1,721,363 research outputs found
Preparation of benzo[b]isothiazol-3-one benzenesulfonamide derivatives for treatment of HIV.
No full text
Therapeutical compositions having anti-HIV activity consisting of 2', 3'-didesoxyadenosine and substances inhibiting adenosine deaminase.
No full textTherapeutical compositions, having enhanced anti-HIV activity consisting of 2', 3'-didesoxy-
adenosine and of substances inhibiting the adenosine-deaminase selected from the group
consisting of 9-(erythro-2-hydroxy-3-nonyl) adenine (EHNA), 3-deaza-EHNA, coformycin,
desoxycoformycin, 1-deaza-EHNA, 1, 3-dideaza-EHNA and 7-deaza-EHNA
Anti-HIV evaluation of benzo[d]isothiazole hydrazones
No full textThe synthesis and the anti-HIV-1 activity of novel benzo[d]isothiazole hydrazones are reported. Target compounds tested in MT-4 cells cultures
for their anti-HIV properties against wild type HIV-1 and HIV strains carrying clinically relevant mutations (EFVR, Y181C and K103/
Y181C) showed good activity against wild type HIV-1 and against the EFVR mutant. In terms of SAR the relevant result was that, in the class
of benzisothiazole hydrazones, the benzo[d]isothiazol-3(2H)-one moiety (compounds 1 and 4) is an essential structural requirement for the antiretroviral
activity
Novel Synthesis and Anti-HIV-1 Activity of 2-Arylthio-6-benzyl-2,3-dihydro-1H-pyrimidin-4-ones (Aryl S-DABOs)
No full textThe synthesis and the anti-HIV-1 activity of a series of 2-arylthio-6-benzyl-2,3-dihydro-1H-pyrimidin-4-ones (aryl S-DABOs) are reported. These compounds were synthesized via a coupling reaction of the corresponding 6-benzyl-2-thiouracils with aryl iodides in the presence of neocuproine hydrate, copper(I) iodide, and sodium tert-butoxide. Target compounds showed moderate activity against HIV-1
Potent and Selective Activity of Daphnane Diterpens against HIV-1, HIV-2 and Coxsackievirus
No full textThe antimitotic drug 4,6 dimethyl 2 amino 3,4,5 trimethoxy phenyl pyrimidine inhibits the nucleoside transport system of cells from various animal species
No full text4,6-dimethyl-2-amino-3,4,5-trimethoxyphenyl-pyrimidine (B-31) is a pyrimidine derivative previously reported to arrest the mitotic cycle of mammalian cells in metaphase. In the present study it is shown that B-31 also acts as a specific inhibitor of the cellular uptake of nucleosides. The uptake of purinic and pyrimidinic nucleosides is inhibited by 80-90% at concentrations in the range 5-20 mu g/ml, whereas those of nucleobases, leucine, choline and glucose are unaltered at the maximum nontoxic dose of B-31 (25 mu g/ml). Various mammalian (human, monkey and murine) and avian cell are equally sensitive to the inhibition of nucleoside transport. The antimitotic effect of B-31, by contrast, is species-specific: human cells are the most sensitive whereas monkey and chicken fibroblasts appear resistant to this effect. Both effects can be reversed by removal of B-31 from the medium; inhibition of nucleoside transport can also be reversed by high doses of the nucleosides themselves
Synthesis of some novel 2,6-disubstituted pyridazin-3-ones as TMC120 analogues
No full textDifferent analogues of TMC120 derived from pyridazin-3(2H)-one rings were synthesized by coupling of 3,6-dichloropyridazine with arylacetonitriles, phenols and/or aniline derivative followed by hydrolysis and alkylation with different benzyl bromide derivatives
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