Anti-inflammatory, analgesic, anticonvulsant and antiparkinsonian activities of some pyridine derivatives using 2,6-disubstituted isonicotinic acid hydrazides.
A series of novel thiazolo derivatives 2-15 was synthesized by initial condensation of 2,6-dihydroxyisonicotinohydrazide 1 and 2-chloro-6-hydrazinylisonicotinohydrazide 11 with different organic reagents. The pharmacological screening showed that many of these obtained compounds have good anti-inflammatory, analgesic, anticonvulsant, and antiparkinsonian activities comparable to diclofenac potassium, Voltarene(®), Carbamazepine(®), and Benzotropene(®) as reference drugs. Initially the acute toxicity of the compounds was assayed via the determination of their LD₅₀. The structures of newly synthesized compounds were confirmed by IR, ¹H-NMR, ¹³C-NMR, MS spectral data and elemental analysis. The detailed synthesis, spectroscopic data, LD₅₀ and pharmacological activities of the synthesized compounds were reported.
Department of Pharmaceutical Chemistry, King Saud University, Riyadh, Saudi Arabia.
Mohamed A
MA
Al-Omar
Abd El-Galil E
Ael-G
Amr
Rashad A
RA
Al-Salahi
D000700:Analgesics / Q000138:chemical synthesis*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis*; D000927:Anticonvulsants / Q000138:chemical synthesis*; D000978:Antiparkinson Agents / Q000138:chemical synthesis*; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007538:Isoniazid / Q000737:chemistry*; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D013057:Spectrum Analysis; D013844:Thiazoles / Q000737:chemistry
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D000927:Anticonvulsants; D000978:Antiparkinson Agents; D011725:Pyridines; D013844:Thiazoles; D007538:Isoniazid