Special Issue: Sulfonamides

Supuran, Claudiu T.

doi:10.3390/molecules22101642

Cited by 84 publications

(61 citation statements)

References 47 publications

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“…Sulfonamides constitute an important class of drugs containing many types of pharmacological agents with broad-spectrum bacteriostatic activity. Sulfonamides interrupt the synthesis of folic acid, interfering with the dihydropteroate synthase and dihydrofolate reductase enzymes of bacteria (and protozoa) and inhibiting bacterial growth [179,180]. The sulfadoxine-pyrimethamine combination is used in some settings for the treatment of uncomplicated malaria in pregnant women, and it is the only drug currently recommended for intermittent preventive therapy during pregnancy [181].…”

Section: Sulfonamidesmentioning

confidence: 99%

The Use of Antimalarial Drugs against Viral Infection

et al. 2020

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In recent decades, drugs used to treat malaria infection have been shown to be beneficial for many other diseases, including viral infections. In particular, they have received special attention due to the lack of effective antiviral drugs against new emerging viruses (i.e., HIV, dengue virus, chikungunya virus, Ebola virus, etc.) or against classic infections due to drug-resistant viral strains (i.e., human cytomegalovirus). Here, we reviewed the in vitro/in vivo and clinical studies conducted to evaluate the antiviral activities of four classes of antimalarial drugs: Artemisinin derivatives, aryl-aminoalcohols, aminoquinolines, and antimicrobial drugs.

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Section: Sulfonamidesmentioning

confidence: 99%

The Use of Antimalarial Drugs against Viral Infection

et al. 2020

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“…An important pharmacophore group is a sulfonamide moiety characteristic for many chemical compounds used in medicine. Its importance stems from diverse biological activities such as antibacterial, anti-malarial, hypotensive, diuretic, hypoglycemic, anti-thyroid, anti-parasitic, anti-inflammatory, and anti-glaucomatous activity [5,22]. Furthermore, many studies from various scientific centers have shown that sulfonamides may exhibit an antitumor effect.…”

Section: Introductionmentioning

confidence: 99%

The Effect of Novel 7-methyl-5-phenyl-pyrazolo[4,3-e]tetrazolo[4,5-b][1,2,4]triazine Sulfonamide Derivatives on Apoptosis and Autophagy in DLD-1 and HT-29 Colon Cancer Cells

Gornowicz

Szymanowska

Bielawski

et al. 2020

IJMS

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The discovery of cytotoxic drugs is focused on designing a compound structure that directly affects cancer cells without an impact on normal cells. The mechanism of anticancer activity is mainly related with activation of apoptosis. However, recent scientific reports show that autophagy also plays a crucial role in cancer cell progression. Thus, the objective of this study was to synthesize 7-methyl-5-phenyl-pyrazolo[4,3-e]tetrazolo[4,5-b][1,2,4]triazine utilizing nucleophilic substitution reaction at the position N1. The biological activity of tested compounds was assessed in DLD-1 and HT-29 cell lines. The induction of apoptosis was confirmed by Annexin V binding assay and acridine orange/ethidium bromide staining. The loss of mitochondrial membrane potential and caspase-8 activity was estimated using cytometer flow analysis. The concentration of p53, LC3A, LC3B and beclin-1 was measured using the ELISA technique. Our study revealed that anticancer activity of 7-methyl-5-phenyl-pyrazolo[4,3-e]tetrazolo[4,5-b][1,2,4]triazine derivatives is related with initiation of apoptosis occur on the intrinsic pathway with mitochondrial membrane decrease and extrinsic with increase of activity of caspase-8. Moreover, a decrease in beclin-1, LC3A, and LC3B were observed in two cell lines after treatment with novel compounds. This study showed that novel 7-methyl-5-phenyl-pyrazolo[4,3-e]tetrazolo[4,5-b][1,2,4]triazine derivatives might be a potential strategy in colon cancer treatment.

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“…Sulfonamides constitute an important family of drugs that have been extensively applied in human and veterinary medicine due to their general stability, bioavailability, and ease of preparation. 1 The compounds of this class (Fig. 1) have been clinically in use for decades, and some of which showed potent antitumor activity.…”

mentioning

confidence: 99%

Bioorthogonal release of sulfonamides and mutually orthogonal liberation of two drugs

et al. 2018

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Sulfonamide derivatives have been used in pharmaceutics for decades. Here we report a new approach to release sulfonamides efficiently using a bioorthogonal reaction of sulfonyl sydnonimines and dibenzoazacyclooctyne (DIBAC). The second-order rate constant of the cycloaddition reaction can be up to 0.62 M−1 s−1, and the reactants are highly stable under physiological conditions. Most significantly, we also discovered the mutual orthogonality between the sydnonimine–DIBAC and benzonorbornadiene–tetrazine cycloaddition pairs, which can be used for selective and simultaneous liberation of sulfonamide and primary amine drugs.

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Special Issue: Sulfonamides

Cited by 84 publications

References 47 publications

The Use of Antimalarial Drugs against Viral Infection

The Use of Antimalarial Drugs against Viral Infection

The Effect of Novel 7-methyl-5-phenyl-pyrazolo[4,3-e]tetrazolo[4,5-b][1,2,4]triazine Sulfonamide Derivatives on Apoptosis and Autophagy in DLD-1 and HT-29 Colon Cancer Cells

Bioorthogonal release of sulfonamides and mutually orthogonal liberation of two drugs

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