Design, Synthesis and Pharmacological Evaluation of New Nonsteroidal Anti-Inflammatory Derived from 3-Aminobenzothieno[2,3-<i>d</i>]pyrimidines

Abstract

During the last few years, condensed thienopyrimidine derivatives have received considerable attention. The therapeutic importance of thienopyrimidines prompted us to synthesize some of spiro(benzothieno[2,3-d]pyrimidine-4-one) derivatives. Some of the novel benzothino-pyrimidine derivatives 3a, 9b, 10b, 11a, 11b, and 11c showed considerable potent anti-inflammatory and analgesic activity of superior G.I.T. safety profile in experimental rats in comparing to indomethacin and tramadol as reference drugs.

Qsar Approach to Estimating the Analgesic Activity of a Series of Tri-Substituted Pyrimidine Derivatives

“…They possess several interesting biological properties such as antimycobacterial [23], cardioprotective [24], antimalarial [25], antiparasitic [26] and, of course, analgesic and anti-inflammatory properties [27][28][29][30][31]. Pyrimidine derivatives are thus synthesized and analyzed for their analgesic properties around the world [12,[27][28][29][30][31]. In the classical method, researchers use the SAR methodology (Relation Structure Activity) [32,33], in order to synthesize the molecules likely to have the best effect.…”

Synthesis and Structure Activity Relationship of Some Indole Derivatives as Potential Anti-inflammatory Agents

“…32 If the latter moiety is replaced with any other bulkier N-substituents, efficient binding to COX-1 pocket is prevented. 12,[82][83][84] Taking all this into consideration, and to analyze our SAR, two structural components were considered: the nature of the heterocycle nucleus and the character of the side chain (N-substitution). First, the influence of the nature of the aromatic heterocyclic system: fused pyrrole 1a, 1c, and 1d showed the highest activity over fused pyrrolopyrimidine 5b.…”

Therapeutic importance of synthetic thiophene

“…Hafez et al [37] synthesized some of the novel benzothino-pyrimidine derivatives (Scheme 21) which showed considerable potent anti-inflammatory activity. The anti-inflammatory activity of the newly synthesized compounds were evaluated by applying carrageenan-induced paw edema bioassay in rats using indomethacin as a reference standard.…”