Synthesis, characterization and in vitro biological evaluation of some novel diarylsulfonylureas as potential cytotoxic and antimicrobial agents.
A series of novel diarylsulfonylureas (1-28) have been synthesized and characterized by FTIR, (1)H NMR, (13)C NMR and LC mass spectral analysis. All the synthesized compounds were evaluated for their in vitro cytotoxicity and antimicrobial activities. Among the tested compounds for cytotoxicity using Brine Shrimp Lethality assay, compounds 18 and 22 exhibited significant cytotoxicity at ED(50) values 3.96±0.21 and 4.02±0.19μg/mL, respectively. This level of activity was found comparable to that of the reference drug podophyllotoxin with ED(50) value 3.61±0.17μg/mL and it could be a remarkable starting point to develop new lead molecules with major cytotoxicity. Antimicrobial activity was screened using agar well diffusion assay method against selected Gram-positive, Gram-negative and fungal strains. Most of the compounds showed promising antibacterial and antifungal activity and the activity expressed as the minimum inhibitory concentration (MIC) in μg/mL.
Pharmaceutical Chemistry Division, AU College of Pharmaceutical Sciences, Andhra University, Visakhapatnam 530 003, Andhra Pradesh, India. vasudevaraoavupati@gmail.com
Vasudeva Rao
VR
Avupati
Rajendra Prasad
RP
Yejella
Girijasankar
G
Guntuku
Pradeepsagar
P
Gunta
D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001156:Artemia / Q000166:cytology / Q000187:drug effects*; D001419:Bacteria / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D005658:Fungi / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D014508:Urea