Survey of Antimalarial Agents. Public Health Monograph No. 9

Triazine as a promising scaffold for its versatile biological behavior

“…Chemical modification of quinine nucleus led to the development of other therapeutic agents such as chloroquine [82] (60), pamaquine [83] (61) and mefloquine [84] (62, Fig. 27).…”

Synthesis and Antimicrobial Activity of Benzo[H][1,6]Naphthyridine Derivatives

“…The N-alkylation on 4-aminoquinolines using benzoylacetonitrile, diethyl 2-(ethoxymethylene) malonate was carried under mild reaction conditions. The benzo[h] [1,6] naphthyridine derivatives 8(a-b), 9(a-b) were obtained from open chain analog of 4- aminoquinolines 6(a-b). The open chain quinline derivatives showed antimicrobial activity while cyclic benzo[h] [1,6]naphthyridine derivatives found totally against bacteria utilized.…”

“…For this reason the search is ongoing for new natural or synthetic antimicrobial agents [5]. Quinoline derivatives have been used for the treatment of malaria [6]. Systematic modification of quinine led to the potent antimalarial chloroquine 2 drug [7].…”

“…Recently, 4-amino-7-chloro-quinoline derivatives have demonstrated mycobacterium tuberculosis activity [20][21][22][23][24][25][26][27][28][29]. Benzo[h] [1,6]naphthyridine derivatives also showed antimalarial activity 5 [30].…”

“…The enamine 6 was cyclized by refluxing in diphenylether for 30 min yielded brown colored to desired benzo[h] [1,6]naphthyridine derivatives 8 in 70-75% yield. The compound 6a refluxed in POCl 3 furnished mixture of compounds 8 and 9 as yellow coloured solids in 20 % and 40% yield respectively.…”