ABSTRACT
Certain isothiazole [4,3-d] pyrimidine diones [IV, V, VIa-i and IX] were prepared via condensation of 4-amino-3-carbamoyl-5-carbethoxyisothiazole [III] with phenyl isocyanate and ethyl chloroformate. A suggested mechanism of formation and investigation of the reaction products of [III] with phenyl isocyanate were given. The results of the preliminary antimicrobial screening for some of the prepared pyrimidine diones, in addition to that of certain isothiazolopyrimidine diones reported in previous communications were shown
ABSTRACT
The synthesis of certain Mannich bases of 2-, 4-amino, and 2, 4-diamino-6-methylpyrimidines and their antimicrobial and antileukemic activities are described. Likewise, application of the Mannich conditions to 2-amino-4-[p-hydroxyanilino]-, 4-amino-2-[p- hydroxyanilino]-, and 2-amino-4-[p-acetylanilino]-6-methylprimidines using piperazine as the secondary amine afforded the corresponding bis-Mannich bases
Subject(s)
Anti-Bacterial Agents , Leukemia/therapyABSTRACT
A novel series of the title compounds have been synthesized for studying their antimicrobial activity. Most of them exhibited interesting antibacterial activity. Compound [III showed impressive in-vitro activity against all tested organisms
Subject(s)
AntibiosisABSTRACT
Several hydantoin and 2-thio analog derivatives have been prepared. Condensation of 3-methyl-2,4imidazolidine-dione [IA] with aromatic aldehydes afforded the corresponding arylidene derivatives. Coupling of 3-methyl-2-thioxo-4- imidazolidinone [IB] with diazonium salts yielded the expected 5-aryl- hydrazone derivatives. In addition, Mannich reaction of [IB] with formaldehyde and certain secondary amines gave the desired products. However, attempts to condense [IA] with formaldehyde and secondary amines under the Mannich conditions were abortive and the same hydantoin also failed to couple with aryl diazonium salts. Five compounds have been screened against selected bacteria and some of them were found to possess moderate to fairly good antibacterial activity
Subject(s)
AntibiosisABSTRACT
The reaction of 2-amino-4-chloro-, 4-amino-2-chloro-, and 2,4- dichloro-6-methyl-pyrimidines with primary aromatic amines under acidic conditions is presented. 2-, and 4-w substituted thio- ureide-6- methylpyrimidines were synthesized via the reaction of 2-amino-,and 4- amino-6-methylpyrimidine derivatives with aryl- isothiocyanates: Six compounds were evaluated for their antimicrobial activity and most of them showed a moderate activity against B subtilis, E. coli, and A. Niger