Synthesis, biological evaluation, and molecular modeling studies of new 1,3,4-oxadiazole- and 1,3,4-thiadiazole-substituted 4-oxo-4H-pyrido[1,2-a]pyrimidines as anti-HIV-1 agents

Hajimahdi, Zahra; Zarghi, Afshin; Zabihollahi, Rezvan; Aghasadeghi, Mohammad Reza

doi:10.1007/s00044-012-0241-5

Cited by 56 publications

(27 citation statements)

References 16 publications

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“…Raltegravir (Fig. 2), an HIV integrase strand transfer inhibitor, was approved by FDA in October 2007 [10]. Tan et al [11] synthesized the 1,3,4-oxadiazole analog I as a potent anti-HBV agent with the EC 50 value of 1.63 mM for the inhibition of virion production.…”

Section: Introductionmentioning

confidence: 98%

Synthesis and Anti‐Hepatitis B Virus Evaluation of 7‐Methoxy‐3‐heterocyclic quinolin‐6‐ols

Liu

Feng

et al. 2015

Archiv der Pharmazie

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A series of novel 7-methoxy-3-heterocyclic quinolin-6-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in the HepG2.2.15 cell line. Five compounds, 14a, 15c, 15e, 16b, and 16f, displayed excellent potency and selectivity toward the HBV, with IC values of less than 5.0 µM and selectivity index values of 11.0-71.5. Structure-activity relationship studies indicated that the 1,3,4-thiadiazole and sulfinylmethyl derivatives showed the most potent activities against the HBV.

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Section: Introductionmentioning

confidence: 98%

Synthesis and Anti‐Hepatitis B Virus Evaluation of 7‐Methoxy‐3‐heterocyclic quinolin‐6‐ols

Liu

Feng

et al. 2015

Archiv der Pharmazie

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“…To overcome the MDR limitations many research has taken place and in that oxadiazole is one of the promising scaffold in the medicinal chemistry [2]. Oxadiazoles are physiologically active heterocyclic compounds owing to a vast sphere of biological activities, including anticancer [3][4][5][6][7][8][9][10][11], antidiabetic [12], antiviral [13,14], anti-inflammatory [15,16], antibacterial [17,18], antifungal [19], antimycobacterial [20], analgesic [21], anticonvulsant [22], tyrokinase inhibitor [23] and cathepsin K inhibitor [24] antioxidant [25] properties.…”

Section: Introduction and Experimentalmentioning

confidence: 99%

Synthesis, characterisation and evaluation of oxadiazole as promising anticancer agent

2020

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A unique series oxadiazoles were synthesized by cyclization of benzophenone hydrazide, followed by the nucleophillic alkylation of heterocyclic scaffold. Synthesized title compounds were characterized by the FT-IR, LCMS and NMR spectral techniques. The newly synthesized compounds were screened for the anticancer activity. IC 50 values of the 7h observed for in-vitro anti-cancer activities were 112.6 µg/ml and 126.7 µg/ml, against the MCF-7 and KB cell lines respectively. Most active compounds were found to be less toxic, which were determined by MTT assay method with normal cell line (L292). Biological screening of the synthesized series of compounds reveals that, Compound 7h was the potent molecule.Electronic supplementary material The online version of this article (https ://doi.org/10.1007/s4245 2-020-2511-z) contains supplementary material, which is available to authorized users. * S. V. Mamatha, mamatha.zh32@yahoo.com |

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“…Sulfonamide derivatives has been well known for their antitumor [2], anti-diabetic [3], anti-malarial [4], antimicrobial [5][6], anti-inflammatory [7], antioxidant [8], COX inhibitors [9], lipoxygenase inhibitors [10], alzheimer ' s disease [11], etc. Many literature survey revealed that 1,3,4-oxadiazole possess diverse pharmacological activities such as anticancer [12][13][14], antimicrobial [15][16][17][18], anti-HIV [19], antiproliferative [20], antiviral [21], anti-inflammatory [22][23], anticonvulsant [24]. Some of 2,5-disubstituted 1,3,4oxadiazole based entities have emerged as most potent antimicrobial activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and biological evaluation of sulfonamide-based 1,3,4-oxadiazole derivatives

Kavitha¹,

Nasarullah²,

Kannan³

2019

Bull. Chem. Soc. Eth.

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A novel series of 1,3,4-oxadiazole containing sulfonamide derivatives were synthesized by 5-(5cyclohexyl-1,3,4-oxadiazol-2-yl)-2-methyl-benzenesulfonyl chloride. A good yield of intermediate with various substituted like aryl/hetero was formed. All the synthesized compounds were characterized by FT-IR, 1 H NMR, 13 C NMR and mass spectral studies. These compounds were evaluated for their preliminary bioassay in vitro antimicrobial activity, anti-inflammatory and anti-diabetic activities. In this series, most of the compounds have good anti-inflammatory activity. Particularly, compounds 5c, 5d and 5e showed excellent anti-inflammatory activity with IC50 values of 110, 110, and 111 μg/mL than diclofenac (157 μg/mL). The frontier orbital energy and the global reactivity descriptor were discussed for the tested compounds using RB3LYP/311G(d,p) basis set. Results revealed that the theoretical calculations of antimicrobial activity were closely related to quantum chemical parameters.

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Synthesis, biological evaluation, and molecular modeling studies of new 1,3,4-oxadiazole- and 1,3,4-thiadiazole-substituted 4-oxo-4H-pyrido[1,2-a]pyrimidines as anti-HIV-1 agents

Cited by 56 publications

References 16 publications

Synthesis and Anti‐Hepatitis B Virus Evaluation of 7‐Methoxy‐3‐heterocyclic quinolin‐6‐ols

Synthesis and Anti‐Hepatitis B Virus Evaluation of 7‐Methoxy‐3‐heterocyclic quinolin‐6‐ols

Synthesis, characterisation and evaluation of oxadiazole as promising anticancer agent

Synthesis and biological evaluation of sulfonamide-based 1,3,4-oxadiazole derivatives

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