Design, Synthesis, and Thrombin Inhibitory Activity Evaluation of Some Novel Benzimidazole Derivatives

2016 ◽  
Vol 99 (4) ◽  
pp. 325-332 ◽  
Author(s):  
Weixin Ren ◽  
Yujie Ren ◽  
Minghui Dong ◽  
Yonghong Gao
Keyword(s):  
Inhibitory Activity ◽  
Benzimidazole Derivatives ◽  
Design Synthesis ◽  
Activity Evaluation

Design, synthesis, α-glucosidase inhibitory activity, molecular docking and QSAR studies of benzimidazole derivatives

2016 ◽  
Vol 1114 ◽  
pp. 84-94 ◽  
Author(s):  
Leila Dinparast ◽  
Hassan Valizadeh ◽  
Mir Babak Bahadori ◽  
Somaieh Soltani ◽  
Behvar Asghari ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Benzimidazole Derivatives ◽  
Design Synthesis ◽  
Qsar Studies

Design, synthesis, docking study and urease inhibitory activity evaluation of novel 2-((5-amino-1,3,4-thiadiazol-2-yl)thio)-N-arylacetamide derivatives

2021 ◽  
Vol 30 (3) ◽  
pp. 729-742
Author(s):  
Mohammad Nazari Montazer ◽  
Mehdi Asadi ◽  
Saeed Bahadorikhalili ◽  
Faezeh Sadat Hosseini ◽  
Arash Amanlou ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Docking Study ◽  
Design Synthesis ◽  
Activity Evaluation ◽  
Urease Inhibitory

Design, Synthesis, Molecular Docking and Biological Evaluation of 1-(benzo[d]thiazol-2-ylamino)(phenyl)methyl)naphthalen-2-ol Derivatives as Antiproliferative Agents

2019 ◽  
Vol 16 (10) ◽  
pp. 837-845
Author(s):  
Sandhya Jonnala ◽  
Bhaskar Nameta ◽  
Murthy Chavali ◽  
Rajashaker Bantu ◽  
Pallavi Choudante ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Inhibitory Activity ◽  
Chinese Hamster Ovary Cells ◽  
Chinese Hamster ◽  
Mouse Skin ◽  
Coupling Reaction ◽  
Binding Mode ◽  
Biological Evaluation ◽  
Design Synthesis

A class of 1-((benzo[d]thiazol-2-ylamino)(phenyl)methyl)naphthalen-2-ol derivatives (4a-t) has been synthesized in good yields through a three component coupling reaction. The newly synthesized compounds were evaluated for their in vitro antiproliferative activity against five cell lines such as DU145 (human prostate cancer), MDA-MB-B231 (human breast cancer), SKOV3 (human ovarian cancer), B16-F10 (mouse skin melanoma) and CHO-K1 (Chinese hamster ovary cells), a noncancerous cell line. In vitro inhibitory activity indicates that compounds 4a, 4b, 4c, 4d, 4g, 4j, and 4o exhibited potent anti-proliferative behavior. Among them, compounds 4g, 4j and 4o found to be the most active members exhibiting remarkable growth inhibitory activity. Molecular docking facilitates to investigate the probable binding mode and key active site interactions in tubulins α and β proteins. The docking results are complementary to experimental results.

Phenanthridine Sulfonamide Derivatives as Potential DPP-IV Inhibitors: Design, Synthesis and Biological Evaluation

2020 ◽  
Vol 16 ◽  
Author(s):  
Reema Abu Khalaf ◽  
Shorooq Alqazaqi ◽  
Maram Aburezeq ◽  
Dima Sabbah ◽  
Ghadeer Albadawi ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Ligand Docking ◽  
Biological Assessment ◽  
Hypoglycemic Agents ◽  
Binding Affinities ◽  
Oral Hypoglycemic Agents ◽  
Design Synthesis ◽  
Dpp Iv

Background: Diabetes mellitus is a chronic metabolic disorder, characterized by hyperglycemia over a prolonged period, disturbance of fat, protein and carbohydrate metabolism, resulting from defective insulin secretion, insulin action or both. Dipeptidyl peptidase-IV (DPP-IV) inhibitors are relatively a new class of oral hypoglycemic agents that reduces the deterioration of gut-derived endogenous incretin hormones that are secreted in response to food ingestion to stimulate the secretion of insulin from beta cells of pancreas. Objective: In this study, synthesis, characterization, and biological assessment of twelve novel phenanthridine sulfonamide derivatives 3a-3l as potential DPP-IV inhibitors was carried out. The target compounds were docked to study the molecular interactions and binding affinities against DPP-IV enzyme. Methods: The synthesized molecules were characterized using 1H-NMR, 13C-NMR, IR, and MS. Quantum-polarized ligand docking (QPLD) was also performed. Results: In vitro biological evaluation of compounds 3a-3l reveals comparable DPP-IV inhibitory activities ranging from 10%-46% at 100 µM concentration, where compound 3d harboring ortho-fluoro moiety exhibited the highest inhibitory activity. QPLD study shows that compounds 3a-3l accommodate DPP-IV binding site and form H-bonding with the R125, E205, E206, S209, F357, R358, K554, W629, S630, Y631, Y662, R669 and Y752 backbones. Conclusion: In conclusion, phenanthridine sulfonamides could serve as potential DPP-IV inhibitors that require further structural optimization in order to enhance their inhibitory activity.

scholarly journals Design, Synthesis and Biological Screening of New Benzimidazole Derivatives

2021 ◽  
Vol 1879 (2) ◽  
pp. 022056
Author(s):  
Ali Mohammed Sabur ◽  
Muayad Ahmed Rdaiaan
Keyword(s):  
Benzimidazole Derivatives ◽  
Biological Screening ◽  
Design Synthesis

Design, synthesis, and antitumor activity evaluation of steroidal oximes

2021 ◽  
pp. 116360
Author(s):  
Ana R. Gomes ◽  
Ana S. Pires ◽  
Ana M. Abrantes ◽  
Ana C. Gonçalves ◽  
Saul C. Costa ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Design Synthesis ◽  
Activity Evaluation
Sign in / Sign up

Export Citation Format

Share Document