l-Proline-catalysed facile green protocol for the synthesis and antimycobacterial evaluation of [1,4]-thiazines

Indumathi, Sethuraman; Perumal, S.; Banerjee, D.; Yogeeswari, Perumal; Sriram, Dharmarajan

doi:10.1016/j.ejmech.2009.09.001

Cited by 24 publications

(9 citation statements)

References 20 publications

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“…Most of these compounds have high antitubercular activity and are effective in microgram concentration, thus 1,3-thiazine derivatives have potential antimycobacterial activities [53]. The ethyl 6-(4-chlorobenzoyl)-1,1-dioxo-3,5-diaryl derivatives of the 1,4-thiazinane-2-carboxylates are also highly active compound against different species of mycobacterium that are highly resistant to other drugs [54]. They can be obtained very easily by treating ethyl 2-[(2-oxo-2-arylethyl)sulfonyl]acetates with various branched aromatic aldehydes and amines and the reaction is catalyzed by l -proline [54].…”

Section: Biological Activities Of Thiazine and Benzothiazine Derivmentioning

confidence: 99%

“…The ethyl 6-(4-chlorobenzoyl)-1,1-dioxo-3,5-diaryl derivatives of the 1,4-thiazinane-2-carboxylates are also highly active compound against different species of mycobacterium that are highly resistant to other drugs [54]. They can be obtained very easily by treating ethyl 2-[(2-oxo-2-arylethyl)sulfonyl]acetates with various branched aromatic aldehydes and amines and the reaction is catalyzed by l -proline [54]. The advantages of this method are that the products (1,4-thiazines) are obtained in good yield and it is a green synthesis method [54].…”

Section: Biological Activities Of Thiazine and Benzothiazine Derivmentioning

confidence: 99%

“…They can be obtained very easily by treating ethyl 2-[(2-oxo-2-arylethyl)sulfonyl]acetates with various branched aromatic aldehydes and amines and the reaction is catalyzed by l -proline [54]. The advantages of this method are that the products (1,4-thiazines) are obtained in good yield and it is a green synthesis method [54].…”

Section: Biological Activities Of Thiazine and Benzothiazine Derivmentioning

confidence: 99%

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Bioactive Thiazine and Benzothiazine Derivatives: Green Synthesis Methods and Their Medicinal Importance

Badshah

Akhtar

2016

Molecules

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Abstract:Thiazines are a group of heterocyclic organic compounds that are still largely unexplored for their pharmacological activities. There are different available methods for the synthesis of thiazine derivatives in the literature. In this review, we discuss available methods of thiazine preparation through green synthesis methods. Beside their synthesis, many thiazine derivatives are biologically active and play an important role in the treatment of various diseases and show promising results of varying degrees, where they act as antibacterial, antifungal, antitumor, antimalarial, antineoplastic, antiviral, anti-inflammatory, analgesic and anticancer agents and thus they represent an interesting class of heterocyclic medicinal compounds worthy of further exploration.

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Section: Biological Activities Of Thiazine and Benzothiazine Derivmentioning

confidence: 99%

Section: Biological Activities Of Thiazine and Benzothiazine Derivmentioning

confidence: 99%

Section: Biological Activities Of Thiazine and Benzothiazine Derivmentioning

confidence: 99%

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Bioactive Thiazine and Benzothiazine Derivatives: Green Synthesis Methods and Their Medicinal Importance

Badshah

Akhtar

2016

Molecules

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“…Amsacrine which is a 9-anilinoacridine derivative with primary DNA-inter collating agent, which is more signi icant and the chromophore intercalates with DNA base pairs (Rastogi et al, 2002;Kalira-jan et al, 2012a). Likewise, thiazine derivatives also reported for various biological activities (Sondhi et al, 2005;Plouvier et al, 1994) like antimicrobial (Kalirajan et al, 2009), anticancer (Kalirajan et al, 2019a) analgesic, antiin lammatory (Sondhi et al, 2005), antimycobacterial (Indumathi et al, 2009)etc.…”

Section: Introductionmentioning

confidence: 98%

Activity of Thiazine substituted 9-anilinoacridines against Corona virus (COVID19): An In-silico approach

Rajagopal¹,

Varakumar²,

Aparna³

et al. 2020

ijrps

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Coronavirus Disease 2019 (COVID-19), a life-threatening viral disease affected first in Wuhan, China, and quickly spread to more than 200 countries in the world in the year 2020. So many scientists are trying to discover novel drugs and vaccines for coronavirus and treatment for COVID-19. In the present article, in-silico studies have been performed to explore the binding modes of Thiazine substituted 9-anilinoacridines (1a-z) against SARS CoV 2 main protease (PDB id - 5R82) targeting the coronavirus using Schrodinger suit 2019-4. The molecular docking studies are performed by Glide module, in-silico ADMET screening was performed by Qik prop module, and the binding free energy of ligands was calculated using PRIME MM-GB/SA module of Schrodinger suite 2019-4, Maestro 21.2 version. From the in-silico results, Thiazine substituted 9-anilinoacridines like 1m, 1j, 1s and 1b are significantly active against SARS CoV 2 main protease with Glide score more than -5.4 when compared with the currently recommended drug for COVID19, Hydroxychloroquine (G score -5.47). The docking results of the Thiazine substituted 9-anilinoacridines exhibited similar mode of interactions with COVID19 and the residues GLN19, THR24, THR25, THR26, LEU27, HIE41, SER46, MET49, ASN142, GLN143, HIE164, MET165, ASP187, ARG188 and GLN189, play a crucial role in binding with ligands.

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“…In an effort to discover new and effective chemotherapeutic agent for the treatment of TB, the antimycobacterial activities of various phthalazin-4-yl acetamides [ 25 ], thiazolylthiosemicarbazones [ 26 ], chromeno[3,2-c]pyridine-3-yl derivatives [ 27 ], [1,4]-thiazines [ 28 ], thieno-[2,3-b]thiophene [ 29 ], spirocyclohexanones derivatives [ 30 ], thieno[3,2-b]indoles [ 31 ], furan-2-yl derivatives [ 32 ], thiadiazoles derivatives [ 33 ], imidazole derivatives [ 34 , 35 ], acyclic deoxy monosaccharide derivatives [ 36 ], benzoic acid hydrazine class [ 37 ], calanolide A, a naturally occurring coumarin derivatives [ 38 , 39 ], purine derivatives [ 40 , 41 ], pyrrole derivatives [ 42 , 43 ], benzoxazine derivatives [ 44 ], diterpenoids derived from plants [ 45 , 46 ], and quinoline and quinoxaline derivatives [ 47 ] have been reported.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Structural Activity Relationship Study of Antitubercular Carboxamides

Ugwu

Ezema

Eze

et al. 2014

International Journal of Medicinal Chemistry

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The unusual structure and chemical composition of the mycobacterial cell wall, the tedious duration of therapy, and resistance developed by the microorganism have made the recurrence of the disease multidrug resistance and extensive or extreme drug resistance. The prevalence of tuberculosis in synergy with HIV/AIDS epidemic augments the risk of developing the disease by 100-fold. The need to synthesize new drugs that will shorten the total duration of effective treatment and/or significantly reduce the dosage taken under DOTS supervision, improve on the treatment of multidrug-resistant tuberculosis which defies the treatment with isoniazid and rifampicin, and provide effective treatment for latent TB infections which is essential for eliminating tuberculosis prompted this review. In this review, we considered the synthesis and structure activity relationship study of carboxamide derivatives with antitubercular potential.

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l-Proline-catalysed facile green protocol for the synthesis and antimycobacterial evaluation of [1,4]-thiazines

Cited by 24 publications

References 20 publications

Bioactive Thiazine and Benzothiazine Derivatives: Green Synthesis Methods and Their Medicinal Importance

Bioactive Thiazine and Benzothiazine Derivatives: Green Synthesis Methods and Their Medicinal Importance

Activity of Thiazine substituted 9-anilinoacridines against Corona virus (COVID19): An In-silico approach

Synthesis and Structural Activity Relationship Study of Antitubercular Carboxamides

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