2001 pyrimidine derivatives

pyrimidine derivativesR 0510

45 - 167Design and Synthesis of Novel Antibacterial Agents with InhibitoryActivity Against DNA Polymerase III. — Reaction of pyrimidine (I)with disubstituted anilines (II) yields the pyrimidine analogues (III) which areweakly active Pol III inhibitors and some of them exhibit antibacterial activityagainst Gram-positive bacteria. Variation of substituents in the 4-position of(III) leads to derivatives (V) and (VI). In general, the phenoxy derivatives (V)are weaker inhibitors than the parent 4-chloro compounds (III). However, 3-or 4-substituted phenoxy derivatives (Vc) and (Vd) show improved activitycompared to parent compounds (III). Surprisingly, related analogues of (Vc),cf. (Va) and (Vb), are poor inhibitors of Pol III. — (ALI, AMJAD; ET AL.;Bioorg. Med. Chem. Lett. 11 (2001) 16, 2185-2188; Dep. Med. Chem., MerckRes. Lab., Rahway, NJ 07065, USA; EN)

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