Nanoemulsion composed of 10-(4,5-dihydrothiazol-2-yl)thio)decan-1-ol), a synthetic analog of 3-alkylpiridine marine alkaloid: development, characterization, and antimalarial activity

Silva, Marina Goulart da; Cardoso, Jéssica Ferreira; Perasoli, Fernanda Barçante; Branquinho, Renata Tupinambá; Mourão, Renata Silva; Tavares, Harley Da Silva; Xocaira, Maria Luiza Costa Trench; Guimarães, Daniel Silqueira Martins; Viana, Gustavo Henrique Ribeiro; Varotti, Fernando de Pilla; Silva, Gisele Rodrigues Da

doi:10.1016/j.ejps.2020.105382

Cited by 14 publications

(8 citation statements)

References 28 publications

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“…Various chemical compounds are possible by virtue of Benzoin condensation and Stetter reaction, in which the thiazolium salts serve as catalyst. 4 Thiazoles containing compounds have different biological activities like antibacterial, 5 anticancer, 6 antimalarial, 7 antifungal, 8 anti-inflammatory, 9 antiepileptic, 10 and antioxidants. 11…”

Section: Introductionmentioning

confidence: 99%

Thiazoles: A Retrospective Study on Synthesis, Structure-activity Relationship and Therapeutic Significance

Sharma¹,

Devgun²,

Narang³

et al. 2022

IJPER

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Thiazole or 1,3-thiazole is a distinct heterocyclic compound which incorporates sulphur and nitrogen atoms. It is a vital framework present in numerous pharmacologically active compounds, be it of natural origin or of synthetic nature. Many thiazoles having antitumor and antiviral activities, originate from microbes and marine organisms. A variety of synthetic drugs, having thiazole group, like antimicrobial sulfathiazole, antibiotic penicillin, antidepressant pramipexole, antineoplastic agent bleomycin, antiretroviral drug ritonavir, histamine H 2 receptor antagonist nizatidine, anti-inflammatory drug meloxicam, antifungal stilbene derivatives have been in the markets for quite some time. Hofmann and Hantzsch laid the groundwork for further development in the field of thiazole chemistry. The interaction of α-haloketones or α-halogenaldehyde and thioamide to obtain thiazoles is beautifully described by Hantzsch. Various studies have reported methods for the synthesis of the thiazoles; thioforamide, thiourea, α-thiocyanotoketones, and vinyl bromide have been extensively employed to synthesize thiazoles. The thiazoles have immense potential and this study tries to enlighten the crucial role of thiazoles for the betterment of society. The review provides different directions in the synthesis of novel thiazoles and also reveals diverse targets for augmentation in the field of designing of novel thiazoles.

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Section: Introductionmentioning

confidence: 99%

Thiazoles: A Retrospective Study on Synthesis, Structure-activity Relationship and Therapeutic Significance

Sharma¹,

Devgun²,

Narang³

et al. 2022

IJPER

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“…A similar experiment was carried with 10-(4,5-dihydrothiazol-2-yl)thio)decan-1-ol) ( 35 ), a derivative of 3-alkylpiridine (naturally found in marine sponge Theonella sp. ), against the P. berghei infection in mice [ 37 ]. According to the authors, the treatment with 50 mg/kg suppressed the parasitemia by 20% in comparison to the untreated group.…”

Section: Marine Alkaloids With Biological Activity In Vivomentioning

confidence: 99%

Marine Alkaloids: Compounds with In Vivo Activity and Chemical Synthesis

Munekata¹,

Pateiro²,

Conté-Júnior

et al. 2021

Marine Drugs

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Marine alkaloids comprise a class of compounds with several nitrogenated structures that can be explored as potential natural bioactive compounds. The scientific interest in these compounds has been increasing in the last decades, and many studies have been published elucidating their chemical structure and biological effects in vitro. Following this trend, the number of in vivo studies reporting the health-related properties of marine alkaloids has been increasing and providing more information about the effects in complex organisms. Experiments with animals, especially mice and zebrafish, are revealing the potential health benefits against cancer development, cardiovascular diseases, seizures, Alzheimer’s disease, mental health disorders, inflammatory diseases, osteoporosis, cystic fibrosis, oxidative stress, human parasites, and microbial infections in vivo. Although major efforts are still necessary to increase the knowledge, especially about the translation value of the information obtained from in vivo experiments to clinical trials, marine alkaloids are promising candidates for further experiments in drug development.

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“…The study provide by Silva et al (2020) developed an O / W nanoemulsion for oral administration containing the antimalarial thiazoline. The system consists of thiazoline, a water-soluble substance, little aqueous hydrophobic, oleic acid (solubilizing agent), paraben solution (methylparaben and propylparaben in propylene glycol) (preservative) and butylhydroxyanisole (antioxidant), as an oily phase; and Solutol HS 15 (surfactant) and ultrapure water, as an aqueous phase.…”

Section: Pharmaceutical Nanotechnologymentioning

confidence: 99%

“… Úlcer Oral Lin et al, 2012 NE Thiazoline oleic acid (2.75 g), paraben in a 6% (w / v) solution of methylparaben and 3% (w / v) of propylparaben in propylene glycol (0.22 g), butylhydroxyanisole (0.001 g) 0, Solutol HS 15 (1.5 g) as an organic phase plus ultrapure water (5.97 g) that made up the aqueous phase. Malária Oral Silva et al, 2020 NE02 Oligonucleotide CpG Double-chain cationic surfactant (DODAC), class B oligonucleotide - murine TLR9 agonist (TLR9 / CpG - ODN 1826), sterile water H5N1 Intramuscular WANG et al, 2020 Rif NE Rifampicin rifampicin (0.1% w / w), oleic acid (1.0% w / w), polysorbate 80 (0.9% w / w) Mili-Q water Ocular tuberculosis eyepiece Henostroza et al, 2020 NE2b acyclovir Water (w / w), ACV 0.25% w / w, polaxamer 407 15.3% (w / w), polaxamer 188 1.33% (w / w) Transcutol®P (w / w), Triacetin (w / w) Herpes eyepiece Mahboobian et al, 2020 NE (Nanoemulsion); SQVM NE (Nanoemulon carried with siquinavir mesylate); Lf-IDV-NEs (idinavir and lactoferrin nanoemulsion); CUR NE (Curcumin Nanoemulsion); CLN (cefuroxime nanoemulsion); Baicalin NE (baicalin nanoemulsion; HBV (chronic hepatitis B); HIV (human immunodeficiency virus); Neuro AIDS (acquired immunodeficiency syndrome); NE2b (acyclovir nanoemulsion); NE02 (nanoemulsion) containing oligonucleotide CpG); Rif NE (Ripamficin Nanoemulsion). …”

Section: Pharmaceutical Nanotechnologymentioning

confidence: 99%

Nanotechnological strategies for systemic microbial infections treatment: A review

Ramos

Santos

Silva

et al. 2020

International Journal of Pharmaceutics

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Nanoemulsion composed of 10-(4,5-dihydrothiazol-2-yl)thio)decan-1-ol), a synthetic analog of 3-alkylpiridine marine alkaloid: development, characterization, and antimalarial activity

Cited by 14 publications

References 28 publications

Thiazoles: A Retrospective Study on Synthesis, Structure-activity Relationship and Therapeutic Significance

Thiazoles: A Retrospective Study on Synthesis, Structure-activity Relationship and Therapeutic Significance

Marine Alkaloids: Compounds with In Vivo Activity and Chemical Synthesis

Nanotechnological strategies for systemic microbial infections treatment: A review

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