Antiinflammatory, Analgesic and Antiamoebic Activity Evaluation of Pyrimido[1,6-a]benzimidazole Derivatives Synthesized by the Reaction of Ketoisothiocyanates with Mono and Diamines
| Autor: | Amir Azam, Neelam Bharti, Shefali Rajvanshi, Sham M. Sondhi, Monika Johar, Ashok K. Singh |
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| Rok vydání: | 2003 |
| Předmět: |
Benzimidazole
Magnetic Resonance Spectroscopy medicine.drug_class Pyridines Analgesic Carrageenan Chemical synthesis Anti-inflammatory Inhibitory Concentration 50 Mice Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Inhibitory concentration 50 Structure–activity relationship Organic chemistry Animals Edema Amebicides Pain Measurement Pharmacology Analgesics Organic Chemistry Anti-Inflammatory Agents Non-Steroidal Entamoeba histolytica Nuclear magnetic resonance spectroscopy General Medicine Combinatorial chemistry Rats chemistry Benzimidazoles Nuclear chemistry |
| Zdroj: | ChemInform. 34 |
| ISSN: | 1522-2667 0931-7597 |
| DOI: | 10.1002/chin.200313035 |
| Popis: | (UN) substituted o-phenylenediamines 1a-g reacted with 3-isothiocyanatobutanal to give pyrimidobenzimidazole derivatives, 2a-g, respectively. Products 4, 6 and 8, 10 were obtained by condensation of 3-isothiocyanatobutanal with 2,3-diaminopyridine, 1,4-diaminobutane and 3-isothiocyanatopropanal with 4,5-dimethyl-1,2-phenylenediamine, o-nitroaniline, respectively. S-Methylation of 2f and 11b gave products 12a and 12b, respectively. Anti-inflammatory and analgesic activity evaluations of 2a-g and 12b were carried out at 50 mg kg(-1) p.o. Compound 2c exhibited good anti-inflammatory (46%) and mild analgesic activity (50%). Antiamoebic activity evaluations (using microdilution method) of 2a-g against Entamoeba-histolytica (strain HM1: IMSS) were carried out and compounds 2a, 2b, 2d and 2g exhibited good antiamoebic activity in vitro. |
| Databáze: | OpenAIRE |
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