Synthesis, antimicrobial evaluation and QSAR studies of novel piperidin-4-yl-5-spiro-thiadiazoline derivatives
2
Department of Pharmacology, PSG College of Pharmacy, Coimbatore 641 004, India
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Тип публикации: Journal Article
Дата публикации: 2010-12-01
scimago Q2
wos Q2
БС2
SJR: 0.472
CiteScore: 5.1
Impact factor: 2.2
ISSN: 0960894X, 14643405
PubMed ID:
21035335
Organic Chemistry
Drug Discovery
Biochemistry
Molecular Biology
Pharmaceutical Science
Clinical Biochemistry
Molecular Medicine
Краткое описание
In an attempt to find a new class of antimicrobial agents, a series of new 1,3,4-thiadiazolines were synthesized from 2,6-diarylpiperidin-4-ones, via the corresponding 4'-phenylthiosemicarbazones. All the synthesized compounds (23-39) were virtually screened against bacterial (Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and Salmonella typhi) and fungal strains (Candida albicans, Rhizopus sp, Aspergillus niger and Aspergillus flavus) by serial dilution method. QSAR study indicated that the increase in weakly polar component of solvent accessible surface area will favour antibacterial activity while increase in polarizability and decrease in ionisation potential and hydrogen bond donor will favour antifungal activity.
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Umamatheswari S. et al. Synthesis, antimicrobial evaluation and QSAR studies of novel piperidin-4-yl-5-spiro-thiadiazoline derivatives // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 23. pp. 6909-6914.
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Umamatheswari S., Balaji B., Ramanathan M., Kabilan S. Synthesis, antimicrobial evaluation and QSAR studies of novel piperidin-4-yl-5-spiro-thiadiazoline derivatives // Bioorganic and Medicinal Chemistry Letters. 2010. Vol. 20. No. 23. pp. 6909-6914.
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TY - JOUR
DO - 10.1016/j.bmcl.2010.10.002
UR - https://doi.org/10.1016/j.bmcl.2010.10.002
TI - Synthesis, antimicrobial evaluation and QSAR studies of novel piperidin-4-yl-5-spiro-thiadiazoline derivatives
T2 - Bioorganic and Medicinal Chemistry Letters
AU - Umamatheswari, Seeman
AU - Balaji, Bhaskar
AU - Ramanathan, Muthiah
AU - Kabilan, Senthamaraikannan
PY - 2010
DA - 2010/12/01
PB - Elsevier
SP - 6909-6914
IS - 23
VL - 20
PMID - 21035335
SN - 0960-894X
SN - 1464-3405
ER -
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@article{2010_Umamatheswari,
author = {Seeman Umamatheswari and Bhaskar Balaji and Muthiah Ramanathan and Senthamaraikannan Kabilan},
title = {Synthesis, antimicrobial evaluation and QSAR studies of novel piperidin-4-yl-5-spiro-thiadiazoline derivatives},
journal = {Bioorganic and Medicinal Chemistry Letters},
year = {2010},
volume = {20},
publisher = {Elsevier},
month = {dec},
url = {https://doi.org/10.1016/j.bmcl.2010.10.002},
number = {23},
pages = {6909--6914},
doi = {10.1016/j.bmcl.2010.10.002}
}
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MLA
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Umamatheswari, Seeman, et al. “Synthesis, antimicrobial evaluation and QSAR studies of novel piperidin-4-yl-5-spiro-thiadiazoline derivatives.” Bioorganic and Medicinal Chemistry Letters, vol. 20, no. 23, Dec. 2010, pp. 6909-6914. https://doi.org/10.1016/j.bmcl.2010.10.002.