A few analogues of atevirdine or 1-[(5-methoxyindol-2-yl) carbonyl]-4-[3- (ethylamino)-2-pyridyl] piperazine – an anti-HIV belonging to non-nucleoside reverse transcriptase inhibitors were synthesized and evaluated for anti-HIV activity. Replacement of indolyl moiety with 2-alkylthio-1-benzyl-5-imidazolyl substituent afforded 1-[2-(alkylthio-1-benzyl-5-imidazolyl) carbonyl]-4-[3-(isopropylamino...

Treatment of N(2),N(6)-bis(6-acrylamidopyridin-2-yl)pyridine-2,6-dicarboxamide with benzimidazole gives the acyclic aza-Michael addition product N(2),N(6)-bis(6-(3-(1H-benzo[d]imidazol-1-yl)propanamido)pyridin-2-yl)pyridine-2,6-dicarboxamide (2). The macrocycle N(1),N(7)-pyridine-2,6-dimethyl-N(2),N(6)-bis(6-(3-(1H-benzo[d]imidazol-1-yl)propanamido)pyridin-2-yl)pyridine-2,6-dicarboxamide dibrom...

New 3,5-disubstituted-1,2,4-thiadiazoles were synthesized and together with a series of their analogs obtained earlier tested for cytotoxic activity to breast adenocarcinoma MCF-7 lung carcinoma A 549 cells. The selectivity action was determined in comparison etiologically noncancerous epithelial cells MCF-10A fibroblasts VA13. From five- six-fold revealed 3,4-dichlorophenyl-{3-[2-(2-morpholin-...

In this study appropriate hydrazide compounds, furan-2-carboxylic acid hydrazide (1) and phenylacetic acid hydrazide (2) were converted into 1,4-substituted thiosemicarbazides 4a-e and 5a-e and 4-amino-5-(furan-2-yl or benzyl)-4H-1,2,4-triazole-3-thiols 7 and 10. The 1,4-substituted thiosemicarbazides were then converted into 5-(furan-2-yl or benzyl)-4-(aryl)-4H-1,2,4-triazole-3-thiols 8a-e and...

The asymmetric unit of the title compound, C(16)H(13)N(2)O(+)·NCS(-)·C(16)H(12)N(2)O, contains two N-(pyridin-4-yl)naphthalene-2-carboxamide mol-ecules, both are partially protonated in the pyridine moiety, i.e. the H atom attached to the pyridine N atom is partially occupied with an occupancy factor of 0.61 (3) and 0.39 (3), respectively. In the crystal, protonated and neutral N-(pyridin-4-yl)...

The chemokine receptor CXCR3 is involved in various inflammatory diseases, such as rheumatoid arthritis, multiple sclerosis, psoriasis, and allograft rejection in transplantation patients. The CXCR3 ligands CXCL9, CXCL10, and CXCL11 are expressed at sites of inflammation, and they attract CXCR3-bearing lymphocytes, thus contributing to the inflammatory process. In this study, we characterize fi...

The p38 mitogen-activated protein kinase (MAPK) is a key mediator in cytokine-induced signaling events that are activated in response to a variety of extracellular stimuli such as stress factors, apoptosis, and proliferation. Therefore, the MAPK family plays an integral role in disease states including oncogenesis, autoimmune diseases, and inflammatory processes. Inhibition of these protein kin...

Four copper(ii) complexes with multidentate ligands, ([CuL1Cl2]), ([Cu(HL2)Cl2]), ([Cu2(L2)2](ClO4)2) and ([CuL3(HOCH3)ClO4]) {L1 = N,N-bis((pyridin-2-yl)methyl) prop-2-yn-1-amine, HL2 = 2-((((1-methyl-1H-imidazol-2-yl)methyl)(pyridin-2-ylmethyl)amino)methyl)phenol and HL3 = 2-((((1-methyl-1H-imidazol-2-yl)methyl)(pyridin-2-ylmethyl)amino)methyl)-2-t-butyl-phenol} are reported. The complexes we...