Amino acid and peptide derivatives as anti-allergic and anti-inflammatory agents

It was proved that current anti-allergic drugs comprise piperazine and acrylic acid segments. These compounds were structurally designed as 5-lipoxygenase inhibitors depending on two action mechanisms of the ready drugs used to treat allergy e.g.[Oxatomide], which contains piperzine moiety, its anti-allergic effects possess antagonist activities against chemical mediators such as histamine, serotonine and leukotrienes [which cause allergy]. Also, [Tranilast], which contains acrylic acid segment; its activity depends on inhibition of mediator release. In harmony with these findings new structures having anti-allergic properties are proposed in this manuscript. New products, [5a-u] with expected better biological activities and decreased side effects were synthesized by the addition of an amino acid conjugate of cinnamic acid to a piperazine segment. Their anti-allergic and anti-inflammatory activities were evaluated. Most of them show promising activities

Synthesis of some F-heterocyclic compounds of potential anticancer activity using 8-fluoro-1- benzosuberone as a synthon

8-fluoro-1-benzosuberone I condensed with aromatic aldehydes in the presence of potassium hydroxide to yield the arylmethylene derrivatives II, which condensed with phenylhydrazinc and thiourea to give the corresponding pyrazol and pyrimidine derivatives III and IV, respectively Compound IV reacted with chloroctic acid, alpha - bromopropionic acid or beta-bromopropionic acid to afford the thiazolopy-rimidine, methylthiazolopyrimia and thiazinopyrimidine derivatives V, VI and VII, respectively. Compound V condensed with aromatic aldehydes to afford the arylmethycine derivativcs VIII. Also, the pyrano and pyridino-fluorobenzosubcronc derivatives IX and X were synthesized. The obtained products were preliminarily tested as anticancer agents and it was found that the products IIa, IIb, IXa, IXb and X showed promising activity against non-small cell lung cancer

Synthesis and antimicrobial activity of some new Chiral Bridged macrocyclic pyridines

The utilization of 2,6-pyridinedicarboxylic acid [dipicolinic acid] in the synthesis of some chiral pridged bicyclic pyridine tripeptides is described. The antimicrobial activity of these natural cyclic peptides was tested

Synthesis and antimicrobial activity of 3,5-bis- [1-3,4-oxadiazol-5-yl] -, [1,3-thiazolo] hydrazony1-and [7H] s-Triazolo- [3,4-b] -1,3,4 Thiadiazinyl] pyridine derivatives

Different 3, 5-bis [oxadiazolyl] pyridine derivatives 3-5 have been obtained from 1 depending on the reaction condition. Reaction of 5 with amines or alkylhalides afforded the corresponding Mannich bases 6 or s-alkyl derivatives 7. The latter derivatived were treated with ammonium acetate to give 9 and with hydrazine hydrate affording bis bicyclic pyridine derivatives 10. Preliminary antimicrobial tests showed products 6e and 8 to possess higher activity when compared with oxytetracycline