Newer 1,2,3-oxathiazino [5,6-c] Quinolin-5 (6H) One-2,2-dioxidederivatives: Synthesis, Molecular Properties Prediction and Biological Evaluation as Potent Antibacterial, Anticoagulant Agents

Newer 1,2,3-oxathiazino [5,6-c] Quinolin-5 (6H) One-2,2-dioxidederivatives: Synthesis, Molecular Properties Prediction and Biological Evaluation as Potent Antibacterial, Anticoagulant Agents

A new heterocycle 1,2,3-oxathiazino[5,6-c]quinolin-5(6H)one-2,2-dioxide analogues have been generated by annelating quinolone and oxathiazine scaffolds in to a single core. 3-Formyl-4-hydroxy quinolin-2-one and chlorosulfonyl isocyanate underwent smooth cyclisation to afford title compounds in good...

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Main Authors: Naveen Polkam, Parsharamulu Rayam, Tejeswara Rao Allaka, Shankaraiah Malthum, Naveen Kuntala, Bhaskar Kummari, Malleshwar Darbarwar, Gautami Konda, Jaya Shree Anireddy
Format: บทความวารสาร
Language:English
Published: Science Faculty of Chiang Mai University 2019
Online Access:http://it.science.cmu.ac.th/ejournal/dl.php?journal_id=8473
http://cmuir.cmu.ac.th/jspui/handle/6653943832/63966
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Institution: Chiang Mai University
Language: English
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spelling th-cmuir.6653943832-639662019-05-07T09:59:40Z Newer 1,2,3-oxathiazino [5,6-c] Quinolin-5 (6H) One-2,2-dioxidederivatives: Synthesis, Molecular Properties Prediction and Biological Evaluation as Potent Antibacterial, Anticoagulant Agents Naveen Polkam Parsharamulu Rayam Tejeswara Rao Allaka Shankaraiah Malthum Naveen Kuntala Bhaskar Kummari Malleshwar Darbarwar Gautami Konda Jaya Shree Anireddy A new heterocycle 1,2,3-oxathiazino[5,6-c]quinolin-5(6H)one-2,2-dioxide analogues have been generated by annelating quinolone and oxathiazine scaffolds in to a single core. 3-Formyl-4-hydroxy quinolin-2-one and chlorosulfonyl isocyanate underwent smooth cyclisation to afford title compounds in good yields. All the newly synthesized compounds were characterized by various spectroscopic techniques. Among the tested, screening results indicate that products 3c-e demonstrated promising antibacterial activity against Gram +ve (S. aureus) and 3c-d against Gram -ve (E. coli) strains at 5 mg. Compound 3e displayed best anticoagulant activity. In silico investigations of the designed compounds revealed that none of them violated rule of five suggesting them as good antibacterial agents. 2019-05-07T09:59:40Z 2019-05-07T09:59:40Z 2017 บทความวารสาร 0125-2526 http://it.science.cmu.ac.th/ejournal/dl.php?journal_id=8473 http://cmuir.cmu.ac.th/jspui/handle/6653943832/63966 Eng Science Faculty of Chiang Mai University
institution Chiang Mai University
building Chiang Mai University Library
country Thailand
collection CMU Intellectual Repository
language English
description A new heterocycle 1,2,3-oxathiazino[5,6-c]quinolin-5(6H)one-2,2-dioxide analogues have been generated by annelating quinolone and oxathiazine scaffolds in to a single core. 3-Formyl-4-hydroxy quinolin-2-one and chlorosulfonyl isocyanate underwent smooth cyclisation to afford title compounds in good yields. All the newly synthesized compounds were characterized by various spectroscopic techniques. Among the tested, screening results indicate that products 3c-e demonstrated promising antibacterial activity against Gram +ve (S. aureus) and 3c-d against Gram -ve (E. coli) strains at 5 mg. Compound 3e displayed best anticoagulant activity. In silico investigations of the designed compounds revealed that none of them violated rule of five suggesting them as good antibacterial agents.
format บทความวารสาร
author Naveen Polkam
Parsharamulu Rayam
Tejeswara Rao Allaka
Shankaraiah Malthum
Naveen Kuntala
Bhaskar Kummari
Malleshwar Darbarwar
Gautami Konda
Jaya Shree Anireddy
spellingShingle Naveen Polkam
Parsharamulu Rayam
Tejeswara Rao Allaka
Shankaraiah Malthum
Naveen Kuntala
Bhaskar Kummari
Malleshwar Darbarwar
Gautami Konda
Jaya Shree Anireddy
Newer 1,2,3-oxathiazino [5,6-c] Quinolin-5 (6H) One-2,2-dioxidederivatives: Synthesis, Molecular Properties Prediction and Biological Evaluation as Potent Antibacterial, Anticoagulant Agents
author_facet Naveen Polkam
Parsharamulu Rayam
Tejeswara Rao Allaka
Shankaraiah Malthum
Naveen Kuntala
Bhaskar Kummari
Malleshwar Darbarwar
Gautami Konda
Jaya Shree Anireddy
author_sort Naveen Polkam
title Newer 1,2,3-oxathiazino [5,6-c] Quinolin-5 (6H) One-2,2-dioxidederivatives: Synthesis, Molecular Properties Prediction and Biological Evaluation as Potent Antibacterial, Anticoagulant Agents
title_short Newer 1,2,3-oxathiazino [5,6-c] Quinolin-5 (6H) One-2,2-dioxidederivatives: Synthesis, Molecular Properties Prediction and Biological Evaluation as Potent Antibacterial, Anticoagulant Agents
title_full Newer 1,2,3-oxathiazino [5,6-c] Quinolin-5 (6H) One-2,2-dioxidederivatives: Synthesis, Molecular Properties Prediction and Biological Evaluation as Potent Antibacterial, Anticoagulant Agents
title_fullStr Newer 1,2,3-oxathiazino [5,6-c] Quinolin-5 (6H) One-2,2-dioxidederivatives: Synthesis, Molecular Properties Prediction and Biological Evaluation as Potent Antibacterial, Anticoagulant Agents
title_full_unstemmed Newer 1,2,3-oxathiazino [5,6-c] Quinolin-5 (6H) One-2,2-dioxidederivatives: Synthesis, Molecular Properties Prediction and Biological Evaluation as Potent Antibacterial, Anticoagulant Agents
title_sort newer 1,2,3-oxathiazino [5,6-c] quinolin-5 (6h) one-2,2-dioxidederivatives: synthesis, molecular properties prediction and biological evaluation as potent antibacterial, anticoagulant agents
publisher Science Faculty of Chiang Mai University
publishDate 2019
url http://it.science.cmu.ac.th/ejournal/dl.php?journal_id=8473
http://cmuir.cmu.ac.th/jspui/handle/6653943832/63966
_version_ 1681425993606103040

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