In Pursuit of Multicomponent Crystals of the Sulfa Drugs Sulfapyridine, Sulfathiazole, and Sulfamethoxazole

2021 ◽  
Author(s):  
Matthew C. Scheepers ◽  
Andreas Lemmerer
Keyword(s):  
Sulfa Drugs

Synthesis, Characterization and Thermal studies of Novel Organomercury Driven from Sulfa Drugs Part 1

2011 ◽  
Vol 7 (2) ◽  
pp. 1338-1347
Author(s):  
Tarek Ali Fahad ◽  
Shaker.A.N. AL-Jadaan
Keyword(s):  
Thermal Decomposition ◽  
Thermal Behavior ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Thermal Studies ◽  
Spectroscopic Techniques ◽  
Sulfa Drugs ◽  
Acid Base ◽  
Ph Values ◽  
Multi Stage

Two new heterocyclic Organmercury compounds   were prepared from the reaction of Sulfamethaxazole and Sulfadiazine with 4-acetaminophenol as a coupler and separated as solids with characteristic colors. these compounds were characterized by F.T.IR-spectroscopy 1H-NMR , Micro-elemental Analysis and UV-Vis spectroscopic techniques . The work involves a study of acid – base properties compounds at different pH values, the ionization and protonation constants were calculated. The thermal behavior of these two compounds   were investigated on the basis of thermogravimetric (TGA) and differential thermogravimetric (DTG) analyses, Thermal decomposition of these compounds is multi-stage processes.

scholarly journals Synthesis, characterization, and biological evaluation of some 4-((thiophen-2-yl-methylene)amino)benzenesulfonamide metal complexes

2021 ◽  
Vol 10 (1) ◽  
Author(s):  
E. Vijaya Sekhar ◽  
Subhas S. Karki ◽  
Javarappa Rangaswamy ◽  
Mahesh Bhat ◽  
Sujeet Kumar
Keyword(s):  
Escherichia Coli ◽  
Schiff Base ◽  
Aspergillus Niger ◽  
Metal Complexes ◽  
Antimicrobial Properties ◽  
Azomethine Nitrogen ◽  
Diffusion Method ◽  
Sulfa Drugs ◽  
Zone Of Inhibition ◽  
Penicillium Rubrum

Abstract Background Sulfonamides (sulfa drugs) and the metals like mercury, copper, and silver bear antimicrobial properties. The discovery of broad-spectrum antibiotics such as penicillins, cephalosporins, and fluoroquinolones has reduced their use. However, in some instances these drugs are the first-line treatment. The metal-based sulfonamide (e.g., silver sulfadiazine) is considered as first choice treatment in post-burn therapy while the use of silver nanoparticle-cephalexin conjugate to cure Escherichia coli infection explains the synergistic effect of sulfa drugs and their metal conjugates. With growing interest in metal-based sulfonamides and the Schiff base chemistry, it was decided to synthesize sulfonamide Schiff base metal complexes as antioxidant and antimicrobial agent. Results The Fe (III), Ru (III), Co (II), Ni (II), Cu (II), Pd (II), Zn (II), Cd (II), and Hg (II) metal complexes of 4-((thiophen-2-ylmethylene)-amino)-benzenesulfonamide (TMABS) were prepared and studied for thermal stability, geometry, and other electronic properties. The ligand TMABS (Schiff base) and its metal complexes were screened in-vitro for 2,2-diphenyl-1-picrylhydrazyl (DPPH) free radical scavenging and antimicrobial properties against Gram-positive (+ve) Bacillus subtilis (MTCC-441), Staphylococcus aureus (MTCC 7443), Gram-negative (-ve) Escherichia coli (MTCC 40), Salmonella typhi (MTCC 3231), and fungal strains Aspergillus niger (MTCC-1344) and Penicillium rubrum by agar well diffusion method. Results summarized in Tables 3, 4, and 5 represent the inhibitory concentration (IC50) in micromole (μM). The zone of inhibition (ZI) in millimeter (mm) represents antimicrobial properties of TMABS and its metal complexes. Conclusions The synthesized sulfanilamide Schiff base (TMABS) behaved as a neutral and bidentate ligand coordinating with metal ions through its azomethine nitrogen and thiophene sulfur to give complexes with coordination number of 4 and 6 (Fig. 3). The nucleophilic addition of sulfanilamide amino group (–NH2) group to carbonyl carbon (>C=O) of benzaldehyde gave sulfanilamide Schiff base (imine) (Fig. 2). All the metal complexes were colored and stable at room temperature. With IC50 of 9.5 ± 0.1 and 10.0 ± 0.7 μM, the Co, Cu, and Pd complexes appeared better antioxidant than the ligand TMABS (155.3±0.1 μM). The zone of inhibition (ZI) of Hg (28 mm) and Ru complexes (20 mm) were similar to the ligand TMABS (20 mm) against Aspergillus niger (MTCC-1344) as in Figs. 4, 5, and 6. None of the synthesized derivatives had shown better antimicrobial properties than the standard streptomycin sulfate and fluconazole.

scholarly journals Vitamin B3confers resistance to sulfa drugs inSaccharomyces cerevisiae

2005 ◽  
Vol 251 (1) ◽  
pp. 137-141 ◽  
Author(s):  
Olga Kornfeld ◽  
Brian P. Nichols
Keyword(s):  
Sulfa Drugs

Sulfa Drugs and the Treatment of Wounds

Science ◽  
1942 ◽  
Vol 95 (2455) ◽  
pp. 8-10
Author(s):  
Jane Stafford
Keyword(s):  
Sulfa Drugs ◽  
Treatment Of Wounds

Behind the Sulfa Drugs

1943 ◽  
Vol 36 (6) ◽  
pp. 464
Author(s):  
&NA; &NA;
Keyword(s):  
Sulfa Drugs

scholarly journals Reversal of Azole Resistance inCandida albicansby Sulfa Antibacterial Drugs

2017 ◽  
Vol 62 (3) ◽  
Author(s):  
Hassan E. Eldesouky ◽  
Abdelrahman Mayhoub ◽  
Tony R. Hazbun ◽  
Mohamed N. Seleem
Keyword(s):  
Treatment Options ◽  
Antifungal Drugs ◽  
Infection Model ◽  
Azole Resistance ◽  
Global Public Health ◽  
Sulfa Drugs ◽  
Antibacterial Drugs ◽  
Content Type

ABSTRACTInvasive candidiasis presents an emerging global public health challenge due to the emergence of resistance to the frontline treatment options, such as fluconazole. Hence, the identification of other compounds capable of pairing with fluconazole and averting azole resistance would potentially prolong the clinical utility of this important group. In an effort to repurpose drugs in the field of antifungal drug discovery, we explored sulfa antibacterial drugs for the purpose of reversing azole resistance inCandida. In this study, we assembled and investigated a library of 21 sulfa antibacterial drugs for their ability to restore fluconazole sensitivity inCandida albicans. Surprisingly, the majority of assayed sulfa drugs (15 of 21) were found to exhibit synergistic relationships with fluconazole by checkerboard assay with fractional inhibitory concentration index (ΣFIC) values ranging from <0.0312 to 0.25. Remarkably, five sulfa drugs were able to reverse azole resistance in a clinically achievable range. The structure-activity relationships (SARs) of the amino benzene sulfonamide scaffold as antifungal agents were studied. We also identified the possible mechanism of the synergistic interaction of sulfa antibacterial drugs with azole antifungal drugs. Furthermore, the ability of sulfa antibacterial drugs to inhibitCandidabiofilm by 40%in vitrowas confirmed. In addition, the effects of sulfa-fluconazole combinations onCandidagrowth kinetics and efflux machinery were explored. Finally, using aCaenorhabditis elegansinfection model, we demonstrated that the sulfa-fluconazole combination does possess potent antifungal activityin vivo, reducingCandidain infected worms by ∼50% compared to the control.

Sign in / Sign up

Export Citation Format

Share Document