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1.
Figure 2

Figure 2. From: Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. 1. Sildenafil analogs.

Strategy for exploration of the sildenafil core.

Cuihua Wang, et al. Bioorg Med Chem Lett. ;22(7):2579-2581.

CitationFull text

2.
Figure 1

Figure 1. From: Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. 1. Sildenafil analogs.

Human PDE5 inhibitors marketed for erectile dysfunction.

Cuihua Wang, et al. Bioorg Med Chem Lett. ;22(7):2579-2581.

CitationFull text

3.
Scheme 4

Scheme 4. From: Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. 1. Sildenafil analogs.

Synthesis of 26a–c. Reagents and Conditions. a) 2-chloronicotinic acid, PyBroP, Et3N; (b) R-OH, KOtBu.

Cuihua Wang, et al. Bioorg Med Chem Lett. ;22(7):2579-2581.

CitationFull text

4.
Scheme 2

Scheme 2. From: Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. 1. Sildenafil analogs.

Synthesis of 20–22. Reagents and Conditions.(a) CDI, A,70 °C, EtOAc, o/n; (b) PyBroP, A, Et3N, DCE, MW 120 °C 20 min; (c) SOCl2; (d) NH3, iPrOH; (e) NaOEt, EtOH, MW 120 °C 10 min.

Cuihua Wang, et al. Bioorg Med Chem Lett. ;22(7):2579-2581.

CitationFull text

5.
Scheme 3

Scheme 3. From: Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. 1. Sildenafil analogs.

Synthesis of 24a–d. Reagents and Conditions. (a) R5CO2H, imidazole-HCl, CDI, then 23, 50 °C, o/n;. b) EtOH, NaOEt, 120 °C, 2 h. Refer to for the identity of R-groups.

Cuihua Wang, et al. Bioorg Med Chem Lett. ;22(7):2579-2581.

CitationFull text

6.
Scheme 1

Scheme 1. From: Synthesis and evaluation of human phosphodiesterases (PDE) 5 inhibitor analogs as trypanosomal PDE inhibitors. 1. Sildenafil analogs.

Synthesis of 5–14. Reagents and Conditions. (a) PyBroP, TEA, DCE, 120 °C, MW, 10 min; (b) NH4OH, dioxane, rt; (c) NaOEt/EtOH, 120 °C, MW, 10 min; (d) R1-I, CuI, trans-cyclohexane-1,2-diamine, Cs2CO3,DMF, 110 °C; (e) NaH, 2-bromoacetamide, 0 °C to rt. Refer to for the identity of R-groups.

Cuihua Wang, et al. Bioorg Med Chem Lett. ;22(7):2579-2581.

CitationFull text

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