Conventional and microwave assisted synthesis of small molecule based biologically active heterocyclic amidine derivatives.
Heterocyclic amidine derivatives have been synthesized by condensation of 2-cyanopyrazine, 4-cyanopyridine and 2-cyanopyridine with furfurylamine, histamine, 1-(3-aminopropyl)imidazole, 4-picolylamine, 2-picolylamine, and tryptamine respectively, in the presence of sodium methoxide as well as via microwave irradiation in good yields. All these compounds were screened for anti-inflammatory and anticancer activities. At a dose of 50mg/kg p.o. compounds 3a (36.6%), 3d (32%), 4d (31.0%) and 4e (33.8%) exhibited good anti-inflammatory activity, comparable to standard drug ibuprofen which showed 39% activity at 50mg/kg p.o.
Sondhi
Sham M
SM
Department of Chemistry, Indian Institute of Technology-Roorkee, Roorkee 247667 Uttaranchal, India.
Rani
Reshma
R
Roy
Partha
P
Agrawal
S K
SK
Saxena
A K
AK
D000578:Amidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D006571:Heterocyclic Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007052:Ibuprofen / Q000494:pharmacology; D008872:Microwaves; D015394:Molecular Structure
D000578:Amidines; D000893:Anti-Inflammatory Agents; D000970:Antineoplastic Agents; D006571:Heterocyclic Compounds; D007052:Ibuprofen