R. Datema

In an effort to improve the gastrointestinal absorption of (R,S)-9-[4-hydroxy-2-(hydroxymethyl)butyl]guanine [(+/-)2HM-HBG], various salts and esters of the compound were synthesized and pharmacokinetic experiments were performed in rats and monkeys. The sodium or hydrochloride salts and short-chain esters of (+/-)2HM-HBG showed bioavailability characteristics that were equally as poor as those of (+/-)2HM-HBG. However, the esters given as salts tended to be better absorbed than the parent compound. The 6-deoxy and 6-deoxydiacetate analogs were extensively oxidized in vivo and represent prodrugs with considerable potential in improving the absorption of oral (+/-)2HM-HBG.

Hydroxymethyl

Hydrochloride

10.1128/aac.33.1.110

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Citations (9)

Didanosine

Antiviral chemistry & chemotherapy (1991)

C. McLaren R. Datema C A Knupp Robert A. Buroker

The evaluation and development of didanosine as a therapy for HIV-infection has demonstrated that results of cell-culture studies are only approximate predictors of clinical effects. Whereas the antiviral activity of didanosine is achieved in cell culture at concentrations much higher than those of zidovudine, the two drugs appear to achieve similar effects on markers of HIV-infection at similar clinical doses. The effect of the differing intracellular-half-life of the respective nucleoside triphosphates on the clinical effects is unknown. Similarly, preclinical toxicology studies, while suggesting a low potential for didanosine-induced haematological toxicities, did not predict the findings of peripheral neuropathy and pancreatitis in clinical studies. Thus, the results of controlled clinical studies are required in order to more fully define the therapeutic and safety profile of didanosine.

Didanosine

Zalcitabine

Nucleoside analogue

Stavudine

10.1177/095632029100200601

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Citations (23)

Inhibition of HIV-1 reverse transcriptase by 5′-triphosphates of 5-substituted uridine analogs

Antiviral Research (1989)

Pei‐Zhen Tao Nils Gunnar Johansson Göran Stening Bo Öberg R. Datema

Primer (cosmetics)

Reverse-transcriptase inhibitor

RNA-Directed DNA Polymerase

10.1016/0166-3542(89)90054-5

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Citations (5)

Inhibitors of protein glycosylation and glycoprotein processing in viral systems

Pharmacology & Therapeutics (1987)

R. Datema Sigvard Olofsson Pedro Romero

Membrane glycoproteins

10.1016/0163-7258(87)90066-0

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Citations (83)

MITOCHONDRIAL POLYSOMES FROM NEUROSPORA CRASSA

Elsevier eBooks (1974)

Etienne Agsteribbe R. Datema A.M. Kroon

Polysome

10.1016/b978-0-12-426750-3.50032-9

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Citations (5)

Asymmetric Synthesis of L-[3-11C]Alanine.

Acta chemica Scandinavica/Acta chemica Scandinavica. B, Organic chemistry and biochemistry/Acta chemica Scandinavica. A, Physical and inorganic chemistry/Acta chemica Scandinavica. Series B. Organic chemistry and biochemistry/Acta chemica Scandinavica. Series A, Physical and inorganic chemistry (1986)

Gunnar Antoni Bengt Långström R. Datema Stefan Oscarson Curt R. Enzell

Alanine

10.3891/acta.chem.scand.40b-0152

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Citations (24)

Synthesis of Siphulin, a Naturally Occurring Homoflavone.

Acta chemica Scandinavica/Acta chemica Scandinavica. B, Organic chemistry and biochemistry/Acta chemica Scandinavica. A, Physical and inorganic chemistry/Acta chemica Scandinavica. Series B. Organic chemistry and biochemistry/Acta chemica Scandinavica. Series A, Physical and inorganic chemistry (1985)

Anders Kjær Dana Kjær Chr. Rømming Brandon Oberg R. Datema

Synthese a partir de benzyloxy-4' heptyl-6' hydroxy-2' acetophenone et de carboxy-2 dibenzyloxy-3,5 benzene acetate de methyle

10.3891/acta.chem.scand.39b-0065

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Citations (5)

Inhibition of β-1,4-Glucan Biosynthesis by Deoxyglucose

PLANT PHYSIOLOGY (1983)

R. Datema Ralph Τ. Schwarz Liliana A. Rivas Rafael Pont Lezica

GDP- and UDP-deoxyglucose inhibit the incorporation of glucose from UDP-glucose into dolichyl phosphate glucose and dolichyl pyrophosphate oligosaccharides. GDP-deoxyglucose inhibits by competing with the physiological nucleotide sugars for dolichyl phosphate, and dolichyl phosphate deoxyglucose is formed. This inhibition is reversed by excess of dolichyl phosphate. UDP-deoxyglucose does not give rise to a lipid-linked derivative, and inhibition by this analog is not reversed by dolichyl phosphate. The UDP- and GDP-derivatives of deoxyglucose inhibit the incorporation of glucose into glucose-containing glycoproteins. This effect seems to be the result of the inhibition of lipid intermediates glucosylation and is comparable to the effect produced by coumarin. Cellulose synthetase activity is not affected by UDP- or GDP-deoxyglucose. On the other hand, deoxyglucose inhibits the formation of beta-1,4-glucans in vivo.

Deoxyglucose

10.1104/pp.71.1.76

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Citations (17)

ChemInform Abstract: Structure‐Activity Relationships in Distamycin A Analogues: Effect of Alkyl Groups on the Pyrrole Nitrogen at the Non‐amidine End of the Molecule Combined with Methyl Elimination in the Following Ring.

Chemischer Informationsdienst (1986)

Leif Grehn Ulf Ragnarsson R. Datema

Abstract The distamycin Aanalogues (V) were synthesized using the previously described strategy with some improved modifications and screened for their effects on herpes simplex virus (HSV‐l).

Amidine

Pyrrole

10.1002/chin.198626331

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Citations (0)

The Presence of Dolichol in Liver Supernatant.

Acta chemica Scandinavica/Acta chemica Scandinavica. B, Organic chemistry and biochemistry/Acta chemica Scandinavica. A, Physical and inorganic chemistry/Acta chemica Scandinavica. Series B. Organic chemistry and biochemistry/Acta chemica Scandinavica. Series A, Physical and inorganic chemistry (1985)

E.L. Appelkvist Tadeusz Chojnacki Gustav Dallner Kenneth L. Rinehart R. Datema

Dolichol

10.3891/acta.chem.scand.39b-0072

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Citations (9)