Synthesis and Pharmacological Evaluation of Some Novel 2-Mercapto Benzimidazole Derivatives

Abstract

ABSTRACT. The present study is synthesis of derivatives of N'-(4-amino-5-sulfanyl-4H-1,2,4-triazole-3-yl)-2-(1H-benzimidazole-2-ylsulfanyl) acetohydrazide (IV). Antibacterial activity tested against the E. coli and A. Substilis. Biological activities conducted by disc diffusion method. Compound 2MB1, 2MB3, 2MB5 inhibit the appreciable microbial growth while rest of the compound possess the moderate activities. Anti-inflammatory activity tested by reduces local edema induced in the rat paw by injection of phlogestic agent. Compound 2MB1, 2MB8, 2MB5, 2MB3 and 2MB6 exhibit satisfying anti-inflammatory activity while analgesic activity conducted by acetic acid induced writhing effect in mice while compound 2MB1, 2MB4 and 2MB7 having the good analgesic activity. The chemical structures of all newly synthesized compounds were confirmed by their IR, 1 H NMR and mass spectral data.

Functionalized Benzimidazole Scaffolds: Privileged Heterocycle for Drug Design in Therapeutic Medicine

“…), respectively . Analgesic activity at 20 mg/kg dose unveiled high inhibitory efficiency of 51 with inhibition of 74.9% , 52 with 59.7% , and 53 with 56.9% . However, at 50 mg/kg p.o., good analgesic activity was exhibited by 54 with basal reaction time 5.00 ± 0.57 s .…”

Synthesis of Novel Benzimidazole and Benzothiazole Derivatives Bearing a 1,2,3-triazole Ring System and their Acetylcholinesterase Inhibitory Activity

“…Compounds 3, 10, 11 and 13 were prepared according to the procedure described in the literature. [27][28][29] Synthesis of compounds 7; general procedure A mixture of benzyl halide derivative 4 (0.5 mmol), sodium azide 5 (0.040 g, 0.6 mmol), Cu(OAc) 2 (0.030 g, 0.15 mmol), ascorbic acid (0.025 g, 0.14 mmol) and sodium carbonate (0.02 g, 0.19 mmol) was stirred in EtOH (5 mL) at 60-70 °C for 30 min. Then, compound 3 (0.25 mmol) was added to the reaction mixture and the desired product 7 was obtained after 12-20 h. After completion of the reaction (checked by TLC), the mixture was filtered, the solvent was removed and the crude product was obtained by extraction with ethyl acetate (2 × 15 mL).…”

New multitarget directed benzimidazole‐2‐thiol‐based heterocycles as prospective anti‐radical and anti‐Alzheimer's agents

“…The literature is full of benzimidazole‐2‐thiol (BT, 2‐MBI) as medicinally active structures such as (BT) acyclic nucleosides as antibacterial agents (Figure 2e) (Amer, Ali, & El‐Kafaween, 2017), aminoacetylenic‐5‐ethoxy‐2‐mercaptobenzimidazoles as antibacterial and antifungal agents (Figure 2f) (Alkhafaji et al, 2018), 2‐MBI incorporated with thiazolidinone and isoxazole heterocycles as potent anticonvulsant and antiinflammatory/analgesic agents (Figure 2g,k) (Keri, Hiremathad, Budagumpi, & Nagaraja, 2015), 2‐MBI triazolylacetohydraziedes as antimicrobial, antiinflammatory, and analgesic agents (Figure 2h) (Nevade, Lokapure, & Kalyane, 2013), afobazole as potent anxiolytic drug (Figure 2i) (Syunyakov & Neznamov, 2016), and 2‐MBI oxadiazoles as antidiabetic agents (Figure 2j) (Aboul‐Enein & El Rashedy, 2015).…”