Synthesis and anti-HIV activity of a new isoxazole containing disubstituted 1,2,4-oxadiazoles analogs
Prem Kumar Kushwaha
1
,
Kumar Vaibhav Srivastava
2
,
Neha Kumari
1
,
Rajan Kumar
1
,
Debashis Mitra
2
,
Ashoke Sharon
1
Publication type: Journal Article
Publication date: 2022-02-01
scimago Q2
wos Q1
SJR: 0.608
CiteScore: 6.7
Impact factor: 3.0
ISSN: 09680896, 14643391
PubMed ID:
35026631
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Abstract
Continuing on our antiviral drug discovery research, we intended to diversify our lead anti-HIV-1 inhibitor by non-classical isosteric replacement of amide to 1,2,4-oxadiazoles. The resulting molecules isoxazole-1,2,4-oxadiazole analogs were synthesized using mild bases in ethanol under microwave irradiation. The anti-HIV potential was checked in human CD4+ reporter cell lines, TZM-bl and CEM-GFP, at the highest non-cytotoxic concentration (HNC), demonstrating that 3-((3-(p-tolyl)isoxazol-5-yl)methyl)-1,2,4-oxadiazole and 3-((3-(4-chlorophenyl)isoxazol-5-yl)methyl)-1,2,4-oxadiazole inhibit HIV-1 replication significantly and could be considered as a new lead candidate against HIV-1.
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17
Total citations:
17
Citations from 2024:
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(64.7%)
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Kumar Kushwaha P. et al. Synthesis and anti-HIV activity of a new isoxazole containing disubstituted 1,2,4-oxadiazoles analogs // Bioorganic and Medicinal Chemistry. 2022. Vol. 56. p. 116612.
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Kumar Kushwaha P., Srivastava K. V., Kumari N., Kumar R., Mitra D., Sharon A. Synthesis and anti-HIV activity of a new isoxazole containing disubstituted 1,2,4-oxadiazoles analogs // Bioorganic and Medicinal Chemistry. 2022. Vol. 56. p. 116612.
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RIS
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TY - JOUR
DO - 10.1016/j.bmc.2022.116612
UR - https://doi.org/10.1016/j.bmc.2022.116612
TI - Synthesis and anti-HIV activity of a new isoxazole containing disubstituted 1,2,4-oxadiazoles analogs
T2 - Bioorganic and Medicinal Chemistry
AU - Kumar Kushwaha, Prem
AU - Srivastava, Kumar Vaibhav
AU - Kumari, Neha
AU - Kumar, Rajan
AU - Mitra, Debashis
AU - Sharon, Ashoke
PY - 2022
DA - 2022/02/01
PB - Elsevier
SP - 116612
VL - 56
PMID - 35026631
SN - 0968-0896
SN - 1464-3391
ER -
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BibTex (up to 50 authors)
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@article{2022_Kumar Kushwaha,
author = {Prem Kumar Kushwaha and Kumar Vaibhav Srivastava and Neha Kumari and Rajan Kumar and Debashis Mitra and Ashoke Sharon},
title = {Synthesis and anti-HIV activity of a new isoxazole containing disubstituted 1,2,4-oxadiazoles analogs},
journal = {Bioorganic and Medicinal Chemistry},
year = {2022},
volume = {56},
publisher = {Elsevier},
month = {feb},
url = {https://doi.org/10.1016/j.bmc.2022.116612},
pages = {116612},
doi = {10.1016/j.bmc.2022.116612}
}
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