Synthesis, analgesic and anti-inflammatory activities evaluation of some bi-, tri- and tetracyclic condensed pyrimidines

Design, synthesis and biological evaluation of novel condensed pyrrolo[1,2-c]pyrimidines featuring morpholine moiety as PI3Kα inhibitors

“…Reaction of 2-dicyanomethylidinopyrrolidine 1 with ethyl or phenyl isothiocyanates followed by sodium borohydride mediated reduction afforded the enaminonitrile derivatives 3a,b as reported [19,[22][23][24]. Acylation of the intermediates 3a,b with 3-or 4-anisoyl chloride followed by in situ intramolecular cyclization gave the tricyclic pyrimido [5,4-e]pyrrolo [1,2-c]pyrimidinones 4a-d. Chlorination of the latter, using excess POCl 3 was achieved only upon using drops of dimethylformamide (DMF) to yield the chlorointermediates 5a-d.…”

Design, synthesis, and pharmacological studies of some new Mannich bases and S-alkylated analogs of pyrazole integrated 1,3,4-oxadiazole

“…Such enhanced activity of halo substituents might be due to the ability of the halogen to act as polar hydrogen or hydroxyl mimic [35]. The antiinflammatory inhibition value for the ester analogue of S-alkylated product (6b) was greater than that for methyl (6a) analogue, indicating that functionality in the side chain increased the activity [36]. In the S-alkylated acetamide series 7a-f, the products containing 3-chloro-4-fluoro (7b), o-trifluoromethyl (7c), and m-trifluoromethyl (7d) phenyl substituent showed better activity than the other compounds.…”

Synthesis, anti-inflammatory and ulcerogenicity studies of some substituted pyrimido[1,6-a]azepine derivatives

“…In the course of a research devoted to the development of new classes of anti-inflammatory drugs, several condensed pyrimidine derivatives have been synthesized and have shown potential anti-inflammatory activity with good gastrointestinal safety [11,12]. These are exemplified by the pyrimido[1,6-a]azepine compounds I and II which are few of many other structurally related derivatives ( Fig.…”