Synthesis and antiplatelet aggregation activity evaluation of some 2-aminopyrimidine and 2-substituted-4,6-diaminopyrimidine derivatives

A series of novel 2-aminopyrimidine and 2-Substituted-4,6-diaminopyrimidine derivatives have been synthesized and their antiplatelet aggregation activities were assessed against ADP and arachidonic acid-induced platelet aggregation in human plasma using light transmission aggregometry. Among the tested derivatives, compounds Ia, I[b], I[B] and II[16] exhibited the highest antiplatelet aggregation activity [36.75, 72.4, 62.5 and 80 microM]. None of the compounds showed satisfactory activity against the aggregation induced by ADP but acceptable activities were observed against the aggregation induced by arachidonic acid. 2- aminopyrimidines were more active than 4,6- diaminopyrimidines in this respect

Synthesis and evaluation of new fluorinated anti-tubercular compounds

Treatment of tuberculosis [TB] and the discovery of effective new anti tubercular drugs is one of the most urgent priorities in health organizations all around the world. In the present study, fluorinated analogs of some of the most important anti-TB agents such as p-aminosalicylic acid [PAS], thiacetazone and pyrazinamide were synthesized and tested against TB. The fluorinated analog of thiacetazone was 20 times more potent than the parent compound against M.tuberculosis H37-RV, while the fluorinated PAS was almost three times less potent than PAS. A few other halogenated analogs of thioacetazone were also synthesized and subjected to anti-TB screening tests. The best halogen substituent was found to be fluorine which has the smallest size from one hand and the strongest electronegativity from the other hand among the halogen atoms. This fact reemphasizes the unique nature of fluorine as a golden substituent in medicinal chemistry