1188164-01-3

Upstream product

• 100880-52-2 methyl 4‐(1H‐benzo[d]imidazol‐2‐yl)benzoate 
• 906816-18-0 ethyl 4-(1H-benzo[d]imidazol-2-yl)benzoate 
• 1571-08-0 methyl 4-formylbenzoate 
• 95-54-5 1,2-diamino-benzene 

Downstream Products

• 1237050-31-5 C₂₂H₁₅F₃N₄O 
• 1237050-24-6 C₂₂H₁₈N₄O 
• 1237050-22-4 C₂₁H₁₅FN₄O 
• 1237050-16-6 C₂₁H₁₅ClN₄O 
• 1237050-29-1 C₂₁H₁₅N₅O₃ 
• 1237050-10-0 C₂₁H₁₆N₄O 
• 303205-18-7 C₂₁H₁₆N₄O₂ 
• 1237050-28-0 C₂₂H₁₈N₄O₂ 
• 1237050-32-6 C₂₂H₁₆N₄O₃ 
• 1237050-20-2 C₂₁H₁₅BrN₄O 
• 1237050-35-9 C₂₂H₁₅N₅O 
• 1237050-15-5 C₂₃H₂₁N₅O 

Relevant academic research and scientific papers

New Benzimidazole-1,2,4-Triazole Hybrid Compounds: Synthesis, Anticandidal Activity and Cytotoxicity Evaluation

Owing to the growing need for antifungal agents, we synthesized a new series 2-((5-(4-(5-substituted-1H-benzimidazol-2-yl)phenyl)-4-substituted-4H-1,2,4-triazol-3-yl)thio)-1-(substituted phenyl)ethan-1-one derivatives, which were tested against Candida species. The synthesized compounds were characterized and elucidated by FT-IR 1H-NMR 13C-NMR and HR-MS spectroscopies. The synthesized compounds were screened in vitro anticandidal activity against Candida species by broth microdiluation methods. In vitro cytotoxic effects of the final compounds were determined by MTT assay. Microbiological studies revealed that compounds 5m 5o 5r 5t 5y 5ab and 5ad possess a good antifungal profile. Compounds 5w was the most active derivative and showed comparable antifungal activity to those of reference drugs ketoconazole and fluconazole. Cytotoxicity evaluation of compounds 5m 5o 5r 5w 5y 5ab and 5ad showed that compounds 5w and 5ad were the least cytotoxic agents. Effects of these two compounds against ergosterol biosynthesis were observed by LC-MS-MS method which is based on quantification of ergosterol level in C. albicans. Compounds 5w and 5d inhibited ergosterol biosynthesis concentration dependently. A fluorescence microscopy study was performed to visualize effect of compound 5w against C. albicans at cellular level. It was determined that compound 5w has a membrane damaging effect which may be related with inhibition of biosynthesis of ergosterol.

Synthesis, spectral characterization, thermal study and antimicrobial activity of (E)-4-(substituted 1-Benzo[d]imidazole-2-yl)-N'-(substituted Benzylidene)benzohydrazide schiff bases

Antimicrobial properties casing wide applicability in water detoxification, pharmaceutics and in industries. Present work focus on the synthesis of a new series of Schiff Bases (E)-4-(1 substituted-1H Benzo[d]imidazole-2-yl)-N'-(substituted Benzylidene)benzohydrazide (5a-5l) were synthesized. The convenient route for the synthesis of new analogues by the condensation of 4-(substituted -1H-Benzo[d]imidazole-2-yl)-N'- Hydrazine with different derivatives of aromatic aldehydes were described using different solvents and catalysts. The structures of the synthesized compounds were ascertain by spectral techniques viz. IR, 1H NMR, MS and Physical Elemental data. Compounds were also subjected to thermal analysis to study their physical and chemical properties. The title compounds were also screened for their antimicrobial activity against various bacterial & Fungal strains. Results of bioassay vary with diverse group attached to Benzimdazole motif and could be helpful for the development of other bioactive molecules.

Synthesis, docking studies and biological activity of new benzimidazole- Triazolothiadiazine derivatives as aromatase inhibitor

In the last step of estrogen biosynthesis, aromatase enzyme catalyzes the conversion of androgens to estrogens. Aromatase inhibition is an important way to control estrogen-related diseases and estrogen levels. In this study, sixteen of benzimidazole-triazolothiadiazine derivatives have been synthesized and studied as potent aromatase inhibitors. First, these compounds were tested for their anti-cancer properties against human breast cancer cell line (MCF-7). The most active compounds 5c, 5e, 5k, and 5m on MCF-7 cell line were subject to further in vitro aromatase enzyme inhibition assays to determine the possible mechanisms of action underlying their activity. Compound 5e showed slight less potent aromatase inhibitory activity than that of letrozole with IC50 = 0.032 ± 0.042 μM, compared to IC50 = 0.024 ± 0.001 μM for letrozole. Furthermore, compound 5e and reference drug letrozole were docked into human placental aromatase enzyme to predict their possible binding modes with the enzyme. Finally, ADME parameters (absorption, distribution, metabolism, and excretion) of synthesized compounds (5a–5p) were calculated by QikProp 4.8 software.

Synthesis of novel benzimidazole–oxadiazole derivatives as potent anticancer activity

DNA topoisomerase I regulates DNA topological structure in many cellular metabolic processes and is a validated target for the development of antitumor agents. In this work, a series of novel 2-[(5-(4-(5(6)-substituted-1H-benzimidazol-2-yl)phenyl)-1,3,4-oxadiazol-2-yl)thio]-1-(4-substitutedphenyl)ethan-1-ones (4a–4s) derivatives have been synthesized and evaluated for DNA Topo I inhibition and cytotoxicity. The structures of the compounds (4a–4s) were confirmed by IR, 1H-NMR, 13C-NMR, 2D NMR, and mass spectroscopy. Anticancer activity of these compounds was assessed against two different human cancer cell lines A549 (human lung adenocarcinoma) and HepG2 (human liver cancer cell line), as well as normal mouse embryonic fibroblast cells (NIH3T3). IC50 values of compounds 4a, 4c, and 4f were highest than those exhibited for the reference drug cisplatin. Then, the inhibitory effect of 4a, 4c, and 4f compounds on topoisomerase I enzyme with the relaxation assay was investigated on supercoiled DNA using agarose gel electrophoresis. The Annexin V-FITC assay demonstrated that these compounds induce cell death by apoptosis.

Antimicrobial activity and a SAR study of some novel benzimidazole derivatives bearing hydrazone moiety

In this study 12 novel benzimidazole compounds bearing hydrazone moiety were synthesized in order to investigate their possible antibacterial and antifungal activity. Structures of the synthesized compounds were elucidated by spectral data. Six different gram-negative and four different gram-positive bacterial strains were used in antibacterial activity tests. Antifungal activity tests were also performed against three different fungal strains. Most of the test compounds found to be significantly effective against Proteus vulgaris,Staphylococcus typhimurium,Klebsiella pneumoniae and Pseudomonas aeruginosa gram-negative bacterial strains. A structureeactivity relationship (SAR) study including some electronic parameters was carried out and a connection between antibacterial activity and electronic properties of the target compounds was determined. Toxicity of the most effective compounds was established by performing BrineeShrimp lethality assay.