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)

A series of 1-aryl-1H,3H-thiazolo[3,4-a]benzimidazoles were synthesized by one-pot reaction from o-phenylenediamine, 2-mercaptoacetic acid and a variety of aromatic aldehydes. All compounds obtained were evaluated for antiviral activity against human immunodeficiency virus (HIV). Compounds 4g, 4i, 4j, 4l and 4q exhibit reproducible in vitro anti-HIV activity.
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PMID:Anti-HIV agents. I: Synthesis and in vitro anti-HIV evaluation of novel 1H,3H-thiazolo[3,4-a]benzimidazoles. 168 21

A series of 1-aryl-1H,3H-thiazolo[3,4-a]benzimidazoles was synthesized starting from o-phenylenediamine, disubstituted aromatic aldehydes and 2-mercaptoacetic acid. Their antiviral activity against human immunodeficiency virus (HIV) was explored: the 1-(2',6'-dichlorophenyl) (4c), 1-(2',6'-difluorophenyl) (4i), 1-(2'-chloro,6'-fluorophenyl) (4K) and 1-(2'-chloro,5'-nitrophenyl) (4m) derivatives significantly inhibit in vitro the viral cytopathic effect in HIV-infected CEM cells. Compound 4i was selected by NCI's Review Committee for initial preclinical development studies.
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PMID:Anti-HIV agents II. Synthesis and in vitro anti-HIV activity of novel 1H,3H-thiazolo[3,4-a]benzimidazoles. 168 51

New esters (2b and 2c) and hydrazides (3b and 3c) were synthesized from 6-methyl/fluoro-3-phenyl-4(1H, 3H)-quinazolinone-2-thiones (1b and 1c). Subsequent treatment of 3-phenyl-4(3H)-quinazolinone-2-yl)mercaptoacetic acid hydrazides (3a-e) with 1H-indole-2,3-diones (4a-e) furnished the corresponding 3-[[(3-phenyl-4(3H)-quinazolinone-2-yl)mercaptoacetyl]hydrazono]-1H-2-indolinones (5a-u). The structures of new compounds were determined by analytical and spectral (IR, 1H-NMR, (13)C-NMR, EIMS) methods. Previously reported 3-[[(3-phenyl-4(3H)-quinazolinone-2-yl)mercaptoacetyl]hydrazono]-5-bromo-1H-2-indolinone 5v and compounds 5b, 5d and 5o chosen as prototypes were evaluated against the full panel of 60 human tumour cell lines at a minimum of five concentrations at tenfold dilutions in the National Cancer Institute in vitro primary cytotoxicity assay. Sulforhodamine B protein assay was used to estimate cell stability or growth. 3-[[(6-Chloro-3-phenyl-4(3H)-quinazolinone-2-yl)mercaptoacetyl]hydrazono]-5-fluoro-1H-2-indolinone 5o showed the most favourable cytotoxicity against a renal cancer cell line UO-31 (log(10)GI(50) value -6.68). Compound 5v was also tested against human immunodeficiency virus 1 (HIV-1). Compound 5v was confirmed moderately active against HIV-1.
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PMID:Synthesis and primary cytotoxicity evaluation of 3-[[(3-phenyl-4(3H)-quinazolinone-2-yl)mercaptoacetyl]hydrazono]-1H-2-indolinones. 1283 36

A diversity of novel 2-aryl-3-heteroaryl-2-ylmethyl-1,3-thiazolidin-4-ones were designed and synthesized by reacting heteroaryl-2-ylmethyl amine with various 2,6-dihalosubstituted benzaldehydes and mercaptoacetic acid. The title compounds were evaluated for human immunodeficiency virus type-1 (HIV-1) reverse transcriptase (RT) inhibitory activity. The results of in vitro assays showed that some of the compounds were effective inhibitors of HIV-1 reverse transcriptase enzyme at micromolar concentrations with less cytotoxicity in both MT-4 cells as well as acutely infected human T-lymphoid CEM cells. Compounds 4h and 4k emerged as moderately more potent with EC(50) are at 0.20 and 0.21 microM as compared to reference parent compound thiazolobenzimidazoles EC(50) 0.35 microM in MT-4 cells.
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PMID:2-(2,6-Dihalo-phenyl)-3-heteroaryl-2-ylmethyl-1, 3-thiazolidin-4-ones: anti-HIV agents. 1862 10