Synthesis and in vitro anti-Helicobacter pylori activity of N-[5-(5-nitro-2-heteroaryl)-1,3,4-thiadiazol-2-yl]thiomorpholines and related compounds.
Synthesis and in vitro anti-Helicobacter pylori activity of N-[5-(5-nitro-2-heteroaryl)-1,3,4-thiadiazol-2-yl]thiomorpholines 5-7(a-c) and some related compounds 8a-c and 9a-c were described. The anti-H. pylori activity of target compounds along with commercially available antibiotics such as metronidazole and amoxicillin was evaluated by comparing the inhibition zone diameters determined by the paper disc diffusion bioassay. From our bioassay results against 20 clinical isolates, it is evident that most compounds still had strong activity at 4 and 2 microg/disc (average of inhibition zone >20 mm) while metronidazole had little activity at these doses. Nitrofuran analog 7b containing thiomorpholine S,S-dioxide moiety was the most potent compound tested.
Mirzaei
Javad
J
School of Chemistry, University College of Science, University of Tehran, Tehran, Iran.
Siavoshi
Farideh
F
Emami
Saeed
S
Safari
Fatemeh
F
Khoshayand
Mohammad Reza
MR
Shafiee
Abbas
A
Foroumadi
Alireza
A
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D016480:Helicobacter pylori / Q000187:drug effects* / Q000302:isolation & purification; D006801:Humans; D015394:Molecular Structure; D009025:Morpholines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017672:Nitrogen Compounds / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000737:chemistry*
D000998:Antiviral Agents; D009025:Morpholines; D017672:Nitrogen Compounds; D013830:Thiadiazoles; C058949:1,3,4-thiadiazole; C028971:thiamorpholine