Effect of some arylguanidino- and arylaminopyrimidines on the growth of certain microorganisms
TL;DR: 2,4-Bis(arylamino)-6-hydroxypyrimidines have been found to be the most active of the series and their inhibitory activity seems to be partially due to their interference with the pyrimidine metabolism of the microorganisms.
About: This article is published in Archives of Biochemistry and Biophysics.The article was published on 1961-02-01. It has received 8 citations till now.
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TL;DR: Pyrimidine derivatives have been found to possess fungicidal, antibacterial, antimitotic, antithyroid and surface-anaesthesia activities, with the exception of pyrimidine antibiotics.
Abstract: Publisher Summary The beginning of pyrimidine chemistry may be traced back to the isolation of alloxan, a pyrimidine derivative. The synthesis of barbituric acid from urea and malonic acid perhaps marked the next major event in the development. Since then pyrimidines have occupied a unique and important place in the fields of biological and medicinal chemistry. It is well known that uracil, thymine, and cytosine are essential constituents in nucleic acids; thiamine that possesses antiberiberi activity was the first vitamin discovered in the B series; barbiturates are widely used as sedatives; pyrimethamine is highly potent against erythrocytic parasites in antimalarial study; aminometradine (Mictine) is an orally effective diuretic; and the 5-halogen-substituted uracils and derivatives have recently been reported as antitumour or antiviral agents, or both. Other pyrimidine derivatives have been found to possess fungicidal, antibacterial, antimitotic, antithyroid and surface-anaesthesia activities. With the exception of pyrimidine antibiotics, in this chapter, pyrimidines are classified based on special structural features and functional groups. The chapter discusses the following areas: 2,4- diaminopyrimidines, halogenated pyrimidines, sulphur-substituted pyrimidines, 2-substituted 4-amino-5-hydroxymethylpyrimidines, pyrimidine sulphonamides and pyrimidine antibiotics.
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TL;DR: A novel series of diarylpyrimidine analogues (DAPYs) featuring a naphthyl moiety at the C4 position were designed, with all compounds exhibiting strong activity against wild‐type HIV‐1.
Abstract: A novel series of diarylpyrimidine analogues (DAPYs) featuring a naphthyl moiety at the C4 position were designed, with all compounds exhibiting strong activity against wild-type HIV-1.A novel series of diarylpyrimidine analogues (DAPYs) featuring a naphthyl moiety at the C4 position were synthesized and evaluated for their in vitro activity against HIV in MT-4 cells. All compounds exhibited strong activity against wild-type HIV-1. The most active compound showed activity against wild-type HIV-1 with an EC(50) value of 2.35 nM and against the double mutant strain (K103N+Y181C) with an EC(50) value of 6.6 microM, with a selectivity index greater than 60 000 against wild-type HIV-1. Additionally, some compounds also showed activity against HIV-2 (EC(50)=5.82 microM).
47 citations
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TL;DR: Pyrimidines containing two ethylenimine functions have also been found to possess anticancer activity, and 2, 4-Bis (aziridinyl)-6-chloropyrimidine (CV, ethymidine, etimidin) significantly inhibits growth of many transplantable mouse and rat tumours.
Abstract: Publisher Summary This chapter lists some pyrimidines of biological and medicinal interest, including 5-hydroxypy rimidines, barbituric acid and its derivatives, aminohydroxypyrimidines, pyrimidine amino acids, and nitro and nitrosopyrimidines. The chapter also discusses pyrimidines containing biological alkylating functions. A large number of derivatives of the original nitrogen mustard and other biological akylating agents, such as ethylenimines and epoxides have been prepared as potential anticancer agents. The chapter further explains that the alkylating agents consist of a carrier and the alkylating group, and that differences in selectivity of action upon the tumour, or ability to reach the site of desired action, with minimum damage to the host, are dependent upon the carrier. The chapter also reviews that some pyrimidines containing two ethylenimine functions have also been found to possess anticancer activity. 2, 4-Bis (aziridinyl)-6-chloropyrimidine (CV, ethymidine, etimidin) significantly inhibits growth of many transplantable mouse and rat tumours.
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TL;DR: Investigation of the mechanism of the inhibitory action of the new N-pyrimidyl compounds in S. faecalis revealed that they acted primarily as folic acid antagonists in a manner consistent with an assumption that they interfere with the enzymatic conversion of folic Acid to 5 N-forrnyl tetrahydrofolic acid.
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References
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TL;DR: Evidence is presented that uracil deoxyriboside, which structurally is the simple demethylated form of thymidine, may indeed be the primary acceptor of the methyl group.
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