Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivatives

Al‐Soud, Yaseen A.; Al‐Masoudi, Najim A.; Hassan, H. Gh.; Clercq, Erik De; Pannecouque, Christophe

doi:10.2478/v10007-007-0031-7

Cited by 30 publications

(11 citation statements)

References 24 publications

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“…Al-Soud et al, reported the synthesis of new 5-substituted piperazinyl-4-nitroimidazole derivatives and their evaluation for anti-HIV activity [95]. The target was the synthesis of new 4-nitroimidazoles, leading to inhibition of HIV by inhibition of RT and reduction of the drug-resistance strains [95].…”

Section: Anti-hiv Active Nitroimidazolesmentioning

confidence: 99%

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Synthetic Nitroimidazoles: Biological Activities and Mutagenicity Relationships

Mital

2009

Sci. Pharm.

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Parasitic and bacterial infections affecting the gastrointestinal tract represent a significant cause of morbidity and mortality worldwide. Nitroheterocyclic drugs have been available since the early 1960s for the treatment of anaerobic protozoa. The application of these drugs has widened and they are presently used to treat anaerobic pathogenic bacteria and protozoa. 5-nitroimidazoles are a well-established group of antiprotozoal and antibacterial agents that inhibit the growth of both anaerobic bacteria and certain anaerobic protozoa, such as Trichomonas vaginalis, Entamoeba histolytica and Giardia lamblia. The important antibacterial and antiprotozoal activities of nitroimidazoles are associated with reductive metabolism that has led to considerable interest in nitroimidazole reduction chemistry and the synthesis of new, highly effective drugs. The present review provides a brief account of various biological activities exhibited by synthetic nitroimidazole derivatives as well as their structure-mutagenicity relationships.

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Section: Anti-hiv Active Nitroimidazolesmentioning

confidence: 99%

“…The target was the synthesis of new 4-nitroimidazoles, leading to inhibition of HIV by inhibition of RT and reduction of the drug-resistance strains [95]. Compounds 25 and 26 were found to be most active among the tested compounds inhibiting HIV replication in cell culture ( Figure 5).…”

Section: Anti-hiv Active Nitroimidazolesmentioning

confidence: 99%

Synthetic Nitroimidazoles: Biological Activities and Mutagenicity Relationships

Mital

2009

Sci. Pharm.

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“…We present the synthesis 8-chloro-2,3-dihydroimidazole [1,2b] [1,4,2] benzodithi-azine-5,5-dioxides and 9-chloro-2,3,4-trihydropyrimido [1,2b] [1,4,2] benzodithi-azine-6,6-dioxides (figure 1). Succesfully identified anti-HIV activity ECO 50 0.09 μM.…”

Section: Imidazole Compound and Derivatesmentioning

confidence: 99%

Synthesis of Metal-Organic (Complexes) Compounds Copper(ii)-Imidazole for Antiviral Hiv Candidate

Sucipto

Martak

2016

IJTID

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The human immunodeficiency virus (HIV) is viruses known as rotaviruses. Potential target for therapeutic is reverse transcriptase (RT), possesses an RNA-dependent DNA polymerase, DNA-dependent DNA polymerase and ribonuclease H fuctions. Imidazoles have high anti-HIV inhibitory activity, some derivates of imidazole reported drugs . 8-chloro-2,3-dihydroimidazole[1,2-b] [1,4,2]benzodithiazine-5,5-dioxides and 9-chloro-2,3,4-trihydropyri-mido[1,2-b] Key words: Complexes compound, copper, imidazole, antiviral, HIV ABSTRAK Human immunodeficiency virus (HIV) adalah virus yang termasuk golongan rotavirus. Target potensial untuk terapi adalah reverse transcriptase (RT), memiliki sebuah DNA-dependent RNA polimerase, DNA-dependent DNA polimerase dan ribonuklease. Imidazol memiliki aktivitas penghambatan anti-HIV yang tinggi, beberapa turunan dari imidazol melaporkan obat. 8-kloro-2,3-dihydroimidazole [1,2-b] [1,4,2] benzodithi-azine-5,5-dioksida dan 9-chloro-2,3,4-trihydropyri-mido [1,2-b]

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“…In continuation for our attempts in searching for new anti-HIV agents, [15][16][17][18][19][20][21][22][23] and on the basis of above promising biological results, we considered benzimidazoles and their analogs particularly interesting to optimize the synthetic approaches to our antiviral agents. In this study, the angiotensin-converting enzyme (ACE) inhibitor 'captopril' 24 has been selected as a main backbone for the synthesis of new benzimidazole, benzothiazole derivatives and their analogs as well as the thioether-captopril analogs, utilizing microwave irradiation method.…”

Section: Introductionmentioning

confidence: 99%

Amino acid derivatives. Part 6. New analogues of the angiotensin-converting enzyme 'Captopril'. Synthesis and anti-HIV activity

Al‐Masoudi¹,

Hamad²,

Hameed³

et al. 2010

Arkivoc

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The development of new HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs) offers the possibility of generating structures of increased potency. On this basis, new derivatives of the angiotensin-converting enzyme 'Captopril' bearing benzimidazoles, benzothiazole, purine and pyridine residues were synthesized with the aim of developing new NNRTIs. Alternatively, the thioether analogs bearing carboxymethylthio, 2-amino-2-oxo-ethylthio, 2-(phthalimido-2-yl)-2-ethylthio, 1-benzyl-2-ethyl-4-nitro-imidazol-5-yl)-piperazin-1-yl)-2-oxo-ethylthio, and the carboxamide analogs were prepared from condensation of Captopril with various halide derivatives. The new compounds were assayed against HIV-1 and HIV-2 in MT-4 cells. The compound having a 4-chlorobenzimidazole group was the most active in inhibiting HIV-1, with EC 50 = 0.24 µg/ml, with therapeutic indexes (SI) of 21, is a leading candidate for further development.

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Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivatives

Cited by 30 publications

References 24 publications

Synthetic Nitroimidazoles: Biological Activities and Mutagenicity Relationships

Synthetic Nitroimidazoles: Biological Activities and Mutagenicity Relationships

Synthesis of Metal-Organic (Complexes) Compounds Copper(ii)-Imidazole for Antiviral Hiv Candidate

Amino acid derivatives. Part 6. New analogues of the angiotensin-converting enzyme 'Captopril'. Synthesis and anti-HIV activity

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