High analgesic and anti-inflammatory in vivo activities of six new hybrids NSAIAs tetrahydropyran derivatives

Synthesis and Anticancer Activities of Novel Guanylhydrazone and Aminoguanidine Tetrahydropyran Derivatives

“…The oxidation of tetrahydropyran alcohols to the corresponding ketones 8a-c (step iii, Scheme 1) was performed in high yields by using PCC in dichloromethane as a solvent (95%-98% yields). The guanylhydrazone 2-4 ( Figure 1) were prepared in quantitative yields (100% yields) by reacting ketones 8a-c with aminoguanidine hydrochloride and ethanol as a solvent (no catalysts were used) promoted by 5 min of microwave In connection to our interest in the stereoselective synthesis of tetraydropyran derivatives using the Prins cyclization reaction [14][15][16][17][18], and considering that guanylhydrazone [19] and aminoguanidine groups [20,21] potentiate the anticancer activity of some drugs, and these nitrogenated bases could be considered pharmacophoric points, we present in this article the syntheses of six novel tetrahydropyranyl guanylhydrazone and aminoguanidine 2-7 ( Figure 2). That way, we performed in vitro evaluation for anticancer activity against cancer cell lines, such as the chronic myeloid leukemia (K562), human acute myeloid leukemia (HL-60), human breast adenocarcinoma (MCF-7), human colon adenocarcinoma (HT-29), and L929 (murine fibroblast) and the human peripheral blood of patients with chronic myeloid leukemia (PBMC/CML) cells.…”

Design and Synthesis of Benzimidazole Analogs Endowed with Oxadiazole as Selective COX‐2 Inhibitor

“…In order to make high potency drug molecules, one of the strategies would be to combine two bioactive molecules belonging to a particular therapeutic category. This approach is gaining importance in therapeutic categories such as cytotoxicity and anti-inflammatory areas [21][22][23]. Recent trends in medicinal chemistry showed the popularity of molecular hybridization for drug design and development, which is based on combination of pharmacophoric moieties of different bioactive substances to make a new hybrid molecule with improved affinity and efficacy, as compared to parent drug [24][25][26].…”

Multicomponent Reactions of Acetoacetanilide Derivatives with Aromatic Aldehydes and Cyanomethylene Reagents to Produce 4<i>H</i>-Pyran and 1,4-Dihydropyridine Derivatives with Antitumor Activities

“…several starting materials combine in one reaction to form the product; they exhibit a very high bond-forming-index (BFI), e.g. several non-hydrogen atom bonds are formed in one synthetic transformation.2,3) Therefore MCRs are often a useful alternative to sequential multistep synthesis.In view of the increasing interest in the preparation of a large variety of heterocyclic compound libraries, the development of new synthetically valuable MCRs with several diversity points remains a challenge for both academic and industrial institutions.4) 4H-Pyran and its derivatives are an important class of heterocyclic compounds possessing broad biological activities, such as anti-inflammatory, 5) analgesic, 6) antioxidant,antiamoebic 11) and oral analgesic. 12) From the aforementioned reports, it seemed that the development of an efficient, rapid, and clean synthetic route towards focused libraries of such compounds is of great importance to both medicinal and synthetic chemists.…”

“…4) 4H-Pyran and its derivatives are an important class of heterocyclic compounds possessing broad biological activities, such as anti-inflammatory, 5) analgesic, 6) antioxidant,…”

“…4) 4H-Pyran and its derivatives are an important class of heterocyclic compounds possessing broad biological activities, such as anti-inflammatory, 5) analgesic, 6) antioxidant, 7) antitubercular, 8) antidepressant, 9) sedative, 10) antiamoebic 11) and oral analgesic. 12) From the aforementioned reports, it seemed that the development of an efficient, rapid, and clean synthetic route towards focused libraries of such compounds is of great importance to both medicinal and synthetic chemists.…”