Microwave-assisted synthesis of new benzimidazole derivatives with lipase inhibition activity
摘要:
A practical protocol has been used for the synthesis of benzimidazoles. The reaction of iminoester hydrochlorides of phenylacetic with 4,5-dichloro-1,2-phenylenediamine under microwave irradiation leads to the benzimidazole derivatives with good yields and in short reaction times. After the synthesis of benzimidazoles, we synthesized ester and hydrazide derivatives under microwave irradiation with good yields. All compounds were evaluated with regard to pancreatic lipase activity and 3b, 3c, 5a and 6a showed lipase inhibition at various concentrations.
This study presents a synthesis of new series of some benzimidazole, bisbenzimidazole and perimidine derivatives viamicrowavetechnique, which, leads to the good product yields and short reaction times. The structure of newly synthesized compounds was confirmed by 1H NMR and 13C NMR spectra. These compounds were screened for their lipase inhibition activity. Then, all compounds were evaluated with
By using the microwave technology, a new protocol has been developed for the synthesis of new coumarin derivatives including 1,2,4-triazol-3-one skeleton. This protocol proves to be efficient and environmentally friendly in terms of easy work-up and good yields. All newly synthesized compounds were screened for their antimicrobial activity and lipase inhibition. Most of the compounds were found to
通过使用微波技术,已经开发了用于合成包括1,2,4-三唑-3-酮骨架的新香豆素衍生物的新方案。从易于处理和高产量的角度来看,该协议被证明是高效且对环境友好的。筛选所有新合成的化合物的抗菌活性和脂肪酶抑制作用。发现大多数化合物对大肠杆菌有效。N '-[4-氨基-3-(2-溴苄基)-5-氧代-4,5-二氢-1 H -1,2,4-三唑-1-基]乙酰基} -6-溴-2 -oxo-2 H色烯-3-碳酰肼和N '-[4-氨基-3-(3,4-二氯苄基)-5-oxo-4,5-二氢-1 H -1,2,4-三唑-1-基]乙酰基} -6-溴-2-氧代-2 H-色烯-3-碳酰肼对脂肪酶的抑制作用良好。
Rapid and Efficient Synthesis of a New Series of 2-Aryl-5-Fluoro-6-(4-Phenylpiperazin-1-Yl)-1H-Benzimidazoles Using Microwave Heating
iminoester hydrochlorides. 4-Fluoro-5-(4-phenylpiperazin-1-yl)benzene-1,2-diamine was prepared from the reduction of 5-fluoro-2-nitro-4-(4-phenylpiperazin-1-yl)aniline by using Pd/C (10%) catalyst and hydrazine hydrate under microwave irradiation. The structures of newly synthesised compounds were identified by 1H NMR, 13C NMR, mass spectroscopy and elemental analysis data.
procedure is described for the synthesis of 2-substituted perimidines involving the reaction of 1,8-diaminonapthalene with iminoester hydrochlorides of substituted phenylacetic acids under microwave irradiation. This leads to good yields in short reaction times. The results were compared with those that used conventional heating. This new method may be preferable for the synthesis of perimidines.