Synthesis, anti-inflammatory, analgesic and anticonvulsant activities of 1,8-dihydro-1-ary1-8-alkyl pyrazolo(3,4-b)indoles.
A series of 1,8-dihydro-1-aryl-8-alkyl pyrazolo(3,4-b)indoles 4a-j, 5a-j and 6a-j has been synthesized and tested for their anti-inflammatory and anticonvulsant activities. Formation of the pyrazoloindole derivatives was achieved by treating arylhydrazones of N-alkyl indole-3-carbox-aldehydes 1a-j, 2a-j and 3a-j with ten times their mass of polyphosphoric acid as a condensing agent. The newly synthesized compounds were evaluated for their anti-inflammatory, analgesic and anticonvulsant activities compared to indomethacin, flufenamic acid and diazepam as positive controls. Detailed synthesis, spectroscopic and toxicity data are reported.
Mandour
Adel H
AH
Chemistry Department of Natural Compounds, National Research Centre, Gizza, Egypt. ahmandour_z@yahoo.com
El-Sawy
Eslam R
ER
Shaker
Kamel H
KH
Mustafa
Mohamed A
MA
D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D010147:Pain Measurement / Q000187:drug effects / Q000379:methods; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000927:Anticonvulsants; D007211:Indoles; D011720:Pyrazoles