Synthesis of some thiophene, imidazole and pyridine derivatives exhibiting good anti-inflammatory and analgesic activities.
A series of thiophene derivatives 1a-d & 2a-c were synthesized by condensation of 5-nitro-2-thiophene carboxaldehyde with mono and diamines respectively. Various imidazole derivatives 3a-c were obtained by condensing 4-(2-ethylamino)-1H-imidazole with 4-acetylpyridine, 2-acetylpyridine and 4-acetylbenzonitrile respectively. Pyridine derivatives 4a-e were synthesized by condensing 2-hydrazino-pyridine with various carbonyl compounds; 5a-c by condensing 2, 6-pyridine dicarbonyl dichloride with various aryl sulfonylhydrazides; 6, 7 by condensing 2, 6-dialdehyde pyridine with 2-hydrazinopyridine and anthranilonitrile respectively and compound 8 by condensing 2, 5-thiophene dialdehyde with hydrazinopyridine. All the compounds were characterized by IR, (1)HNMR, Mass spectra and elemental analysis. Compounds 1a-d; 2a-c; 3a-c; 4a-e; 5a-c, 6, 7 and 8 were screened for anti-inflammatory and analgesic activities. Compounds 1b and 2c exhibited good anti-inflammatory (26.5% and 33.4% at 50mg/kg p.o. respectively) and 3a, 3c good analgesic (100% and 75% at 100 mg/kg p.o. respectively) activities.
Sondhi
Sham M
SM
Department of Chemistry, Indian Institute of Technology Roorkee (IIT R), Roorkee-247667, UA, India. sondifcy@iitr.ernet.in
Jain
Shubhi
S
Dinodia
Monica
M
Kumar
Ashok
A
D018712:Analgesics, Non-Narcotic / Q000737:chemistry*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry*; D004353:Drug Evaluation, Preclinical; D006573:Heterocyclic Compounds, 1-Ring / Q000138:chemical synthesis* / Q000627:therapeutic use*; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000627:therapeutic use; D011725:Pyridines / Q000138:chemical synthesis / Q000627:therapeutic use; D013057:Spectrum Analysis; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000138:chemical synthesis / Q000627:therapeutic use
D018712:Analgesics, Non-Narcotic; D000894:Anti-Inflammatory Agents, Non-Steroidal; D006573:Heterocyclic Compounds, 1-Ring; D007093:Imidazoles; D011725:Pyridines; D013876:Thiophenes