Synthesis, docking molecule study and antibacterial activity of N’-(4-Fluorobenzylidene)-4-hydroxybenzohydrazide and N’(4-Fluorobenzylidene)-4-hydroxybenzohydrazide)

Many antibacterial are already resistant, so new antibacterial is needed. Objective:The compounds of N'- (4-Fluorobenzylidene) -4-hydroxybenzohydrazide, and N' - (3Bromobenzylidene)-4-hydroxybenzohydrazide as antibacterial generally contain azometin (HN-N=CH-) and halogen groups. Before the compounds to be synthesized were done docking molecule study, to predict its activity as antibacterial. The synthesis was carried out by microwave and identification of the results with FT-IR, MS, 1H-NMR, and 13C-NMR, docking molecule study with the Molegro Virtual Docker program, and antibacterial activity by diffusion method. The obtained compounds of N '- (4-Fluorobenzylidene) -4hydroxybenzohydrazide, and N'-(3-Bromobenzylidene)-4-hydroxybenzohydrazide 87%,and 81% yield respectively.The results of docking molecule study obtained reranked score lower than the starting material (methyl 4-hydroxybenzoate). The compounds have antibacterial activity against Gram positive (Bacillus subtilis) and Gram negative (Escherichia coli).Conclusion: N '- (4-Fluorobenzylidene) -4-hydroxybenzohydrazide and N' - (3Bromobenzylidene)-4-hydroxybenzohydrazide have been synthesized, characterized and exhibited promised antibacterial

Syntheses, Molecular Docking Study and Anticancer Activity Examination of p-Methoxycinnamoyl Hydrazides

In this study, we attempted to develop a potential anticancer drug by synthesizing some of p-methoxycinnamoyl hidrazides. The compounds were synthesized from the ethyl p-methoxycinnamate (EPMC), isolated from rhizome of Kaemferia galanga Linn. The structures of the compounds were confirmed by UV-vis spectrophotometry, 1H-NMR, 13C-NMR, FTIR, and MS spectroscopic methods. The study was followed by anticancer activity evaluation of the compounds by in silico study using Molegro® ver. 5.5 and by in vitro assay against human breast cancer cells (T47D) by 3-(4,5-Dimethylthiazol2-yl)-2-5-Diphenyltetrazolium Bromide (MTT) method. The yield of derivatives of p-methoxycinnamoylhidrazide was around 25 to 90%. The result showed that 3-(4-methoxyphenyl)-N'-(3-(4-methoxyphenyl) acryloyl) acrylohydrazide has the highest value of rerank score (-124.81). In addition, from the in vitro assay, it was revealed that 2-hydroxybenzohydrazide has the lowest IC50 (0.2 x 106 nM) against T47D as the most effective compound than the others. p-Methoxycinnamoyl hidrazides have been synthesized as low as 25% yields. Among the tested compounds, 2-hydroxybenzohydrazide is the most effective compound against T47D (human breast cancer) cell line in vitro. While in silico study result showed that 3-(4-methoxyphenyl)-N'-(3-(4-methoxyphenyl) acryloyl)acrylo- hydrazide has better activity than the lead compound, EPMC

Antibacterial and Antioxidant Activity Evaluation of 1,3-Diaryl-prop-2-en-1-one Derivatives

Some 1,3-diaryl-propenone derivatives had been synthesized by a conventional Claisen-Schmidt condensation in the previous experiment. This study purposed to examine their antibacterial activity against Staphylococcus aureus, Escherichia coli and Candida albican by using agar diffusion susceptibility method. The tested compounds were also screened for antioxidant activity by DPPH method. The results of antibacterial activity showed that the tested compounds were inactive toward Escherichia coli, but still had modest ability to inhibit Staphylococcus aureus and Candida albican, compared to standard drugs. While the results of antioxidant activity disclosed that the compound with hydroxyl groups which possessed antioxidant ability (16.36%), but not the others

Synthesis and Brine Shrimp Bioassay of Chalcone and Its Two Methoxy Derivatives

Chalcone and its two methoxy derivatives have been synthesized by a simple Claisen-Schmidt condensation in presence of NaOH 60%. The reactions were carried out at room temperature for about 15 -105 minutes and provided the desired compounds in about 73-96% yields. The structure of the compounds was confirmed by 1H-NMR, 13C-NMR, IR, MS and UV-vis spectroscopic methods. Furthermore, all the synthesized compounds were examined their cytotoxic action by BST method (brine shrimp lethality test) and expressed as toxic compound

In vitro antimalarial activity of chalcone and its derivatives

Object: to evaluate in vitro antimalarial activity of chalcone and its derivatives. Method: The Chalcones were tested its anti plasmodial activity against Plasmodium falciparum (3D7 strain) by using candle jar method, introduced by Trager and Jensen (1976). Result and Discussion: The tested compounds gave IC50 (half maximal inhibitory concentration) ranged between 0.242 and > 100 µg/ml. Conclusion: All compounds have lower antimalarial activity than commercially standard antimalarial drug, Chloroquine diphosphate

The Influence of Ratio Pyridine and Triethylamine Catalysts on Synthesis 2-Phenyl-Benzo [D][1, 3] Oxazine-4-On Derivatives

The aim of this research was to compare the effect of pyridine and triethylamine catalyst ratios on the synthesis of 2-phenyl-benzo(d)[1,3] oxazine-4-one derivatives. The catalysts used were triethylene amine (100%), pyridine: triethylamine (1: 4 mol); Pyridine: triethylamine (1: 1 mol) and pyridine (100%). Using pyridine (100%) as a catalyst could increase the percentage of the synthesis of 2-phenyl-benzo[d][1,3] oxazine-4-one derivatives to 2 times greater than pyridine: triethylamine (1: 4 mol) as a catalyst. Using pyridine (100%) as a catalyst in the synthesis of 2-phenyl-benzo[d] [1,3]oxazine-4-one derivatives were more effective and efficient by obtaining the following results we obtained 80% for 2-phenyl-4Hbenzo[1,3]oxazin-4-one and 86% for 2-(3,4-dichlorophenyl)-4H-benzo[1,3]oxazin-4-one and 82% for 2-(2,4-dichlorophenyl)-4H-benzo[1,3]oxazin-4-one and 46% for 2-(4-nitrophenyl)-4H-benzo[1,3]oxazin-4-one

Sintesis Khalkon dan Derivatnya Menurut Reaksi Kondensasi Claisen Schmidt dengan Iradiasi Gelombang Mikro

This research has been done synthesis of chalcone and its derivatives by Claisen Schmidt condensation reaction with microwave irradiation on 400 Watt for 9 minutes using an acid catalyst (bentonite/montmorillonite). The reactions produced chalcone (1,3-diphenyl-2-propen-1-on) and 4-methoxychalcone (1-phenyl-3-(4’-methoxy-phenyl)-2-propen-1-on). Percentage of products were obtained respectively 1.72% and 5.21%. The third compound 2’,4’-dihydroxychalcone couldnot be synthesized with microwave irradiation using bentonite/montmorillonite as catalyst on 400 Watt for 9 minutes. The reaction products were purified by column chromatography. Purity tests were carried out by thin layer chromatography (TLC) and the melting point test. The observed melting points were 51 oC and 73 oC for chalcone and 4-methoxychalcone. Identification of compounds were carried out by UVVIS , FT-IR and 1H-NMR spectroscopies

New Methyl Threonolactones and Pyroglutamates of Spilanthes acmella (L.) L. and Their Bone Formation Activities

In our continuing research for bioactive constituents from natural resources, a new methyl threonolactone glucopyranoside (1), a new methyl threonolactone fructofuranoside (2), 2 new pyroglutamates (3 and 4), and 10 known compounds (5–14) were isolated from the whole plant of Spilanthes acmella (L.) L. The structures of these compounds were determined based on various spectroscopic and chemical analyses. All of the isolated compounds were evaluated on bone formation parameters, such as ALP (alkaline phosphatase) and mineralization stimulatory activities of MC3T3-E1 cell lines. The results showed that the new compound, 1,3-butanediol 3-pyroglutamate (4), 2-deoxy-d-ribono-1,4-lactone (6), methyl pyroglutamate (7), ampelopsisionoside (10), icariside B1 (11), and benzyl α-l-arabinopyranosyl-(1→6)-β-d-glucopyranoside (12) stimulated both ALP and mineralization activities

Pemberdayaan Masyarakat dalam Upaya Pencegahan Penularan COVID-19 melalui Peningkatan Pemahaman dan Keterampilan Pembuatan Sabun Cuci Tangan Bunga Rosella pada Siswa Pesantren Di Gresik Sebagai Implementasi SDGs 3: Community Empowerment in Efforts to Prevent Transmission of COVID-19 through Increasing Understanding and Skills in Making Rosella Flower Hand Washing Soap for Islamic Boarding School Students in Gresik as Implementation of SDGs 3

Efforts to inhibit the transmission of COVID-19 are continuing to this day. One of them is using hand-washing soap to prevent the transmission of this virus. The Faculty of Pharmacy, Airlangga University, seeks to implement SDGs-3 through community service activities to increase community empowerment, especially for the younger generation. The utilization of natural ingredients containing many active compounds has yet to be discovered. The solution is to provide information on the source of the active ingredients for hand washing soap, for example, the Rosella flower, explaining the mechanism of soap in inhibiting the spread of viruses and how to make hand washing soap. The activity was carried out in Gresik with counseling and training methods. The outcome was an increase in participants' understanding, as indicated by an average post-test score of >65, with an increase in score of >10% compared to the pretest. In addition, one product of Rosela flower hand washing soap was also obtained. From this activity, it was concluded that there was an increase in understanding of 28%. It is hoped that this increase in understanding and skills for the younger generation can mobilize the surrounding community so that prevention of the transmission of COVID-19 is more massive and conditions of good health and well-being in society will be achieved.

Six New Phenylpropanoid Derivatives from Chemically Converted Extract of Alpinia galanga (L.) and Their Antiparasitic Activities

Chemical conversion of the extract of natural resources is a very attractive way to expand the chemical space to discover bioactive compounds. In order to search for new medicines to treat parasitic diseases that cause high morbidity and mortality in affected countries in the world, the ethyl acetate extract from the rhizome of Alpinia galanga (L.) has been chemically converted by epoxidation using dioxirane generated in situ. The biological activity of chemically converted extract (CCE) of A. galanga (L.) significantly increased the activity against Leishmania major up to 82.6 ± 6.2 % at 25 μg/mL (whereas 2.7 ± 0.8% for the original extract). By bioassay-guided fractionation, new phenylpropanoids (1–6) and four known compounds, hydroquinone (7), 4-hydroxy(4-hydroxyphenyl)methoxy)benzaldehyde (8), isocoumarin cis 4-hydroxymelein (9), and (2S,3S,6R,7R,9S,10S)-humulene triepoxide (10) were isolated from CCE. The structures of isolated compounds were determined by spectroscopic analyses of 1D and 2D NMR, IR, and MS spectra. The most active compound was hydroquinone (7) with IC50 = 0.37 ± 1.37 μg/mL as a substantial active principle of CCE. In addition, the new phenylpropanoid 2 (IC50 = 27.8 ± 0.34 μg/mL) also showed significant activity against L. major compared to the positive control miltefosine (IC50 = 7.47 ± 0.3 μg/mL). The activities of the isolated compounds were also evaluated against Plasmodium falciparum, Trypanosoma brucei gambisense and Trypanosoma brucei rhodeisense. Interestingly, compound 2 was selectively active against trypanosomes with potent activity. To the best of our knowledge, this is the first report on the bioactive “unnatural” natural products from the crude extract of A. galanga (L.) by chemical conversion and on its activities against causal pathogens of leishmaniasis, trypanosomiasis, and malaria