Synthesis and Antimicrobial Activity of Some Novel Thiazoles, 1,3,4‐Thiadiazines, 1,3,4‐Thiadiazoles Incorporating Coumarin Moiety

Abdel‐Aziem, Anhar

doi:10.1002/jhet.2390

Cited by 18 publications

(9 citation statements)

References 21 publications

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“…Among the promising compounds that act like immunomodulators are the substituted 1,3,4-thiadiazines ( Table 1 ). A variety of biological activities has been reported for many thiadiazine derivatives, such as antimicrobial [ 38 , 39 , 40 , 41 ], antihelmintic [ 42 ], anti-inflammatory [ 43 , 44 ], analgesic [ 45 ], anticancer [ 45 , 46 ], tuberculostatic [ 47 ] and anti-aggregant [ 48 , 49 , 50 ] activities ( Table 1 ).…”

Section: Methodsmentioning

confidence: 99%

Immunomodulatory Action of Substituted 1,3,4-Thiadiazines on the Course of Myocardial Infarction

et al. 2018

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This review focuses on the biological action of the compounds from the group of substituted 1,3,4-thiadiazines on stress response and myocardial infarction. The aim of this review is to propose the possible mechanisms of action of 1,3,4-thiadiazines and offer prospectives in the development of new derivatives as therapeutic agents. It is known, that compounds that have biological effects similar to those used as antidepressants can down-regulate the secretion of proinflammatory cytokines, up-regulate the release of anti-inflammatory ones and affect cell recruitment, which allows them to be considered immunomodulators as well. The results of pharmacological evaluation, in silico studies, and in vivo experiments of several compounds from the group of substituted 1,3,4-thiadiazines with antidepressant properties are presented. It is proposed that the cardioprotective effects of substituted 1,3,4-thiadiazines might be explained by the peculiarities of their multi-target action: the ability of the compounds to interact with various types of receptors and transporters of dopaminergic, serotonergic and acetylcholinergic systems and to block the kinase signal pathway PI3K-AKT. The described effects of substituted 1,3,4-thiadiazines suggest that it is necessary to search for a new agents for limiting the peripheral inflammatory/ischemic damage through the entral mechanisms of stress reaction and modifying pro-inflammatory cytokine signaling pathways in the brain.

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Section: Methodsmentioning

confidence: 99%

Immunomodulatory Action of Substituted 1,3,4-Thiadiazines on the Course of Myocardial Infarction

et al. 2018

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“…Ethyl-5-[(5-bromo-2-hydroxybenzylidene)-hydrazono]-4-phenyl-4,5-dihydro- [1,3,4]thiadiazole-2-carboxylate (11a). ,48.33;H,3.38;Br,17.86;N,12.53;S,7.17.…”

Section: Synthesis Of Coumarin Derivatives 4a-dmentioning

confidence: 99%

“…,48.33;H,3.38;Br,17.86;N,12.53;S,7.17. Found: C,48.42;H,3.25;Br,17.75;N,12.64;S,-hydrazono]-4-phenyl-4,5-dihydro- [1,3,4] (3), 415 (4). Anal.…”

Section: Synthesis Of Coumarin Derivatives 4a-dmentioning

confidence: 99%

“…Calcd for C 20 H 13 BrN 4 O 2 S 2 (485.38): C,49.49;H,2.70;Br,16.46;N,11.54;S,13.21. Found: C,49.39;H,2.81;Br,16.34;N,11.46;S,-hydrazono]-4-phenyl-4,5-dihydro- [1,3,4] 3.24;Br,15.09;N,10.58;S,6.06. Found: C,58.87;H,3.36;Br,15.22;N,10.70;S,6.18.…”

Section: Synthesis Of Coumarin Derivatives 4a-dmentioning

confidence: 99%

“…Due to the interesting activity of coumarins as biological agents, considerable attention has been focused on this class of heterocycles. The pharmaceutical importance of these compounds lies in the fact that they can be utilized as anti‐inflammatory , anticancer , anticoagulant , antimicrobial, and antioxidant activities . A literature survey revealed that a special attention was given to 1,3,4‐thiadiazole derivatives that proved to have promising biological activities such as antimicrobial , anticancer , antioxidant , antiamoebic , anticonvulsant , anti‐inflammatory, and analgesic activities .…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Synthesis and Evaluation of Antimicrobial Activity of Some Novel Heterocyclic Compounds from 5‐Bromosalicylaldehyde

Abdel‐Aziem

Baaiu

Abdelhamid

2017

Journal of Heterocyclic Chem

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A novel series of coumarins, thiadiazoles, thiazoles, and pyridines were synthesized via reaction of 5‐bromosalicylaldehyde with different reagents. Thus, 5‐bromosalicylaldehyde 1 was reacted with compounds 2a–d affording iminocoumarins 3a–d, which on hydrolysis with 10% hydrochloric acid, afforded coumarins 4a–d, respectively. On the other hand, reaction of 1 with benzylhydrazinecarbodithioate 5 afforded derivative 6, which reacted with hydrazonoyl halides 7a–f, afforded 1,3,4‐thiadiazoles 11a–f, respectively. Moreover, thiazoles 15 and 16 were obtained via reaction of 1 with thiocarbohydrazide 13 and hydrazonoyl halides. However, condensation of 2‐acetyl‐5‐bromobenzofuran 17 with benzaldehyde afforded chalcone 18, which reacted with pyridiniumbromides 19a–c, afforded pyridines 20a–c, respectively. Furthermore, pyridines 21–24 were synthesized from the reaction of chalcone 18 with different active methylene compounds. Reaction of 24 with ethylchloroacetate, chloroacetone, and chloroacetonitrile afforded thienopyridines 26a–c, respectively. The structures of the newly synthesized compounds were established based on their spectral data and elemental analyses. Also, selected newly synthesized compounds were screened for their antimicrobial activity against various microorganisms by disk diffusion method.

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Convenient Synthesis and Biological Activity of Mono and Diacyl 2,5‐Dimercapto‐1,3,4‐thiadiazole Derivatives

Jasiak

Kudelko

Wróblowska

et al. 2017

Journal of Heterocyclic Chem

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Synthesis and Antimicrobial Activity of Some Novel Thiazoles, 1,3,4‐Thiadiazines, 1,3,4‐Thiadiazoles Incorporating Coumarin Moiety

Cited by 18 publications

References 21 publications

Immunomodulatory Action of Substituted 1,3,4-Thiadiazines on the Course of Myocardial Infarction

Immunomodulatory Action of Substituted 1,3,4-Thiadiazines on the Course of Myocardial Infarction

Synthesis and Evaluation of Antimicrobial Activity of Some Novel Heterocyclic Compounds from 5‐Bromosalicylaldehyde

Convenient Synthesis and Biological Activity of Mono and Diacyl 2,5‐Dimercapto‐1,3,4‐thiadiazole Derivatives

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