Cytotoxicity and anti-inflammatory activity of methylsulfanyl-triazoloquinazolines.

A series of twenty five 2-methylsulfanyl-[1,2,4]triazolo[1,5-a]quinazoline derivatives 1-25 was previously synthesized. We have now investigated their cytotoxic effects against hepatocellular Hep-G2 and colon HCT-116 carcinoma cells and effect on the macrophage growth, in addition to their influence of the inflammatory mediators [nitric oxide (NO), tumor necrosis factor-α (TNF-α), prostaglandin E-2 (PGE-2) and in bacterial lipopolysachharide (LPS)-stimulated macrophages]. The findings revealed that compounds 13 and 17 showed the highest cytotoxicity and that 3, 6-8 and 25 are promising multi-potent anti-inflammatory agents.

A new investigation for some steroidal derivatives as anti-Alzheimer agents.

We herein report the anti-Alzheimer activity of some synthesized heterocyclic pyrimidine and thiopyrimidine derivatives fused with steroidal structure. Twenty-one of these compounds were synthesized and conveniently screened for their anti-Alzheimer activities using of Flurbiprofen as the reference drug. Some of these compounds were demonstrated to exhibit remarkable activity and their β-amyloid (Aβ) lowering results as IC(50) values reported.

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.

Synthesis of chiral macrocyclic or linear pyridine carboxamides from pyridine-2,6-dicarbonyl dichloride as antimicrobial agents.

A series of chiral linear and macrocyclic bridged pyridines has been prepared starting from pyridine-2,6-dicarbonyl dichloride (2). The coupling of 1 with D-alanyl methyl ester gave 2,6-bis-D-alanyl pyridine methyl ester (3). Hydrazinolysis of 3 with hydrazine hydrate afforded bis-hydrazide 4.