1. Synthesis of novel phosphorylated guanidine derivatives from cyanamide and their anti-inflammatory activity.
- Author
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Katla VR, Syed R, Kuruva CS, Kuntrapakam HK, and Chamarthi NR
- Subjects
- Animals, Anti-Inflammatory Agents chemical synthesis, Carrageenan, Cyanamide chemistry, Edema chemically induced, Edema pathology, Erythrocyte Membrane drug effects, Guanidine chemical synthesis, Humans, Phosphorylation, Rats, Rats, Wistar, Anti-Inflammatory Agents chemistry, Anti-Inflammatory Agents therapeutic use, Edema drug therapy, Foot pathology, Guanidine analogs & derivatives, Guanidine therapeutic use
- Abstract
A series of novel guanidine derivatives were synthesized in three steps and their anti-inflammatory activities in vitro and in vivo evaluated. 2-Aminopyridin-3-ol (1) was reacted with thiophosphoryl chloride (2) to give a monochloride (3). It was further reacted with cyanamide to afford the corresponding cyanamine (4), which was subsequently reacted with different heterocyclic amines to form the title compounds (5a-l). The substituent in the guanidine function affected the potency of anti-inflammatory activity. The compounds having benzothiazole, fluorophenyl, and piperazinyl moieties enhanced the anti-inflammatory activity.
- Published
- 2013
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