Synthesis and antimicrobial activity of new adamantane derivatives I.

A series of fourteen derivatives of adamantane was synthesised. The new compound 4-(adamant-1-ylmethoxycarbonyl)phthalanhydride obtained from 1-adamantane- methanol and trimellitic anhydride chloride appeared very useful for preparation of a number of N-substituted phthalimides. Antimicrobial activity of the newly obtained derivatives such as, for example, 4-(adamant-1-ylmethoxycarbonyl)-N-(5-carboxypentamethylene)phthalimide or 4-(adamant-1-ylmethoxycarbonyl)-N-(L-alanyl)phthalimide was tested against Staphylococcus aureus, Bacillus sp., Micrococcus flavus and Enterococcus faecium. The minimal inhibitory concentration (MIC) for these compounds against S. aureus were 0.022 and 0.05 μg/ml, respectively

ZAWAŁ SERCA Stężenie chemokin MCP-1, MIP-1α i RANTES

Background: Chemokines are supposed to play an important role in the activation of monocytes and in the development of atherosclerosis. There are also suggestions that chemokine-mediated enhanced coagulability may be related to the pathogenesis of acute coronary syndromes.Aim: To assess the kinetics of 3 chemokines: Monocyte Chemoattractant Protein-1 (MCP-1), Macrophage Inflammatory Protein-1alfa (MIP-1α) and Regulated on Activation Normal T cell Expressed and Secreted (RANTES) in patients with ST-elevation myocardial infarction (STEMI).Methods: The study group consisted of 40 patients (pts) with STEMI who were divided into 2 groups - 16 pts with anterior MI (AMI) and 24 pts with inferior or lateral MI (IMI). According to the type of received therapy, the pts were divided into 2 other groups: group A - 30 pts treated with thrombolytic agents or primary angioplasty and group B - 10 pts without recanalisation therapy. The control group consisted of 10 healthy volunteers. Blood samples for MCP-1, MIP-1α and RANTES serum levels was taken on admission and 3 h, 24 h, 48 h, 72 h and 7 days afterwards.Results: The baseline MCP-1 and RANTES levels were significantly higher in pts with STEMI than in controls (1068.9 vs 880.9 pg/ml,

The selectivity of inhibitors of protein kinase CK2:an update

CK2 (casein kinase 2) is a very pleiotropic serine/threonine protein kinase whose abnormally high constitutive activity has often been correlated to pathological conditions with special reference to neoplasia. The two most widely used cell permeable CK2 inhibitors, TBB (4,5,6,7-tetrabromo-1H-benzotriazole) and DMAT (2-dimethylamino-4,5,6,7-tetrabromo-1H-benzimidazole), are marketed as quite specific CK2 blockers. In the present study we show, by using a panel of approx. 80 protein kinases, that DMAT and its parent compound TBI (or TBBz; 4,5,6,7-tetrabromo-1H-benzimidazole) are potent inhibitors of several other kinases, with special reference to PIM (provirus integration site for Moloney murine leukaemia virus)1, PIM2, PIM3, PKD1 (protein kinase D1), HIPK2 (homeodomain-interacting protein kinase 2) and DYRK1a (dual-specificity tyrosine-phosphorylated and -regulated kinase 1a). In contrast, TBB is significantly more selective toward CK2, although it also inhibits PIM1 and PIM3. In an attempt to improve selectivity towards CK2 a library of 68 TBB/TBI-related compounds have been tested for their ability to discriminate between CK2, PIM1, HIPK2 and DYRK1a, ending up with seven compounds whose efficacy toward CK2 is markedly higher than that toward the second most inhibited kinase. Two of these, K64 (3,4,5,6,7-pentabromo-1H-indazole) and K66 (1-carboxymethyl-2-dimethylamino-4,5,6,7-tetrabromo-benzimidazole), display an overall selectivity much higher than TBB and DMAT when tested on a panel of 80 kinases and display similar efficacy as inducers of apoptosis