Chemotherapeutic agents with an imidazole moiety. II. Synthesis and biological activities of new 1,4-diarylimidazoles.
The synthesis, antifungal and pharmacological activities of new 1,4-diarylimidazoles are reported. Antimicrobial data in comparison with antifungal antibiotic pyrrolnitrin pointed out that the 1,4-diaryl-2-mercaptoimidazole derivatives were inactive and all 1,4-diarylimidazoles exhibited a weak antifungal activity. Some compounds showed a selective activity against strains of Candida sp. Instead pharmacological data did not evidence any significant antiinflammatory activity. The tested compounds were prepared by reacting appropriate phenacylanilines with potassium thiocyanate in acidic medium to afford 1,4-diaryl-2-mercapto imidazoles which were then transformed into title compounds by treatment with nitric acid.
Porretta
G C
GC
Istituto di Chimica Farmaceutica e Tossicologia, Facoltà di Farmacia, Università La Sapienza, Roma, Italy.
Cerreto
F
F
Fioravanti
R
R
Scalzo
M
M
Fischetti
M
M
Riccardi
F
F
Capezzone de Joannon
A
A
de Feo
G
G
Mazzanti
G
G
Tolu
L
L
D000818:Animals; D000935:Antifungal Agents / Q000138:chemical synthesis*; D002176:Candida albicans / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D005260:Female; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D051381:Rats; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D007093:Imidazoles