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Emerging Highlights on Natural Prodrug Molecules with Multifarious Therapeutic Perspectives
Published in Debarshi Kar Mahapatra, Cristóbal Noé Aguilar, A. K. Haghi, Applied Pharmaceutical Practice and Nutraceuticals, 2021
Mojabir Hussen Ansari, Vaibhav Shende, Debarshi Kar Mahapatra
Prontosil, also known as Prontosil rubrum, is a dark red color dye. It was initially given orally as a hydrochloride (HCl) salt but later preferred as a free base as it was less staining. Moreover, this dye is very insoluble in aqueous media and their recourse becomes extremely difficult. Over time, it was formulated to make it more water soluble. Recently, a library of organized, patented compounds has been seen for fabricating derivatives with a greater solubility and can be used in formulating injectables. Prontosil soluble (originally Streptozon S) came into practice through the chemical reaction among the diazotized sulphanilamide with the 2-acetamino-8-hydroxynaphthalene-3,6-disulphonic acid.7 Prontosil later changed into a prodrug form that is specifically used in the formation and improvisation of the sulfonamide molecules. In mixture with diaminopyrimidines, they inhibit the folate pathway in bacteria and are used widely for treating bacteria-oriented infections. In olden times, diaminopyrimi-dines were used along with sulphonamides besides for special indications (infectious diseases) or for the remedy of cystitis.8
Developments of Health Care: A Brief History of Medicine
Published in P. Mereena Luke, K. R. Dhanya, Didier Rouxel, Nandakumar Kalarikkal, Sabu Thomas, Advanced Studies in Experimental and Clinical Medicine, 2021
P. Mereena Luke, K. R. Dhanya, Tomy Muringayil Joseph, Józef T. Haponiuk, Didier Rouxel, S. Thomas
German bacteriologist Gerhard Domagk found the second magic bullet against streptococcal infection after years of systematic research in 1932. This was a red dye called Prontosil. With the aid of the new, powerful electron microscopes which had been in use since the early 1930s, scientists found that the active component was a sulfonamide from coal tar. Soon after French workers found that the Prontosil could be metabolized in the patient to sulfanilamide, which was the active antibacterial molecule. After 1935, this idea was to change when it was found that Prontosil could use against streptococcal infection. In 1936, British physician Leonard Colebrook and co-workers confirmed the effectiveness of both Prontosil and sulfanilamide in streptococcal septicemia [56]. The major befits of sulfonamide drugs was the rapid action, superior potency, broad antibacterial range, with lesser toxicity. The discovery of sulfonamides led to the development of drugs which cured gonorrhea, pneumonia, meningitis, and scarlet fever. In subsequent years many derivatives of sulfonamides, or sulfa drugs, were synthesized and tested for antibacterial and other activities. Most of the antibiotic classes [Penicillins, Macrolides, Fluoroquinolones, Tetracyclines, Aminoglycosides, Sulfonamides, Cephalosporins, Glycopeptides, Carbapenems, Lincosamide, etc.], were discovered and introduced to the market between 1940 and 1962. There are generally several antibiotics in each class that have been found over time or are improved versions of earlier types.
Antibiotics: The Need for Innovation
Published in Nathan Keighley, Miraculous Medicines and the Chemistry of Drug Design, 2020
Sulpha drugs are an example of antibiotics that affect bacterial cell metabolism. It was discovered in 1935 that a red dye called prontosil red was effective against bacteria in vivo (in other words in laboratory animals), but antibacterial effects were not observed in vitro; cultures in petri dishes were unaffected. It was later discovered that bacteria present in the small intestine of the animal metabolised prontosil to give the true antibiotic product called sulphanilamide. This process is illustrated in Figure 3.1. Prontosil was an early example of a pro-drug.
Synthesis, characterisation, biological evaluation and in silico studies of sulphonamide Schiff bases
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2020
Mustafa Durgun, Cüneyt Türkeş, Mesut Işık, Yeliz Demir, Ali Saklı, Ali Kuru, Abdussamat Güzel, Şükrü Beydemir, Suleyman Akocak, Sameh M. Osman, Zeid AlOthman, Claudiu T. Supuran
Some sulphonamide derivatives were screened for their antioxidant activity, which showed good results20–23. Sulphonamides chemically containing sulfamoyl (–SO2NH–) group are derivatives of amide. The first sulphonamide drug identified in 1932 was the prontosil and used as antibacterial agent and since then sulphonamides are most widely used in the world among groups of anti-infectives. Sulphonamides are a biologically significant group of compounds due to well absorption orally and excrete in urine, thus sulphonamides have less toxicity, increased reactivity and are cost-effective molecules24–26. Today, sulphonamides are widely used as antimicrobial27,28, anti-inflammatory29,30, anticancer31–36 and anti-viral agents as well as HIV protease inhibitor37, anti-obesity38, anti-thyroid39, and also act as a potent Carbonic anhydrase hCA inhibitors40,41.
Interaction of drugs with gut microbiota modulators
Published in Drug Metabolism Reviews, 2023
Of azo compounds, prontosil does not exhibit antibacterial activity in vitro. However, orally administered prontosil is transformed to sulfanilamide in the GI tract by gut bacteria azoreductase (Fouts et al. 1957; Gingell et al. 1971; Gingell and Bridges 1973). Prontosil is also metabolized in the liver and blood (Gingell et al. 1971; Gingell and Bridges 1973). However, intraperitoneally injected neoprotonsil is excreted via the bile without metabolism. Orally administered prontonsil and neoprontosil are mainly metabolized to sulfanilamide in the GI tract (Gingell et al. 1971). The metabolite sulfanilamide is absorbed into the body and alleviates systemic infection of pathogens in mice