A row of 1-alkyne (C6-C17) derivatives against tetrahydroisoquinoline have been synthesized. 1-alkyne (C6-C17) derivatives cytotoxicity against three lines of cancer cells and two lines of normal cells was studied. It was found that 1-tridecyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline exhibits a high cytotoxic effect with low toxicity to healthy cells. Antimicrobial activity of 1-alkyne (C6-C17) derivatives against 5 strains of bacteria and fungus was studied. It has been found that 1-nonyl-6,7-dimethoxy-1,3,4-tetrahydroisoquinoline exhibits strong antibacterial and antifungal effects.
Drug addiction is one of the biggest problems of medicine because diagnosis and treatment of drug addiction are difficult compared with some other socially significant diseases. In this study, synthesis and evaluation of four carrier protein-morphine conjugates were experimented. These conjugates were evaluated based on ELISA; soybean protein-based conjugate was selected for further analysis. The total soybean protein was isolated from the local soybean variety and; it was fractioned by the gel-filtration method and their amino acids compositions were studied. After that, the ELISA drug addicts were conducted based on soybean protein-morphine conjugates synthesized with soybean protein fractions. The high molecular weight soybean protein- morphine conjugate showed the highest quality.
The S-(5-aryl-1,3,4-oxadiazol-2-yl) O-alkyl carbonothioate (4-9) and the alkyl 2-((5-aryl-1,3,4-oxadiazol-2-yl)thio) acetate (10-15) were synthesized by interaction of 5-aryl-1,3,4-oxadiazole-2-thiones with alkyl esters of chloroformic acid and chloroacetic acid. The yields of target compounds (7-9) obtained with isobutyl chloroformate were 69-73%, compounds (4-6) with propyl chloroformate - 74-79% and compounds (10-15) with alkyl esters of chloroacetic acid - 86-92%, respectively. The structures of the synthesized compounds were confirmed by IR, UV, 1H and 13C NMR spectra. The antibacterial and antifungal activities of these compounds were investigated. The results of in vitro antimicrobial activity tests showed that S-(5-phenyl(2-chlorophenyl)-1,3,4-oxadiazol-2-yl) O-propyl carbonothioate (4-5) and S-(5-phenyl(2-chlorophenyl)-1,3,4-oxadiazol-2-yl) O-isobutyl carbonothioate (7-8) exhibited weak, but selective antibacterial activity against gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus). At the same time, no activity was shown by compounds with two chlorine atoms in the aromatic ring (13-15) and alkyl 2-((5-aryl-1,3,4-oxadiazol-2-yl) thio) acetate (10-15).
Amidoalkylation of secondary heterocyclic amines by N-[5-(alkylsulfanyl)-1,3,4-thiadiazol-2-yl]-2'-chloroacetamide resulted the new compounds 5-10 that contain 1,3,4-thiadiazole-5-thione moiety alongside pyperidine, morpholine, and cytisine fragments. In vitro screening of antimicrobial activity of synthesized compounds showed that N-[5-(amylsulfanyl)-1,3,4-thiadiazol-2-yl]-2'-morpholinacetamide exhibited an appreciable antibacterial activity against gram-negative bacteria of Escherichia coli (inhibition zone diameter of 16 mm) and gram-positive bacteria of Staphylococcus aureus and Bacillus subtilis (10-13 mm).
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