30065-27-1Relevant academic research and scientific papers
Synthesis of Some Novel Benzimidazole Derivatives as Anticancer Agent and Evaluation for CDK2 Inhibition Activity
El-Hameed, Rania Helmy Abd,Fatahala, Samar Said,Sayed, Amira Ibrahim
, p. 238 - 248 (2022/02/10)
Background: Thiobezimidazoles reveal various pharmacological activities due to similarities with many natural and synthetic molecules; they can easily interact with biomolecules of living systems. Objective: A series of substituted 2-thiobezimidazoles have been synthesized. Twelve final compounds were screened for in vitro anti-cancer activities against sixty different cell lines. Methods: The spectral data of the synthesized compounds were characterized. A docking study for active anticancer compounds and CDK2/CyclinA2 Kinase assay against standard reference; Imatinib, were performed. Results: Two compounds (3c&3l) from the examined series revealed effective antitumor activity in vitro against two-cancer cell lines (Colon Cancer (HCT-116) and Renal Cancer (TK-10). The docking study of synthesized molecules discovered a requisite binding pose in the CDK-ATP binding pocket .3c &3l were promoted in the CDK2/CyclinA2 Kinase assay against standard reference Imatinib. Conclusion: Against all tested compounds; two compounds 3c &3l were found active against two types of cell-lines.
Synthesis of novel benzazole derivatives and evaluation of their antidepressant-like activities with possible underlying mechanisms
Tokg?z, Gamze,?zkay, ümide Demir,Osmaniye, Derya,Yücel, Nazl? Turan,Can, ?zgür Devrim,Kaplanc?kl?, Zafer As?m
, (2018/11/24)
Novel benzazole derivative compounds 4a–4h were obtained by the reaction of corresponding 2-(benzazol-2-ylthio)acetohydrazide and appropriate 4-substituted benzaldehydes. The chemical structures of the synthesized compounds were elucidated by FT-IR, 1H-NMR, 13C-NMR and LCMS spectroscopic methods. Antidepressant-like effects of the compounds were evaluated by tail suspension test (TST) and modified forced swimming tests (MFST). Moreover, locomotor activities of the animals were assessed by an activity cage apparatus. In the series, compounds 4a, 4b, 4e and 4f (at 50 mg/kg) significantly decreased the immobility time of mice in both of the TST and MFST. The same compounds prolonged the swimming time of animals in MFST without any change in the climbing duration. These data indicated that compounds 4a, 4b, 4e and 4f possess significant antidepressant-like activities. Moreover, pre-treatments with p-chloro-phenylalanine methyl ester (an inhibitor of serotonin synthesis), NAN-190 (a 5-HT1A antagonist), ketanserin (a 5-HT2A/2C antagonist), and ondansetron (a 5-HT3 antagonist) reversed the exhibited pharmacological effects. Results of the mechanistic studies suggested the involvement of serotonergic system and contributions of 5-HT1A, 5-HT2A/2C and 5-HT3 receptors to the antidepressant-like effects of compounds 4a, 4b, 4e and 4f. Furthermore, unchanged locomotor activity of mice following the administrations of these four derivatives confirmed that the presented antidepressant-like effects are specific.
Synthesis of some new nucleosides derived from 2-mercapto benzimidazole with expected biological activity
Amer, Hamada H.,Ali, Omar M.,El-Kafaween, Ibrahim Kh.
, p. 2303 - 2310 (2017/11/15)
2-mercaptobenzimidazole derivatives and their acyclic nucleosides were synthesized. The synthesized compounds were tested for their antibacterial activity against Escherichia coli, Staphylococcus aureus and S. epidermidis. Most of tested compounds showed
Anthelmintic evaluation of some novel synthesized 1,2,4-triazole moiety clubbed with benzimidazole ring
Kumar, P. Sudhir,Sahoo
, p. 211 - 217 (2014/06/23)
A series of N-[3-{(1H-benzo[d]imidazol-2-ylthio) methyl}-5-mercapto-4H-1,2, 4-triazol-4-yl]-2-substituted phenoxy acetamide 6(a-g) were synthesized by the mixture of the compound of potassium 2-(2-(1H-benzo[d]imidazol-2-ylthio) acetyl) hydrazinecarbodithioate (4) and arytoxy acid hydrazide (5) in presence of hydrochloric acid. The predicted structures of the synthesized compounds were confirmed by different spectral analysis studies. The title compounds 6(a-g) were screened for anthelmintic activity against Pheretima posthumous. The entire compounds were exhibited good anthelmintic activity when compared with standard drugs such as Albendazole and Piperazine.
Synthesis and pharmacological evaluation of some novel 2-mercapto benzimidazole derivatives
Nevade, Sidram A.,Lokapure, Sachin G.,Kalyane, Navanath V.
, p. 755 - 760 (2014/02/14)
The present study is synthesis of derivatives of N′-(4-amino-5- sulfanyl-4H-1, 2, 4-triazole-3-yl)-2-(1H-benzimi-dazole-2-ylsulfanyl) acetohydrazide (IV). Antibacterial activity tested against the E. coli and A. Substilis. Biological activities conducted
Synthesis of 2-mercaptobenzimidazole derivatives as potential anti-microbial and cytotoxic agents
Hosamani, Kallappa M.,Shingalapur, Ramya V.
, p. 311 - 319 (2011/11/05)
A series of novel 2-(1H-benzimidazol-2-ylsulfanyl)-N-(4-oxo-2-phenyl- thiazolidin-3yl)-acetamide 5a-j have been synthesized from various aldehydes and 2-(5-phenyl-[1,3,4]-oxadiazol-2-ylmethylsulfanyl)-1H-benzimidazole 6a-j from various benzoic acids. Thes
Derivatives of benzimidazole pharmacophore: Synthesis, anticonvulsant, antidiabetic and DNA cleavage studies
Shingalapur, Ramya V.,Hosamani, Kallappa M.,Keri, Rangappa S.,Hugar, Mallinath H.
experimental part, p. 1753 - 1759 (2010/06/17)
In seeking broad spectrum pharmacological activities of benzimidazole derivatives, a group of 4-thiazolidinones 5(a-j) and 1,3,4-oxadiazoles 6(a-j) containing 2-mercapto benzimidazole moiety were synthesized and screened for in vivo anticonvulsant activit
Synthesis, spectral and thermal studies of tin(IV) complexes using 2-benzimidazolylmercaptoaceto hydrazone type of ligands
Naik,Patil,Tallur,Mallur
experimental part, p. 22 - 25 (2009/04/06)
The metal complexes of SnIV with 2-benzimidazolylmercaptoaceto hydrazones of 1:2 metal to ligand stoichiometry have been synthesized. Molar conductance data reveal their non-electrolytic nature. The spectral studies show that the ligands react
Synthesis, spectroscopic and thermal studies of bivalent transition metal complexes with the hydrazone derived from 2-benzimidazblyl mercaptoaceto hydrazide and o-hydroxy aromatic aldehyde
Naik,Sambrani,Mallur
experimental part, p. 1793 - 1797 (2009/07/25)
Syntheses of complexes of a few first transition series bivalent metal ions like Co(II), Ni(II) and Cu(II) complexes with 2-benzimidazolyl mercaptoaceto hydrazone have been reported. The complexes have been characterized on the basis of analytical, molar
Green route for the heterocyclization of 2-mercaptobenzimidazole into β-lactum segment derivatives containing -CONH- bridge with benzimidazole: Screening in vitro antimicrobial activity with various microorganisms
Desai, Krunal G.,Desai, Kishor R.
, p. 8271 - 8279 (2007/10/03)
The efficient and rapid synthesis of novel azetidin-2-ones 4a-j has been established. Thus, both microwave and conventional condensation 2-{(1H-benzimidazol)-ylthio}-N′-2-(substituted phenyl) hydrazide with chloroacetylchloride were carried out in DMF-ben
