Structural Overlay for Diaryl Heterocycle PDS Inhibitors and Newer Developments

10 Structural Overlay for Diaryl Heterocycle PDS Inhibitors and Newer Developments 

Structural overlay of flurtamone, fluridone and NTN-28621 led to a new pyrazolone 28 and pyridine 29, many pyrimidines 30 and some 1,2,4-triazines 31 with the joint possession of 1,3-connected phenyl groups ( 1,3-diaryl-heterocycle ) (Fig. 4.1.11) [34]. A pyrimidine 30 with = CH3O, = H, X = 3-CF3 and 

Y = F has been reported with appUcation rates as low as 63 g ha . Other substituents for are NMe2, CH3 and C02Et while was H. In another series, 

R was kept constant with hydrogen while R could vary from OH to MeS and X was 2-CH3, 2-Cl and 3-CF3. 

Along this line, Table 4.1.3 represents recent developments, from which 32-37 pursue substituted hetarylethers with 3S integrating its ether bridge into a heterocycle. Compounds 38-40 constitute classical pyrimidines, while pyrimidines 41 and 42 are purely aliphatically substituted. Notably, both also inhibit ZDS. Compounds 44 and 45 may be viewed as substituted phenylpyrrolidinones. The keto-morpholine 43, the carbonamide 46 and the carbamate 47 are new PDS leads. 

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