Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0021051 (immunodeficiency)
 71,517 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Imexon (4-imino-1, 3-diazabicyclo-(3.1.0)-hexan-2-one) a cyanoaziridine compound was studied in the treatment of the murine retrovirus-induced immunodeficiency disease model of AIDS (LP-BM5, MAIDS). Imexon, in dose-dependent fashion, partially prevented the development of hypergammaglobulinemia and splenomegaly, and partially prevented the decline in the phytohemagglutinin-induced proliferative response of spleen lymphocytes when started 1 or 15 days after virus inoculation. There was a statistically significant reduction in these disease-associated manifestations. When animals were treated starting 78 or 92 days after virus inoculation, lymphadenopathy was completely abrogated and survival was significantly prolonged in a dose-responsive manner. Since Imexon and other cyanoaziridine compounds have been safely administered to humans, we suggest that this class of compounds be further investigated in both large animal models of HIV infection and in patients with HIV-induced disease.
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PMID:Treatment of the murine, retrovirus-induced lymphoproliferative immunodeficiency disease (LP-BM5) in C57BL/10 mice with the immunomodulator Imexon. 151 14

A six-stage synthesis of 2',3'-dideoxy-2',3'-alpha-methanocytidine (3) from (5S)-5-benzoyloxymethyl-(5H)-furan-2-one (5) is described. The key step involved the stereoselective formation of (1R,4S,5S)-4-benzoyloxymethyl-3-oxabicyclo[3.1.0]hexan-2-one (7) via 1,3-dipolar cycloaddition of diazomethane to 5 followed by photoinduced elimination of nitrogen. Reduction of 7 to the corresponding lactol followed by acetylation yielded primarily 1-O-acetyl-5-O-benzoyl-2,3-dideoxy-beta-D-ribofuranose (8). Reaction of 8 with 2,4-bis(trimethylsilyl)cytosine and EtAlCl2 followed by deprotection and chromatography gave 3, which exhibited only weak activity against the human immunodeficiency virus (HIV).
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PMID:Synthesis of 2',3'-dideoxy-2',3'-alpha-methanocytidine. 217 79