Discovery of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV-1 agents

Barreca, Maria Letizia; Chimirri, Alba; Luca, Laura De; Monforte, Anna Maria; Monforte, P; Rao, Angela; Zappalà, Maria; Balzarini, Jan; Clercq, Erik De; Pannecouque, Christophe; Witvrouw, Myriam

doi:10.1016/s0960-894x(01)00304-3

Cited by 228 publications

(126 citation statements)

References 9 publications

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“…The unique nature of the replicative cycle of HIV-1 provides many potential targets for therapeutic interventions. One of these, reverse transcriptase (RT) is a key enzyme, which is packaged within the HIV virion capsid and plays an essential and multifunctional role in the replication of the virus [102]. The RT inhibitors known to date are of two types: nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs, NtRTIs) and nonnucleoside reverse transcriptase inhibitors (NNRTIs).…”

Section: Antiviral Activitymentioning

confidence: 99%

Pharmacological significance of triazole scaffold

Kharb

Sharma

Yar

2010

Journal of Enzyme Inhibition and Medicinal Chemistry

453

236

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Section: Antiviral Activitymentioning

confidence: 99%

Pharmacological significance of triazole scaffold

Kharb

Sharma

Yar

2010

Journal of Enzyme Inhibition and Medicinal Chemistry

453

236

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“…In IR spectra the strong band at 1680 cm -1 , which belongs to carbonyl group of propiophenone disappeared and two new bands at 3388-3277 cm -1 relating with NH 2 exten-ding seemed which affirmed that cyclization of thiazole [23]. In 1 H NMR spectra of synthesized compounds (4a-f) show singlet signal at δ 6.90 ppm for two protons of NH 2 [24] and 13 C NMR spectra show ten peaks for ten different carbon atoms in compounds (4a-c) and eleven carbon peaks for compounds (4d-f).…”

Section: Resultsmentioning

confidence: 79%

“…It needs to be accounted to show different physiological activities. They found uses as antitubercular [3], antimicrobial [4][5][6][7][8], antiinflammatory [9], anticancer [10], antihistamines [11], anticonvulsant [12] and as antiviral agents especially as anti-HIV agents [11,13,14]. It has been extensively reported that the antibacterial activity strongly depended on the nature of substituents at C2 and N3 of thiazolidinone ring.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antimicrobial Activities of Some Novel 2,3-Substituted-1,3-Thiazolidin-4-ones Derived from 2-Amino-1,3-thiazole

Khalid¹

2017

Asian J. Chem.

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New 2,3-substituted-1,3-thiazolidin-4-one (6a-f) were prepared by cyclocondensation of 2-[6-(4-chlorobenzyloxy)-2-naphthyliden]-4-(4-substituted phenyl)-5-methyl-1,3-thiazole (5a-f) and mercaptoacetic acid in benzene. The synthesized compounds were characterized on the basis of elemental analysis, 1 H NMR, 13 C NMR and FT-IR. The prepared compounds have been screened in vitro against two Grampositive Staphylococcus aureus, Staphylococcus epidermidis, and two Gram-negative Escherichia coli, Pseudomonas aernuginosa for antibacterial activity and two fungal strains Candida albicans, Candida krusei for antifungal activity using ciprofloxacin, ampicillin and ketoconazole with minimal inhibitory concentration (MIC) value of 10 mcg/L in DMSO. Compounds 6a and 6d showed good antibacterial and antifungal activities compared to reference medications utilized within this study.

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“…Since the discovery of heterocyclic nucleus the chemistry of thiazolidinones and their allied compounds continue to draw attention of organic chemists due to their various biological activities such as antibacterial, [1][2][3][4] anticancer, 5 antitubercular, 6,7 antifungal, 8 anti-inflammatory, 9 antiviral, 10 analgesic. 11 Thiazolidinone and their arylidene derivatives are also having highly therapeutic nature such as antioxidants, 12 antitumor agents, 13 agricultural fungicides.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and In-vitro Activity of Some New Class of Thiazolidinone and Their Arylidene Derivatives

Seelam¹,

Shrivastava²

2011

Bulletin of the Korean Chemical Society

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In an attempt to find a new class of anti microbial agents, a series of thiazolidinone and their 5-arylidene derivatives containing 4-(4-methyl benzamido)-benzoyl moiety were synthesized via the reaction of benzocaine with appropriate chemical reagents. These compounds were screened for their antibacterial activity against Gram-positive bacteria (Bacillus subtilis and Bacillus thuringiensis), Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa) and antifungal activity against Botrytis fabae, Fusarium oxysporan and Candida albicans. On the other hand the synthesized compounds were also screened for their anti tubercular activity. IR, 1 H NMR, 13C NMR and MS spectral analyses established the structures of the newly synthesized compounds. The results revealed that some of these compounds have shown promising antimicrobial and anti tubercular activity in comparison with standard drugs.

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Discovery of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV-1 agents

Cited by 228 publications

References 9 publications

Pharmacological significance of triazole scaffold

Pharmacological significance of triazole scaffold

Synthesis and Antimicrobial Activities of Some Novel 2,3-Substituted-1,3-Thiazolidin-4-ones Derived from 2-Amino-1,3-thiazole

Synthesis and In-vitro Activity of Some New Class of Thiazolidinone and Their Arylidene Derivatives

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