Delving into the Latest Updates on Sulfadiazine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

2-sulfanilamidopyrimidine, 2-sulfanilylaminopyrimidine, 4-amino-N-2-pyrimidinylbenzenesulfonamide

+ [18]

Target

bacterial DHPS

Mechanism

bacterial DHPS inhibitors(Bacterial dihydropteroate synthase inhibitors)

Therapeutic Areas

Infectious Diseases

Active Indication

Bacterial Infections

Inactive Indication-

Originator Organization

Lederle Laboratories

Active Organization

Youhua Pharmaceutical (Leshan) Co Ltd

Vita Health Products, Inc.

Inactive Organization

Eli Lilly & Co.

AbbVie, Inc.

Lederle Laboratories

Drug Highest PhaseApproved

First Approval Date

US (11 Aug 1941),

Bacterial Infections

RegulationOrphan Drug (JP)

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Structure

Molecular FormulaC10H10N4O2S

InChIKeySEEPANYCNGTZFQ-UHFFFAOYSA-N

CAS Registry68-35-9

In this study, the absorption and fluorescence characteristics of sulfa drugs, specifically Sulfadiazine (SDZ), Sulfamerazine (SMZ), and Sulfamethazine (STZ), were examined across a pH range of 1-14. The absorption and fluorescence spectra of these sulfa drugs showed significant changes depending on the pH value. Analysis of their pH-dependent absorption and fluorescence properties indicated that these sulfa drugs could used to design molecular logic gates. The absorption and fluorescence behaviors at various wavelength maxima were utilized to design IMPLICATION and Improved-INHIBIT (I-INHIBIT) molecular logic gates.

01 Jan 2025·Talanta

Highly efficient and broad-spectrum antibacterial carbon dots combat antibiotic resistance

Article

Author: Li, Xinlu ; Wu, Jie ; Wang, Panyong ; Du, Yuwei ; Yan, Haiyang ; Dong, Wenfei ; You, Qiannan ; Li, Li ; Miao, Huimin

Bacterial infections have become a major global public health issue, particularly with the emergence of multidrug-resistant strains. Therefore, developing non-antibiotic antimicrobial agents is crucial for treating drug-resistant bacterial infections. Building on previous research into natural products as novel antibacterial agents, this study synthesized curcumin-derived carbon dots using curcumin and ethylenediamine as raw materials through a hydrothermal method. The resulting carbon dots not only improved the water solubility and stability of curcumin but also exhibited highly efficient broad-spectrum antibacterial activity. Detailed investigations into the antibacterial performance and mechanisms of the carbon dots were conducted through experiments such as minimum inhibitory concentration (MIC) determination, live/dead bacterial staining, morphological studies, nucleic acid concentration detection, and reactive oxygen species (ROS) detection. The results indicated that the carbon dots significantly damaged the structural integrity of bacteria and generated large amounts of ROS. They exhibited remarkable antibacterial effects against Escherichia coli, Pseudomonas aeruginosa, and Staphylococcus aureus, and effectively inhibited drug-resistant MRSA. Their antibacterial efficacy was notably superior to that of broad-spectrum antibiotics such as chloramphenicol and Sulfadiazine. This study highlights the potential application of curcumin-derived carbon dots in combating bacterial infections and provides valuable insights for developing novel antibacterial agents derived from natural products.

11 Dec 2024·Journal of Biomolecular Structure and Dynamics

Acetylsalicylic acid-sulfa drugs conjugates as potential urease inhibitors and anti-inflammatory agents: bio-oriented drug synthesis, molecular docking, and dynamics simulation studies

Article

Author: Yousaf, Numan ; Imran, Muhammad ; Muddassar, Muhammad ; Asari, Asnuzilawati ; Hameed, Abdul ; Ahmed, Mahmood ; Abdul Qadir, Muhammad ; Ahmad, Saghir

To explore the new mode of action and reduce side effects, making conjugates of existing drugs is becoming an attractive tool in the realm of medicinal chemistry. In this work, we exploited this approach and synthesized new conjugates to assess their activities against the enzymes involved in different pathological conditions. Specifically, we design and synthesized conjugates involving acetylsalicylic acid and sulfa drugs, validating the newly crafted conjugates using techniques like IR, ¹HNMR, ¹³CNMR, and elemental analysis. These conjugates underwent assessment for their ability to inhibit cyclooxygenase-2 (COX-2), urease enzymes, and their anti-inflammatory potential. A competitive mode of urease inhibition was observed for acetylsalicylic acid conjugated with sulfanilamide, sulfacetamide, and sulfadiazine with IC₅₀ of 2.49 ± 0.35 µM, 6.21 ± 0.28 µM, and 6.57 ± 0.44 µM, respectively. Remarkably, the acetylsalicylic acid-sulfamethoxazole conjugate exhibited exceptional anti-inflammatory activity, effectively curtailing induced edema by 83.7%, a result akin to the reference anti-inflammatory drug indomethacin's performance (86.8%). Additionally, it demonstrated comparable COX-2 inhibition (75.8%) to the reference selective COX-2 inhibitor celecoxib that exhibited 77.1% inhibition at 10 µM concentration. To deepen our understanding, we employed molecular docking techniques to predict the binding interactions of competitive inhibitors with COX-2 and urease receptors. Additionally, MD simulations were carried out, confirming the stability of inhibitor-target complexes throughout the simulation period, devoid of significant conformational changes. Collectively, our research underscores the potential of coupling approved medicinal compounds to usher in novel categories of pharmacological agents, holding promise for addressing a wide spectrum of pathological disorders involving COX-2 and urease enzymes.Communicated by Ramaswamy H. Sarma.

100 Deals associated with Sulfadiazine

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External Link

KEGG	Wiki	ATC	Drug Bank
D00587	Sulfadiazine	J01EC02	DB00359

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Bacterial Infections	CA	Vita Health Products, Inc.	31 Dec 1957

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


ASN2020	Not Applicable	Nephrolithiasis \| Acute Kidney Injury	-	Sulfadiazine	jkcvgclqit(xhfflqokjc) = Our patient developed severe but reversible post-obstructive AKI secondary to high-dose sulfadiazine-induced nephrolithiasis zgajlebmmp (nmjpcydgoz ) View more	Negative	19 Oct 2020
NCT01553708 (CTgov)	Phase 2/3	Burns	34	silver sulfadiazine cream+Epidermal growth factor (Epidermal Growth Factor With Silver Sulfadiazine Cream)	medbuhdtit(afxcipxkxc) = wijucpmxib wuhhxswmay (ggttmcqlis, chwusyqtki - nkajebguhu) View more	-	09 Aug 2012
NCT01553708 (CTgov)	Phase 2/3	Burns	34	Silver zinc sulfadiazine cream (Silver Zinc Sulfadiazine Cream)	medbuhdtit(afxcipxkxc) = kokazfrvbj wuhhxswmay (ggttmcqlis, vgefrrbwgd - qzkgxiigoe) View more	-	09 Aug 2012