In the present study, starting compound 4 was prepared by deamination of compound 2 in the presence of hypophosphorous acid and sodium nitrite. Treatment of compound 4 with ethyl bromoacetate produced ethyl[3-(4-chlorophenyl)-5-(4-methoxybenzyl)-4H-1,2,4-triazol-4-yl]acetate (5), which was converted to the hydrazide derivative (6) by treatment with hydrazine hydrate. The reaction of compound 6 with aromatic aldehydes resulted in the formation of arylidene hydrazides (7). Treatment of 6 with CS 2 in the presence of potassium hydroxide (KOH), followed by cyclization with hydrazine hydrate, afforded 4-amino-5-{[3-(4-chlorophenyl)-5-(4-methoxybenzyl)-4H-1,2,4-triazol-4-yl]-methyl}-2,4-dihydro-3H-1,2,4-triazole-3-thione (9). The condensation of 9 with appropriate aldehydes gave Schiff bases (10), which were converted into Mannich bases (11) in the presence of formaldehyde. All the synthesized compounds were screened for their anti-lipase and anti-urease activities. Compounds 7b, 7d, 11b, 11c, and 11d showed moderate-to-good lipase inhibitory effects compared to orlistat. Compounds 7b and 7d exhibited better anti-lipase activity. Furthermore, among the compounds tested, 11a and 11d were found to show high inhibitory effect against urease with IC 50 values of 12.39 AE 0.35 and 16.12 AE 1.06 mg/mL, respectively. Compound 11c showed moderate inhibitory activity. The Mannich base containing compound 11 may be a source of good leads for the synthesis of lipase and urease dual inhibitors.

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A series of new 1,2,4-triazole-3-one derivatives bearing the salicyl moiety were synthesized by using microwave irradiation, and their chemical structures were identified by IR, (1) H NMR, (13) C NMR, elemental analysis, and LC-MS. The anticonvulsant activities of the compounds 4a-c, 4e, and 5a-e were evaluated by the Anticonvulsant Screening Program of the National Institute of Health, USA. The compounds had moderate anticonvulsant activities in the maximum electroshock-induced seizure and minimal clonic seizure models in mice, without any neurotoxic effects.

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A new series of quinazolinone hybrid molecules containing coumarin, furan, 1,2,4triazole and 1,2,4-thiadiazole rings was designed, synthesized, and screened for their urease inhibition activities. All newly synthesized compounds showed outstanding urease inhibitory potentials with IC 50 values ranging between 1.26 ± 0.07 and 7.35 ± 0.31 μg/mL. Among the series, coumarin derivatives (10a-d) exhibited the best inhibitory effect against urease in the range of IC 50 = 1.26 ± 0.07 to 1.82 ± 0.10 μg/mL, when compared to standard urease inhibitors such as acetohydroxamic acid and thiourea (IC 50 = 21.05 ± 0.96 and 15.08 ± 0.71 μg/mL, respectively). Molecular docking studies were also performed to analyze the binding mode of compound 10b, and supported the experimental results. K E Y W O R D S coumarin, furan, molecular docking, quinazolin-4(3H)-one, thiadiazole, triazole, urease inhibition

Ö Z E T B ir seri tetra-substitüe benzimidazol türevi sentezlendi ve üreaz inhibisyon, anti-ksantin oksidaz (XO) ve antioksidan aktiviteleri incelendi. Bazı bileşiklerin önemli derecede antioksidan aktivite gösterdiği tespit edildi. Özellikle, bileşik 4, 5a, 5b, 5c, 5d ve 6b ABTS•+ radikal katyon temizleme (SC 50 : 9.51-70.43 µg/mL) ve bakır indirgeyici antioksidan kapasite (CUPRAC) tayininde yüksek derecede aktivite gösterdiği belirlendi. Bileşik 6d ise, 125 µg/mL derişimde en yüksek anti-ksantin oksidaz (XO) aktivitesi gösterdi. Bütün bileşikler Jack Bean üreaz aktivite tayin yöntemine göre incelendi ve en aktif üreaz inhibisyonuna sahip bileşiğin 7.41±0.13 µg/mL IC 50 değeriyle (5b) olduğu tespit edildi. Anahtar KelimelerÜreaz, ksantin oksidaz, enzim inhibisyon, antioksidan aktivite, benzimidazol. A B S T R A C TA series of tetra-substitued benzimidazole derivatives were synthesized and screened for their urease inhibition, anti-xanthine oxidase (XO) and antioxidant activities. Some of them were found to possess significant antioxidant activity, especially, compounds 4, 5a, 5b, 5c, 5d and 6b exhibited highly scavenging activity in ABTS•+ radical cation decolorization assay (SC 50 : 9.51-70.43 µg/mL) and cupric reducing antioxidant capacity (CUPRAC) assay. Compound 6d exhibited the highest XO inhibition at 125 µg/mL. All compounds were evaluated with regard to Jack Bean urease activity and the most active compound concerning urease enzyme inhibition was (5b), with an IC 50 value of 7.41±0.13 µg/mL.

A novel series of N′‐(2‐(3,5‐disubstituted‐4H‐1,2,4‐triazol‐4‐yl)acetyl)‐6/7/8‐substituted‐2‐oxo‐2H‐chromen‐3‐carbohydrazides were synthesized and studied for their α‐glucosidase inhibition activity. Most of the synthesized compounds exhibited potential α‐glucosidase inhibition activity with IC50 values ranging from 0.96 ± 0.02 to 32.86 ± 0.73 µg/ml. Among them, compounds 3e and 4e, having a methoxy group on the coumarin ring, proved to be the most potent ones, showing an enzyme inhibition activity with IC50 = 0.96 ± 0.02 and 1.44 ± 0.06 µg/ml, respectively. The kinetic study through Lineweaver–Burk plots revealed that the inhibition mechanism of the most active compounds 3d, 3e, 4d, and 4e, on the α‐glucosidase activity, was found to be in the competitive mode.