TY - JOUR
T1 - IN VITRO ANTIBACTERIAL AND SYNERGISTIC ACTIVITY OF PYRAZOLYL SULPHONAMIDE DERIVATIVES AGAINST STAPHYLOCOCCUS HAEMOLYTICUS
AU - Yahaya, Ewura Seidu
AU - Anak, Jesse Azebiik
AU - Amissah, Nana Ama
AU - Obuah, Collins
AU - Agyei, Phyllis Elsie Owusu
AU - Saahene, Roland Osei
AU - Ainooson, Michael
AU - Ablordey, Anthony
AU - Ekor, Martins
N1 - Publisher Copyright:
© 2024 The authors.
PY - 2024/10/31
Y1 - 2024/10/31
N2 - Background: Antimicrobial resistance has rendered several anti-infective agents ineffective, necessitating the need to intensify efforts to identify and develop novel drugs against microbial infection. Structural modification of existing antibiotics continues to be one of the areas of intense research focus in recent times. Objective: This study assessed the antibacterial and synergistic activity of fifteen pyrazolyl sulphonamide derivatives in Staphylococcus haemolyticus. Methods: Antibacterial activity was determined using the broth microdilution method. The ability of test compounds to interact with tetracycline was assessed using the checkerboard synergy testing method and the Loewe synergy and antagonism model. Results: Seven compounds (46.6%) were significantly active against the bacteria (MIC 1 µg/mL – 16 µg/mL), and four were confirmed to form synergistic combinations with tetracycline in checkerboard and Loewe analysis. Conclusion: Observations from this study has demonstrated the antibacterial activity and the synergistic potential of the novel pyrazolyl sulphonamides with tetracycline, highlighting the possible role of modified sulphonamides as a rich resource for antimicrobial development.
AB - Background: Antimicrobial resistance has rendered several anti-infective agents ineffective, necessitating the need to intensify efforts to identify and develop novel drugs against microbial infection. Structural modification of existing antibiotics continues to be one of the areas of intense research focus in recent times. Objective: This study assessed the antibacterial and synergistic activity of fifteen pyrazolyl sulphonamide derivatives in Staphylococcus haemolyticus. Methods: Antibacterial activity was determined using the broth microdilution method. The ability of test compounds to interact with tetracycline was assessed using the checkerboard synergy testing method and the Loewe synergy and antagonism model. Results: Seven compounds (46.6%) were significantly active against the bacteria (MIC 1 µg/mL – 16 µg/mL), and four were confirmed to form synergistic combinations with tetracycline in checkerboard and Loewe analysis. Conclusion: Observations from this study has demonstrated the antibacterial activity and the synergistic potential of the novel pyrazolyl sulphonamides with tetracycline, highlighting the possible role of modified sulphonamides as a rich resource for antimicrobial development.
KW - Antibacterial activity
KW - Antimicrobial resistance
KW - Staphylococcus haemolyticus
KW - Sulphonamide derivatives
KW - Synergistic activity
UR - http://www.scopus.com/inward/record.url?scp=85210573900&partnerID=8YFLogxK
U2 - 10.69857/joapr.v12i5.658
DO - 10.69857/joapr.v12i5.658
M3 - Article
AN - SCOPUS:85210573900
SN - 2348-0335
VL - 12
SP - 116
EP - 123
JO - Journal of Applied Pharmaceutical Research
JF - Journal of Applied Pharmaceutical Research
IS - 5
ER -