title: Synthesis and anti-inflammatory evaluation of some new acyl-hydrazones bearing 2-aryl-thiazole.
abstract: This work describes recent results from our research program aiming at the synthesis and evaluation of new compounds acting as potential anti-inflammatory drugs. A series of novel acyl-hydrazones bearing 2-aryl-thiazole moiety were synthesized by the condensation between derivatives of 4-[2-(4-methyl-2-phenyl-thiazole-5-yl)-2-oxo-ethoxy]-benzaldehyde and 2, 3 or 4-(2-aryl-thiazol-4-ylmethoxy)-benzaldehyde, respectively and different carboxylic acid hydrazides. The structures of newly synthesized compounds were established by the combined use of IR, (1)H NMR, mass spectral data and elemental analysis. These compounds were tested in vivo for their anti-inflammatory activity, in an acute experimental inflammation. The acute phase bone marrow response, phagocytes' activity and NO synthesis were evaluated. Compounds 10, 15, 17, 18 and 22 reduced the absolute leukocytes count due to the lower neutrophils percentage. Phagocitary index was decreased by all the compounds. Seven of them reduced the phagocitary activity. Five compounds inhibited NO synthesis, 3, 4, 16 and 22 stronger than Meloxicam, the anti-inflammatory reference drug.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Medicine and Pharmacy, 41 Victor Babes Street, RO-400010 Cluj-Napoca, Romania. cris.moldovan@yahoo.com
authors.forename: Cristina Mariana
authors.initials: CM
authors.lastname: Moldovan
authors.forename: Ovidiu
authors.initials: O
authors.lastname: Oniga
authors.forename: Alina
authors.initials: A
authors.lastname: Pârvu
authors.forename: Brînduşa
authors.initials: B
authors.lastname: Tiperciuc
authors.forename: Philippe
authors.initials: P
authors.lastname: Verite
authors.forename: Adrian
authors.initials: A
authors.lastname: Pîrnău
authors.forename: Ovidiu
authors.initials: O
authors.lastname: Crişan
authors.forename: Marius
authors.initials: M
authors.lastname: Bojiţă
authors.forename: Raluca
authors.initials: R
authors.lastname: Pop
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001853:Bone Marrow / Q000187:drug effects / Q000276:immunology; D016207:Cytokines / Q000096:biosynthesis; D006835:Hydrazones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D007249:Inflammation / Q000188:drug therapy*; D007958:Leukocyte Count; D007962:Leukocytes / Q000187:drug effects / Q000276:immunology; D007964:Leukocytosis / Q000276:immunology; D015394:Molecular Structure; D009504:Neutrophils / Q000187:drug effects / Q000276:immunology; D051381:Rats; D013237:Stereoisomerism; D013844:Thiazoles / Q000737:chemistry*
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D016207:Cytokines; D006835:Hydrazones; D013844:Thiazoles