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Synthesis, antimicrobial, and anti-inflammatory activities of novel 2-(1-adamantyl)-5-substituted-1,3,4-oxadiazoles and 2-(1-adamantylamino)-5-substituted-1,3,4-thiadiazoles.
The oxadiazole derivatives 4c, 4g, 4i and 4j produced good dose-dependent anti-inflammatory activity, particularly against the tested Gram-positive bacteria Bacillus subtilis and yeast-like pathogenic fungus Candida albicans. Expand
Synthesis of New Quinazoline-2,4(1H,3H)-dione non-nucleoside Analogues of the reverse transcriptase inhibitor TNK-651
The synthesis is described of a series of new non-nucleoside analogues of the reverse transcriptase inhibitor TNK-651 from quinazoline-2,4(1H,3H)-diones. Compounds 2a–c were silylated and treatedExpand
Synthesis of novel N-1 (allyloxymethyl) analogues of 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine) with improved activity against HIV-1 and its mutants.
Structural-activity relationship studies established a correlation between the anti-HIV-1 activity and the substitution pattern of the N-1 allyloxymethyl group. Expand
Synthesis of 6‐(3,5‐Dichlorobenzyl) Derivatives as Isosteric Analogues of the HIV Drug 6‐(3,5‐Dimethylbenzyl)‐1‐(ethoxymethyl)‐5‐isopropyluracil (GCA‐186)
The HIV‐1 inhibitors described in this paper is closely related to 6‐(3,5‐dimethylbenzyl)‐1‐(ethoxy methyl)‐5‐isopropyluracil (GCA‐186) an anti‐HIV‐1 drug that is highly active against both wild typeExpand
Synthesis of 6-arylvinyl analogues of the HIV drugs SJ-3366 and Emivirine.
The synthesis and the antiviral activities of a series of 6-arylvinyl substituted analogues of SJ-3366, a highly potent agent against HIV, showed activities against HIV-1 wild type in the range of Efavirenz, and moderate activities against Y181C and Y181N mutant strains were also observed. Expand
Some Observations on the Base-Catalyzed Cyclocondensation of 2,6-Dihalobenzaldehydes, Ethyl Cyanoacetate, and Thiourea
The reaction of 2,6-difluorobenzaldehyde, 2-chloro-6-fluorobenzaldehyde, or 2,6-dichlorobenzaldehyde and ethyl cyanoacetate and thiourea, in the presence of potassium carbonate, yielded a mixture ofExpand
Synthesis, antimicrobial, and anti-inflammatory activities of novel 2-[3-(1-adamantyl)-4-substituted-5-thioxo-1,2,4-triazolin-1-yl] acetic acids,
The reaction of 3-(1-adamantyl)-4-substituted-1,2,4-triazoline-5-thiones 3a-g with sodium chloroacetate, in ethanolic sodium hydroxide yielded the corresponding N1-acetic acid derivatives 4a-G, which upon hydrolysis with aqueous sodium Hydroxide afforded the corresponding propionic acid derivatives 6 a-g. Expand