Pharmacokinetic optimization of 4-substituted methoxybenzoyl-aryl-thiazole and 2-aryl-4-benzoyl-imidazole for improving oral bioavailability.

Pharmacokinetic Optimization of 4-Substituted Methoxybenzoyl-Aryl-Thiazole (SMART) and 2-Aryl-4-Benzoyl-Imidazole (ABI) for Improving Oral Bioavailability

Biological activity of 4-substituted methoxybenzoyl-aryl-thiazole: an active microtubule inhibitor.

Formation of microtubules is a dynamic process that involves polymerization and depolymerization of αβ-tubulin heterodimers. Drugs that enhance or inhibit tubulin polymerization can destroy this dynamic process, arresting cells in the G(2)/M phase of the cell cycle. Although drugs that target tubulin generally demonstrate cytotoxic potency in the subnanomolar range, resistance due to drug efflu...

Nano TiO2@SiO2 as an efficient and reusable catalyst for the synthesis of multi-substituted imidazoles

Nano TiO2 supported on SiO2 (Nano TiO2@SiO2) as a solid Lewis acid, was described to be an effective and reusable catalyst for one-pot three-component reaction of benzil, aryl aldehydes and ammonium acetate for the synthesis 2-aryl-4,5-diphenyl-1H-imdazoles synthesis. To explore the high efficacy of the catalytic system the four-component cyclization of benzil, aryl aldehydes, ammonium acetate ...

Mg-Al Hydrotalcite Catalyzed Efficient One-Pot Synthesis of 4-H-Benzo[b]Pyrans, 2-Aryl Benzimidazole and 2-Aryl-4,5-Dihydro-1H- Imidazole Derivatives

An environment friendly synthesis of 2-amino-3-cyano-4-aryl-7,7-dimethyl-5-oxo-4H-5,6,7,8-tetrahydrobenzo[b]pyran, 2aryl benzimidazole and 2-aryl-4, 5-dihydro-1H-imidazole derivatives using Mg-Al hydrotalcite as an efficient catalyst has been developed. The excellent efficiency of the catalyst can be attributed to its Lewis acidic sites which resulted in higher reaction yields for different sub...

Theoretical studies on corrosion inhibition of N-aroyl-N’-aryl thiourea derivatives using conceptual DFT approach

In this paper, quantum chemical parameters at density functional theory (DFT) B3LYP/6-31G** (d,p) level of theory were calculated for three organic corrosion inhibitors [N-benzoyl-N-(p-aminophenyl) thiourea, N-benzoyl-N-(thiazole) thiourea and N-acetyl-N-(dibenzyl) thiourea. The calculated molecular descriptors such as the HOMO, LUMO, dipole moment, chemical potential (μ), chemical hardness (ղ)...