Synthesis and in vitro assessment of anticholinesterase and antioxidant properties of triazineamide derivatives
Cholinesterase inhibitors and radical scavengers have been recognized as powerful symptomatic anti-Alzheimer's disease agents. Hence, the present study aimed to develop new triazineamides as potent anticholinesterase and antioxidant agents. Triazineamide ( ) derivatives were synthesized using c...
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| Veröffentlicht in: | Future medicinal chemistry 2022-12, Vol.14 (23), p.1741-1753 |
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| creator | Vatturu, Murali Rao, Kandrakonda Yelamanda Yesu, Valaparla Bala Basha, Shaik Jeelan Guptha, Tanguturi Prakash Babu, Donka Suresh Sajitha, Kethineni Kalyan, Gundlapalli Pavan Damu, Amooru Gangaiah Srinivasulu, Doddaga |
| description | Cholinesterase inhibitors and radical scavengers have been recognized as powerful symptomatic anti-Alzheimer's disease agents. Hence, the present study aimed to develop new triazineamides as potent anticholinesterase and antioxidant agents.
Triazineamide (
) derivatives were synthesized using cyanuric chloride via nucleophilic substitution followed by condensation. Ellman assay, 2,2-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) radical scavenging assay and molecular docking studies with Autodock 4.2.3 program were conducted.
Triazineamide
was assessed as a potent, selective and mixed-type dual inhibitor of acetylcholinesterase, with and IC
of 5.306 ± 0.002 μM, by binding simultaneously with the catalytic active and peripheral anionic sites of acetylcholinesterase, and it had strong 2,2-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) radical scavenging abilities.
These results suggest that triazineamides may be of interest to establish a structural basis for new anti-Alzheimer's disease agents. |
| doi_str_mv | 10.4155/fmc-2022-0200 |
| format | Article |
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Triazineamide (
) derivatives were synthesized using cyanuric chloride via nucleophilic substitution followed by condensation. Ellman assay, 2,2-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) radical scavenging assay and molecular docking studies with Autodock 4.2.3 program were conducted.
Triazineamide
was assessed as a potent, selective and mixed-type dual inhibitor of acetylcholinesterase, with and IC
of 5.306 ± 0.002 μM, by binding simultaneously with the catalytic active and peripheral anionic sites of acetylcholinesterase, and it had strong 2,2-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) radical scavenging abilities.
These results suggest that triazineamides may be of interest to establish a structural basis for new anti-Alzheimer's disease agents.</description><identifier>ISSN: 1756-8919</identifier><identifier>EISSN: 1756-8927</identifier><identifier>DOI: 10.4155/fmc-2022-0200</identifier><identifier>PMID: 36538284</identifier><language>eng</language><publisher>England</publisher><subject>Acetylcholinesterase - metabolism ; Alzheimer Disease - drug therapy ; Antioxidants - chemistry ; Antioxidants - pharmacology ; Cholinesterase Inhibitors - chemistry ; Cholinesterase Inhibitors - pharmacology ; Humans ; Molecular Docking Simulation ; Structure-Activity Relationship ; Sulfonic Acids - chemistry</subject><ispartof>Future medicinal chemistry, 2022-12, Vol.14 (23), p.1741-1753</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><cites>FETCH-LOGICAL-c249t-5c6f19c65c1a5eb2672e80bcacfdc5715ba762fd440fab0f5e2ac1e2d75c64d13</cites><orcidid>0000-0002-6578-3232 ; 0000-0002-1194-2445</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/36538284$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Vatturu, Murali</creatorcontrib><creatorcontrib>Rao, Kandrakonda Yelamanda</creatorcontrib><creatorcontrib>Yesu, Valaparla Bala</creatorcontrib><creatorcontrib>Basha, Shaik Jeelan</creatorcontrib><creatorcontrib>Guptha, Tanguturi Prakash</creatorcontrib><creatorcontrib>Babu, Donka Suresh</creatorcontrib><creatorcontrib>Sajitha, Kethineni</creatorcontrib><creatorcontrib>Kalyan, Gundlapalli Pavan</creatorcontrib><creatorcontrib>Damu, Amooru Gangaiah</creatorcontrib><creatorcontrib>Srinivasulu, Doddaga</creatorcontrib><title>Synthesis and in vitro assessment of anticholinesterase and antioxidant properties of triazineamide derivatives</title><title>Future medicinal chemistry</title><addtitle>Future Med Chem</addtitle><description>Cholinesterase inhibitors and radical scavengers have been recognized as powerful symptomatic anti-Alzheimer's disease agents. Hence, the present study aimed to develop new triazineamides as potent anticholinesterase and antioxidant agents.
Triazineamide (
) derivatives were synthesized using cyanuric chloride via nucleophilic substitution followed by condensation. Ellman assay, 2,2-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) radical scavenging assay and molecular docking studies with Autodock 4.2.3 program were conducted.
Triazineamide
was assessed as a potent, selective and mixed-type dual inhibitor of acetylcholinesterase, with and IC
of 5.306 ± 0.002 μM, by binding simultaneously with the catalytic active and peripheral anionic sites of acetylcholinesterase, and it had strong 2,2-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) radical scavenging abilities.
These results suggest that triazineamides may be of interest to establish a structural basis for new anti-Alzheimer's disease agents.</description><subject>Acetylcholinesterase - metabolism</subject><subject>Alzheimer Disease - drug therapy</subject><subject>Antioxidants - chemistry</subject><subject>Antioxidants - pharmacology</subject><subject>Cholinesterase Inhibitors - chemistry</subject><subject>Cholinesterase Inhibitors - pharmacology</subject><subject>Humans</subject><subject>Molecular Docking Simulation</subject><subject>Structure-Activity Relationship</subject><subject>Sulfonic Acids - chemistry</subject><issn>1756-8919</issn><issn>1756-8927</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2022</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kEtLAzEQgIMottQevcoevawm2c0-jlJ8QcGDeg7ZZEIj-6iZtFh_jb_FX2aW1s5lhplvhuEj5JLRm5wJcWs7nXLKeUo5pSdkykpRpFXNy9NjzeoJmSN-0BgZr-pCnJNJVois4lU-Jf5114cVoMNE9eb3J3F9snXBD4lCBMQO-pAMNg6D06uhdT1gAK8Q9vzYH76ciTlZ-2ENPjjAcSN4p74jrjpnIDHg3VYFtwW8IGdWtQjzQ56R94f7t8VTunx5fF7cLVPN8zqkQheW1boQmikBDS9KDhVttNLWaFEy0aiy4NbkObWqoVYAV5oBN2XczA3LZuR6fzf-9bmJb8vOoYa2VT0MG5Q8CmKciZJHNN2j2g-IHqxce9cpv5OMytG0jKblaFqOpiN_dTi9aTowR_rfa_YHRH1-0w</recordid><startdate>20221201</startdate><enddate>20221201</enddate><creator>Vatturu, Murali</creator><creator>Rao, Kandrakonda Yelamanda</creator><creator>Yesu, Valaparla Bala</creator><creator>Basha, Shaik Jeelan</creator><creator>Guptha, Tanguturi Prakash</creator><creator>Babu, Donka Suresh</creator><creator>Sajitha, Kethineni</creator><creator>Kalyan, Gundlapalli Pavan</creator><creator>Damu, Amooru Gangaiah</creator><creator>Srinivasulu, Doddaga</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><orcidid>https://orcid.org/0000-0002-6578-3232</orcidid><orcidid>https://orcid.org/0000-0002-1194-2445</orcidid></search><sort><creationdate>20221201</creationdate><title>Synthesis and in vitro assessment of anticholinesterase and antioxidant properties of triazineamide derivatives</title><author>Vatturu, Murali ; Rao, Kandrakonda Yelamanda ; Yesu, Valaparla Bala ; Basha, Shaik Jeelan ; Guptha, Tanguturi Prakash ; Babu, Donka Suresh ; Sajitha, Kethineni ; Kalyan, Gundlapalli Pavan ; Damu, Amooru Gangaiah ; Srinivasulu, Doddaga</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c249t-5c6f19c65c1a5eb2672e80bcacfdc5715ba762fd440fab0f5e2ac1e2d75c64d13</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2022</creationdate><topic>Acetylcholinesterase - metabolism</topic><topic>Alzheimer Disease - drug therapy</topic><topic>Antioxidants - chemistry</topic><topic>Antioxidants - pharmacology</topic><topic>Cholinesterase Inhibitors - chemistry</topic><topic>Cholinesterase Inhibitors - pharmacology</topic><topic>Humans</topic><topic>Molecular Docking Simulation</topic><topic>Structure-Activity Relationship</topic><topic>Sulfonic Acids - chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Vatturu, Murali</creatorcontrib><creatorcontrib>Rao, Kandrakonda Yelamanda</creatorcontrib><creatorcontrib>Yesu, Valaparla Bala</creatorcontrib><creatorcontrib>Basha, Shaik Jeelan</creatorcontrib><creatorcontrib>Guptha, Tanguturi Prakash</creatorcontrib><creatorcontrib>Babu, Donka Suresh</creatorcontrib><creatorcontrib>Sajitha, Kethineni</creatorcontrib><creatorcontrib>Kalyan, Gundlapalli Pavan</creatorcontrib><creatorcontrib>Damu, Amooru Gangaiah</creatorcontrib><creatorcontrib>Srinivasulu, Doddaga</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Future medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Vatturu, Murali</au><au>Rao, Kandrakonda Yelamanda</au><au>Yesu, Valaparla Bala</au><au>Basha, Shaik Jeelan</au><au>Guptha, Tanguturi Prakash</au><au>Babu, Donka Suresh</au><au>Sajitha, Kethineni</au><au>Kalyan, Gundlapalli Pavan</au><au>Damu, Amooru Gangaiah</au><au>Srinivasulu, Doddaga</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and in vitro assessment of anticholinesterase and antioxidant properties of triazineamide derivatives</atitle><jtitle>Future medicinal chemistry</jtitle><addtitle>Future Med Chem</addtitle><date>2022-12-01</date><risdate>2022</risdate><volume>14</volume><issue>23</issue><spage>1741</spage><epage>1753</epage><pages>1741-1753</pages><issn>1756-8919</issn><eissn>1756-8927</eissn><abstract>Cholinesterase inhibitors and radical scavengers have been recognized as powerful symptomatic anti-Alzheimer's disease agents. Hence, the present study aimed to develop new triazineamides as potent anticholinesterase and antioxidant agents.
Triazineamide (
) derivatives were synthesized using cyanuric chloride via nucleophilic substitution followed by condensation. Ellman assay, 2,2-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) radical scavenging assay and molecular docking studies with Autodock 4.2.3 program were conducted.
Triazineamide
was assessed as a potent, selective and mixed-type dual inhibitor of acetylcholinesterase, with and IC
of 5.306 ± 0.002 μM, by binding simultaneously with the catalytic active and peripheral anionic sites of acetylcholinesterase, and it had strong 2,2-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) radical scavenging abilities.
These results suggest that triazineamides may be of interest to establish a structural basis for new anti-Alzheimer's disease agents.</abstract><cop>England</cop><pmid>36538284</pmid><doi>10.4155/fmc-2022-0200</doi><tpages>13</tpages><orcidid>https://orcid.org/0000-0002-6578-3232</orcidid><orcidid>https://orcid.org/0000-0002-1194-2445</orcidid></addata></record> |
| fulltext | fulltext |
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| ispartof | Future medicinal chemistry, 2022-12, Vol.14 (23), p.1741-1753 |
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| source | MEDLINE; PubMed Central |
| subjects | Acetylcholinesterase - metabolism Alzheimer Disease - drug therapy Antioxidants - chemistry Antioxidants - pharmacology Cholinesterase Inhibitors - chemistry Cholinesterase Inhibitors - pharmacology Humans Molecular Docking Simulation Structure-Activity Relationship Sulfonic Acids - chemistry |
| title | Synthesis and in vitro assessment of anticholinesterase and antioxidant properties of triazineamide derivatives |
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