline compound chloroquine, in infections of Plasmodium falciparum in certain regions of South America and South East Asia, has focused attention upon drug resistance as a problem in the therapeutic treatment of malaria, since this drug is widely used in prophylaxis and treatment of the clinical attack. Resistance to oth...

Due to growing problems with drug resistance, there is an outstanding need for new, cost-effective drugs for the treatment of malaria. The 4-aminoquinolines have provided a number of useful antimalarials, and Plasmodium falciparum, the causative organism for the most deadly form of human malaria, is generally slow to develop resistance to these drugs. Therefore, diverse screening libraries of q...

Synthesis of novel aminoquinoline derivatives has been accomplished and their activity against malaria strains examined. The compounds showed moderate in vitro antimalarial two P. falciparum strains, 3D7 (CQ susceptible clone) Dd2 resistant clone). Three aminoquinolines were further examined for efficacy a mouse model using modified Thompson test. In this model, mice infected with berghei-infec...