- 5,5-Disubstituted Hydantoins: Syntheses and Anti-HIV Activity
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A series of 5,5-disubstituted hydantoin derivatives was synthesized by alkylating 5,5-bis(mercaptomethyl)-2,4-imidazolidinedione (3) with various halomethylaromatic or halomethylheteroaromatic precursors, or by using the Buchener-Berg procedure on the required ketone.When evaluated for their ability to inhibit HIV-induced cell killing and virus production in CEM or MT-2 cells only compounds 2, 4n, 4o, and 4i demonstrated modest activity, the latter with an IC50 = 53 μM
- Comber, Robert N.,Reynolds, Robert C.,Friedrich, Joyce D.,Manguikian, Roupen A.,Buckheit, Robert W.,et al.
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p. 3567 - 3572
(2007/10/02)
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- Synthesis of Functionally Substituted α,β-Unsaturated Carbonyl Compounds
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Epichlorohydrin and glycidol are transformed in a four step sequence into β-dimethylamino-α-phenylthio-substituted α,β-unsaturated carbonyl compounds 5, possessing differently O-protected oxymethyl substituents at the carbonyl group.These compounds are of
- Apparao, Satyam,Schmidt, Richard R.
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p. 896 - 899
(2007/10/02)
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- Nitrogen- and sulfur-containing models for metallo-enzymes. Part I. Synthesis and physical studies of 2(2-pyridyl)-1,3-dithioalkyl-2-propanols, 2(2-pyridyl)- and 2(2-imidazolyl)-1,3-dimercapto-2-propanols
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Several compounds of the title class have been synthesized as small-molecule analogues for the metal-binding sites in such biochemical systems as ADH.The ligands containing pyridine and two thioethers do not bind divalent metals Co(2+), Zn(2+), Cu(2+), N
- Curtis, N. J.,Brown, R. S.
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- Hypocholesterolemic activity of 1,3 bis(substituted phenoxy) 2 propanones
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A series of 1,3 bis (substituted phenoxy) 2 propanones was found to be active hypocholesterolemic agents at 10 mg/kg/day. The p chloro and p methyl substituted phenoxy compounds possess the highest activity. These compounds did not possess the estrogenic and antifertility activities of the related previously reported derivatives of the bis (β phenylethyl) ketone series. The 1,3 bis (p methylphenoxy) 2 propanone (7) also lowered serum triglycerides and glycerol which appeared to be due to increased levels of serum lipase and reduced activity of liver lipase. There was reduced incorporation of free fatty acids into complex lipids by the liver. Cholesterol was excreted faster in the treated animals.
- Piantadosi,Hall,Wyrick,Ishaq
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p. 222 - 229
(2007/10/12)
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