Antimosquito Properties of 2-Substitutedphenyl/benzylamino-6-(4-chlorophenyl)-5-methoxycarbonyl-4-methyl-3,6-dihydropyrimidin-1-ium Chlorides against the Anopheles arabiensis

VENUGOPALA K.N.; GLEISER, R.M.; CHALANNAVAR R.K.; ODHAV B.

MEDICINAL CHEMISTRY

BENTHAM SCIENCE PUBL LTD

Lugar: Oak Park; Año: 2014 vol. 10 p. 211 - 219

1573-4064

Eight novel dihydropyrimidine analogs named DHPM1-DHPM8 were synthesized 13 in their hydrochloride salt form using one pot synthesis between methyl 2-chloro-4-(4-14 chlorophenyl)-6 methyl-1,4-dihydropyrimidine-5-carboxylate and substituted arylamines in 15 isopropanol. The antimosquito effect of the test compounds were assessed against the adult 16 mosquito Anopheles arabiensis. For adulticidal properties the test compounds were sprayed 17 onto ceramic tiles and screened using the cone bio-assay method. The larvicidal activity was 18 tested by monitoring larval mortality daily and up to 3 days of exposure. Repellency 19 properties were tested in a feeding-probe assay using unfed female Anopheles arabiensis. 20 Compounds DHPM1, DHPM4, DHPM5 and DHPM6 exerted larval mortality equivalent to 21 temephos (trade name Abate, a commercial anti-larvicidal compound). Compounds DHPM1 22 to DHPM5 repelled or knocked down 92 to 98% of mosquitoes exposed to rodent skin treated 23 with the compounds. None of the compounds showed any significant activity against the 24 adult mosquito Anopheles arabiensis.