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Synthesis, antibacterial, anti-inflammatory and anti-allergy activities of 2,4-pyridinedicarbohydrazide and its related derivatives

O.I.Abd El-Salam, A.E.Amr, S.M.Abu-Bakr, F.A.Bassyouni, M.Abdullah

2,4-Pyridinedicarbohydrazide (3) was used in synthesizing several new heterocyclic compounds with expected potential biological activity, via its reaction with various chemical reagents. A series of bis- (arylmethylidene)pyridine-2,4-dicarbohydrazides (4a-e) were synthesized by condensation of (3) with various aldehydes. Further, replacement of the dicarbxylic acid functionality of (1) with five membered heterocycles, in the hope of obtaining additional pharmacological activity, encouraged us to synthesize some 2,4-bis-{pyrazoly1 (5); pyrazolony1 ( 6); 1,3,4-oxadiazolyl (7), (9), (11), (14); 1,2,4-triazolyl (15) and triazolo[3,4-b][1,3,4]thiadiazinyl (17)}pyridines. The structures of the synthesized products were identified by elemental analysis, IR, 1H NMR and EIMS spectroscopy. The synthesized compounds were screened for their in vitro growth inhibiting activity against different strains of bacteria and compared with the standard antibiotic (Chloramphenicol) at triplicate concentration (5, 2.5,1 ìg/ml).Also, they were screend for their in vivo anti-inflammatory activity [%Inhibition of oedema and % inhibition of plasma prostaglandin (PGE2)] and antiallergic activity (anti-histamine). Their toxicity (ALD50 mg kg-1 p.o.) and ulcerogenic (UD50 mg kg-1 i.p.) activities were measured and promising results were obtained.