Introduction 1 2A 2B 3 1 2 3 2B 4 6 3 7 8 9 10 11 3 12 13 12 13 3 9 12 13 3 14 15 3 16 3 17 23 1 1–3 17 23 Fig. 1 3 3 8 5 17 21 2 3 3 2B 24 5 4 5 5 Chemistry 4, 5 8 6 18 7 8 1 Scheme 1 Preparation of designed compounds Results and discussion 4, 5 2, 3 1 2A 3 3 1 3 2A 3 25 2B 1 Table 1 4, 5 2, 3 Compound R 1 a 2A b 2B c 50 3 d 1 3 2A 3 2 CONHPh 310 (295–327) 27.7 (13.3–57.8) 3,440 (2,880–4,110) 1.80 (0.88–3.68) 172 15 3 2 1,040 (864–1,260) 282 (201–375) 12,620 (9,730–16,400) 0.92 (0.80–1.06) 1,130 360 4 COPh 2,030 (1,710–2,400) 879 (643–1,200) >30,000 15.7 (7.85–31.5) 129 56 5 2 20,700 (16,700–25,700) 6,060 (5,170–7,110) >30,000 744 (534–1,040) 28 8 Data are expressed as geometric means, with 95% confidence limits a 3 1 n b 3 2A c 50 2B d 3 3 2, 3 1 2 3 2A 2A 3 3 3 5 4 3 5 2–5 5 17 23 3 26 29 Experimental Section 29 30 3 5 3 3 3 3 2–4 2 17 23 Fig. 2 2–4 5 2 5 2–4 C=O C=O C=O 3 1 2 1 2A 2B 5 1 2 3 5 2–4 5 5 5 5 3 5 3 5 5 Fig. 3 5 5 5 5 5 2–4 5 4 5 4 Fig. 4 4 5 5 3 Conclusions 3 5 5 3 Experimental section Chemistry General 254 1 3 6 1 General procedures for the preparation of 5-(benzoyl)amino-8-methyl-2-(2-furyl)-pyrazolo[4,3 ]-1,2,4-triazolo[1,5-c]pyrimidine (4) and 5-benzensulfonamido-8-methyl-2-(2-furyl)-pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine (5) 6 2 4 4, 5 5-(Benzoyl)amino-8-methyl-2-(2-furyl)-pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine (4) −1 6 18 13 7 2 5-Benzensulfonamido-8-methyl-2-(2-furyl)-pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine (5) −1 6 17 13 7 3 Biology 25 g g 1 3 3 2A 3 3 3 31 2B 50 i 32 Computational methodologies 33 34 35 3 3 3 3 36 R 3 3 36 37 −1 −1 34 Ligand-based homology modeling 3 28 38 34 34 34 i 34 3 39 40 −1 −1 34