Synthesis of (1)-N-(4-methoxybenzyl)-1,10-phenanthroline bromide from 1,10-phenanthroline monohydrate and 4-methoxybenzaldehyde as starting material and evaluation of its antiplasmodial activities have been carried out. The 4-methoxybenzyl alcohol was prepared from 4-methoxy-benzaldehyde using sodium borohydride (NaBH4) reagent and ethanol absolute solution. The mixture was refluxed for 3 h. To yield colorless dilution compound with 90.41 % in efficiency. Furthermore, bromination of 4-methoxybenzyl alcohol with phosphorus bromide (PBr3) was conducted by refluxing for 3 h. The product of this reaction was yellow liquid of 4-methoxybenzyl bromide, 79.03% yield and 95.34 % purity. The final step of reaction was benzylation of 1,10-phenanthroline monohydrate with 4-methoxybenzyl bromide reagent. It was conducted by refluxing in aceton for 8 h at 55 oC. The yield of the reaction was (1)-N-(4-methoxybenzyl)-1,10-phenanthroline bromide (77.63%). It is pink solid form, and its melting point is 192-193 oC. Identification of the product was carried out by means of GC-MS, IR and 1H-NMR spectrometers. The in vitro antiplasmodial activity on chloroquine-resistant Plasmodium falciparum FCR-3 strain and chloroquine sensitive P. falciparum D10 strain for (1)-N-(4-methoxybenzyl)-1,10-phenanthroline bromide were determined by microscopic method. The result showed that after 72 h incubation, it has IC50 0.93±0.02 µM and 1.21±0.09 µM, respectively. Keywords: 1,10-phenanthroline, (1)-N-(4-methoxybenzyl)-1,10-phenanthroline bromide, 4 methoxybenzaldehyde, antiplasmodial activities
Quantitative Electronic Structure-Activity Relationship (QSAR) analysis of a series of 1,10-phenanthroline derivatives as antiplasmodial compounds have been conducted using atomic net charges (q), dipole moment (μ) ELUMO, EHOMO, polarizability (α) and log P as the descriptors. The descriptors were obtained from computational chemistry method using semi-empirical PM3. Antiplasmodial activities were taken as the activity of the drugs against chloroquine-resistant Plasmodium falciparum FCR3 strain and are presented as the value of ln (1/IC50) where IC50 is an effective concentration inhibiting 50% of the parasite growth. The best model of QSAR model was determine by multiple linear regression method and giving equation of QSAR: ln 1/IC50 = 3.732 + (5.098) qC5 + (7.051) qC7 + (36.696) qC9 + (41.467) qC11 -(135.497) qC12 + (0.332) μ - (0.170) α + (0.757) log P. The equation was significant on the 95% level with statistical parameters: n=16; r=0.987; r2= 0.975; SE=0.317; Fcalc/Ftable = 15.337 and gave the PRESS=0.707. Its means that there were only a relatively few deviations between the experimental and theoretical data of antimalarial activity. Keywords: QSAR, antimalarial, semi-empirical method, 1,10-phenanthroline.
The synthesis of 5-nitro-1,10-phenanthroline hydrate 2 derivatives from 1,10-phenanthroline monohydrate as starting material has been carried out. The 5-nitro-1,10-phenanthroline hydrate 2 was obtained through nitration reaction using H 2 SO 4 and HNO 3 as catalyst and reagent, respectively. Synthesis of (1) -N-alkyl-6-nitro-and (1)-Nbenzyl-6-nitro-1,10-phenanthrolinium have been prepared using dimethyl sulphate (DMS), diethyl sulphate (DES), benzyl chloride, benzyl bromine, and benzyl iodide. The reagents of benzyl bromine, and benzyl iodide were synthesized from benzyl chloride using NaBr in ethanol absolute and
The phospholipids (PL) of pumpkin (Cucurbita moschata (Duch) Poir) seed kernel and their fatty acid composition were investigated. The crude oil was obtained by maceration with isopropanol followed by steps of extraction yielded polar lipids. The quantitative determination of PLs content of the dried pumpkin seed kernel and their polar lipids were calculated based on the elemental phosphorus (P) contents which was determined by means of spectrophotometric methods. PL classes were separated from polar lipids via column chromatography. The fatty acid composition of individual PL was identified by gas chromatography-mass spectrometry (GC-MS). The total of PL in the pumpkin seed kernels was 1.27% which consisted of phosphatidylcholine (PC), phosphatidylserine (PS) and phosphatidyletanolamine (PE). The predominant fatty acids of PL were oleic and palmitic acid in PC and PE while PS's fatty acid were dominantly consisted of oleic acid and linoleic acid.
A chitinolytic microorganism had been isolated from mud fields in Ketintang Surabaya area by using a minimal media containing 0.4% colloidal chitin. Activity assay is based on released N-acetyl-glucosamine which reacted with 3,5 dinitrosalicyclic acid. Mud fields produce 63 bacterial isolates with chitinase activity (TNH1 – TNH63 isolates). The highest activity was shown by TNH11 isolate with specific activity 1.27 U/mg. TNH11 isolates was Gram negative, rod-cocoid cell, has a colony of yellow, round shape, convex elevation, flat margin and the colony diameter 3–5 mm.
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