scholarly journals Synthesis and In Vitro Evaluation of C-methylcalix[4]resorcinaryl octacinnamate and C-methylcalix[4]resorcinaryl octabenzoate as the Sunscreen

2017 ◽  
Vol 17 (1) ◽  
pp. 63 ◽  
Author(s):  
Budiana I Gusti M. Ngurah ◽  
Jumina Jumina ◽  
Chairil Anwar ◽  
Sunardi Sunardi ◽  
Mustofa Mustofa
Keyword(s):  
Benzoic Acid ◽  
Mtt Assay ◽  
13C Nmr ◽  
Benzoyl Chloride ◽  
Spectroscopic Method ◽  
Activity Test ◽  
Acid Catalyzed ◽  
Amino Benzoic Acid

The present study was aimed to synthesize and evaluate sunscreen activity of C-methylcalix[4]resorcinaryl octacinnamate and C-methylcalix[4]resorcinaryl octabenzoate. The target compounds were synthesized in 2 steps. They were a synthesis of C-methylcalix[4]-resorcinarene via acid catalyzed the condensation of resorcinol and acetaldehyde by using HCl catalyst, followed by esterification using cinnamoyl chloride and benzoyl chloride. The characterization of the target compounds was performed by IR, 1H-NMR, 13C-NMR, and LC-MS spectrometers. The sunscreen activity test was conducted by spectroscopic method and MTT-assay. Commercial sunscreen p-amino benzoic acid (PABA) was used as a comparator to the MTT assay. The sunscreen activity test used spectroscopic showed that C-methylcalix[4]resorcinaryl octacinnamate and C-methylcalix[4]resorcinaryl octabenzoate can absorb the ultraviolet radiation between 280 and 320 nm (UV-B) with the maximum absorption at 290 nm (ε = 31.535 M-1 cm-1) and 282 nm (ε = 42.217 M-1 cm-1), respectively. The results of MTT-assay indicated that the IC50 of C-methylcalix[4]resorcinaryl octacinnamate, C-methylcalix[4]resorcinaryl octabenzoate and PABA are 12.006, 20.568 and 12.564 ppm, respectively, it means that the order of sunscreen activity is C-methylcalix-[4]resorcinaryl octacinnamate, PABA and C-methylcalix[4]resorcinaryl octabenzoate.

scholarly journals Synthesis and Characterization of some New 1,3,4-Oxadiazole derivatives based on 4-amino benzoic acid

2016 ◽  
Vol 13 (4) ◽  
pp. 762-769
Author(s):  
Baghdad Science Journal
Keyword(s):  
Schiff Base ◽  
Benzoic Acid ◽  
Spectral Data ◽  
1H Nmr ◽  
Synthesis And Characterization ◽  
Oxadiazole Derivatives ◽  
Ft Ir ◽  
Amino Benzoic Acid

Various of 2,5- disubstituted 1,3,4-oxadiazole (Schiff base, ?- lactam and azo) were synthesized from 2,5-di (4,4?-amino-1,3,4-oxadiazole which usequently synth-esized from mixture of 4- amino benzoic acid and hydrazine arch of polyphosphorus acid. The synthesized compounds were cherecterized by using some spectral data (UV, FT-IR , and 1H-NMR)

Fabrication and characterization of bovine hydroxyapatite-gelatin-alendronate scaffold cross-linked by glutaraldehyde for bone regeneration

2021 ◽  
Vol 32 (4) ◽  
pp. 555-560
Author(s):  
Samirah ◽  
Aniek Setiya Budiatin ◽  
Ferdiansyah Mahyudin ◽  
Junaidi Khotib
Keyword(s):  
Compressive Strength ◽  
Bone Regeneration ◽  
Mtt Assay ◽  
Local Treatment ◽  
Swelling Ratio ◽  
High Concentration ◽  
Proliferation And Differentiation ◽  
Bovine Hydroxyapatite

Abstract Objectives Alendronate are widely used in the treatment of bone disorders characterized by inhibit osteoclast-mediated bone resorption such as Paget’s disease, fibrous dysplasia, myeloma, bone metastases and osteoporosis. In recent studies alendronate improves proliferation and differentiation of osteoblasts, thereby facilitating for bone regeneration. The disadvantages of this class are their poor bioavailability and side effects on oral and intravenous application such as stomach irritation and osteonecrosis in jaw. Thus, local treatment of alendronate is needed in order to achieve high concentration of drug. Bovine hydroxyapatite-gelatin scaffold with alendronate was studied. Glutaraldehyde was used as cross-linking agent, increase the characteristics of this scaffold. The objectives of this study were to manufacture and characterize alendronate scaffold using bovine hydroxyapatite-gelatin and crosslinked by glutaraldehyde. Methods Preparation of cross-linked bovine hydroxyapatite-gelatin and alendronate scaffold with different concentration of glutaraldehyde (0.00, 0.50, 0.75, and 1.00%). The scaffolds were characterized for compressive strength, porosity, density, swelling ratio, in vitro degradation, and cytotoxicity (the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide assay, shorted as MTT assay). Results Bovine hydroxyapatite-gelatin-alendronate scaffold cross-linked with glutaraldehyde showed lower density than without glutaraldehyde. As glutaraldehyde concentration increased, porosity also increased. Eventually, it reduced compressive strength. Swelling ratio and in vitro degradation was negatively dependent on glutaraldehyde concentration. In addition, the scaffold has a good safety by MTT assay. Conclusions Bovine hydroxyapatite-gelatin-alendronate scaffold was fabricated with various concentrations of glutaraldehyde. The presence of glutaraldehyde on bovine hydroxyapatite-gelatin-alendronate is safe and suitable candidate scaffold for bone regeneration.

scholarly journals Arylsulfonamides From the Roots and Rhizomes of Tupistra chinensis Baker

2020 ◽  
Vol 15 (4) ◽  
pp. 1934578X2092166
Author(s):  
Yue Xu ◽  
Xiaofei Liang ◽  
Yuze Li ◽  
Zhuofei Liang ◽  
Wenli Huang ◽  
...  
Keyword(s):  
Benzoic Acid ◽  
Cell Lines ◽  
Human Cancer ◽  
Acid Methyl Ester ◽  
Spectroscopic Methods ◽  
Tumor Cell Lines ◽  
Human Cancer Cell Lines ◽  
Acid Methyl ◽  
Amino Benzoic Acid

One new arylsulfonamide (1) and a novel natural product (2) were isolated from the roots and rhizomes of Tupistra chinensis Baker. Their structures were characterized by physicochemical properties and spectroscopic methods, as 2-[2-([1,1′-biphenyl]-4-ylsulfonylamino)-benzoylamino]-benzoic acid methyl ester (1), 2-[([1,1′-biphenyl]-4-ylsulfonyl)amino]-benzoic acid (2), respectively. Additionally, the cytotoxic activity of 1-2 was evaluated on human HCT116, HT29, A549, and H1299 tumor cell lines in vitro, respectively. Whereas, the result showed that these compounds displayed weak cytotoxicity in the human cancer cell lines.

Synthesis and structural characterization of binuclear ytterbium(III) complexes with 2-amino and 3-amino benzoic acid

2014 ◽  
Vol 40 (9) ◽  
pp. 686-694 ◽  
Author(s):  
S. Hussain ◽  
I. U. Khan ◽  
M. Akkurt ◽  
S. Ahmad ◽  
M. N. Tahir
Keyword(s):  
Benzoic Acid ◽  
Structural Characterization ◽  
Amino Benzoic Acid

In Methanolic Solvent Synthesis of New MnII, CoII, NiII and CuII Schiff Base of Aromatic β Amino Acids: Spectroscopic, Thermal, Molecular Docking and Antimicrobial Studies

2020 ◽  
Vol 12 (8) ◽  
pp. 1137-1148 ◽  
Author(s):  
Asma S. Al-Wasidi ◽  
Nawal M. Al-Jafshar ◽  
Amal M. Al-Anazi ◽  
Moamen S. Refat ◽  
Nashwa M. El-Metwaly ◽  
...  
Keyword(s):  
Schiff Base ◽  
Molecular Docking ◽  
Amino Acid ◽  
Benzoic Acid ◽  
Molar Conductance ◽  
Schiff Base Complexes ◽  
Proton Nuclear Magnetic Resonance ◽  
Antimicrobial Studies ◽  
Amino Benzoic Acid

In this article, four new Schiff base complexes of Mn(II), Co(II), Ni(II) and Cu(II) complexes have been synthesized with two different compositions as [M(L)2Cl2] · nH2O and [M(L)2(H2O)2]Cl2 · nH2O [where L1 = benzoin-o-amino benzoic acid (aromatic β amino acid) and L2 = benzoin bromo-o-amino benzoic acid (aromatic β amino acid); M = MnII, CoII, NiII and CuII; n = 1, 2 and 4]. These Schiff base complexes were discussed by many tool of analyses like elemental analysis, magnetic susceptibility, molar conductance, mass spectra, infrared spectra "IR," proton nuclear magnetic resonance "1H-NMR," electronic spectral and thermogravimetric analysis (TG/DTG). These complexes have an electrolytic nature within range of 78–174 Ω1 cm–1 mol –1 based on conductance measurements. Magnetic moment and electronic spectral results deduced that the geometry of Mn2+, Co2+ and Ni2+ and Cu2+ complexes has an octahedral configuration. The number of coordinated and uncoordinated water molecules for the synthesized complexes were calculated based on the thermal analysis technique. The kinetic thermodynamic data were estimated by using commonly integral equations of Horowitz-Metzger (HM) and Coats-Redfern (CR). In vitro the antimicrobial activity of both free L1 and L2 ligands in comparable with their metal complexes were evaluated. This study was strengthen by molecular docking against three protein receptors, which attributing to selected organisms already used in vitro study.

Synthesis and Characterization of some new Schiff base Compounds derived from 4-Amino benzoic acid and study their Biological activity

2019 ◽  
Vol 12 (5) ◽  
pp. 2207
Author(s):  
Mahdi F. Radi ◽  
Suhair S. Husain ◽  
Abrar Natek Mohammed Zaki ◽  
Alaa A. Sultan ◽  
Wejdan Mahmmod Hamed ◽  
...  
Keyword(s):  
Biological Activity ◽  
Schiff Base ◽  
Benzoic Acid ◽  
Synthesis And Characterization ◽  
Amino Benzoic Acid

scholarly journals Synthesis, characterization and anthelmintic activity evaluation of pyrimidine derivatives bearing carboxamide and sulphonamide moieties

2018 ◽  
Vol 83 (4) ◽  
pp. 401-409 ◽  
Author(s):  
David Ugwu ◽  
Uchechukwu Okoro ◽  
Narendra Mishra
Keyword(s):  
Amino Acids ◽  
Boric Acid ◽  
1H Nmr ◽  
13C Nmr ◽  
Benzoyl Chloride ◽  
Anthelmintic Activity ◽  
Pharmacological Properties ◽  
Pyrimidine Derivatives ◽  
Different Types

Pyrimidines, sulphonamides and carboxamides have shown a large number of pharmacological properties against different types of diseases including helminthiasis. Seventeen new pyrimidine derivatives bearing sulphonamide and carboxamide were synthesized and investigated for their in vitro anthelmintic properties. Substituted benzenesulphonyl chlorides 15a?c were treated with various amino acids (16a?h) to obtain benzenesulphonamide derivatives 17a?l. Compounds 17a?f were subsequently treated with benzoyl chloride to obtain the N-benzoylated derivatives 19a?f. Further reactions of compounds 19a?f and 17g?l with 4- or 2-aminopyrimidine (20) using boric acid as a catalyst gave the required sulphonamide carboxamide derivatives 21a?q in excellent yields. The compounds were isolated in their analytical grade and characterized using FTIR, 1H-NMR, 13C-NMR and HRMS. The in vitro anthelmintic studies showed that all the synthesized compounds possessed anthelmintic property. Compounds 21a?c, e, g, m and p showed mean paralyzing times of 15, 19, 14, 18, 19, 19 and 18 min, respectively, at 100 mg mL-1 compared to 10 min for albendazole. Compounds 21a?c, g and m had mean death times of 18, 24, 16, 20 and 25 min, respectively, at 100 mg mL-1 compared to 13 min for albendazole.

Synthesis and Characterization of Novel 1,3,5-Thiadiazine Derivatives Integrated with Quinoline Moiety as Potent Antimicrobial Agents

2020 ◽  
Vol 5 (2) ◽  
pp. 149-155
Author(s):  
M. Idrees ◽  
Naqui J. Siddiqui ◽  
Yogita G. Bodkhe ◽  
Satish Kola
Keyword(s):  
13C Nmr ◽  
Mass Spectra ◽  
Antimicrobial Agents ◽  
Synthesis And Characterization ◽  
Pathogenic Microorganism ◽  
Bacterial Strains ◽  
Gram Negative ◽  
E Coli

An expeditious synthesis of series of novel 1,3,5-thiadiazine (5a-f) and (6a-f) derivatives have been described. These compounds were synthesized by reaction of 1-(N-((6-methyl-2-(p-tolyloxy)quinoline- 3-yl)methylene)carbamimidoyl)-3-arylthiourea (3a-b) derivatives with N-aryl isocyanodichloride (4a-c) in chloroform followed by basification with dilute NH4OH to give the target compounds 5a-f; which were acetylated further to afford six novel 1,3,5-thiadiazin-3-(6H)-yl)ethanone (6a-f) derivatives. Synthesis of intermediate compounds 3a-b was obtained by reacting 6-methyl-2-(p-tolyloxy)quinoline-3- carbaldehyde (2a) and 1-carbamimidoyl-3-aryllthiourea (1a-b) in chloroform. Structures of compounds 5a-f and 6a-f were established by FTIR, 1H & 13C NMR, mass spectra and further supported by elemental analysis. All synthesized compounds were investigated for their in vitro antimicrobial screening against a panel of pathogenic microorganism comprising S. aureus as Gram positive while E. coli, P. vulgaris, S. typhi as Gram-negative bacterial strains.

scholarly journals In Vitro Activities of Position 2 Substitution-Bearing 6-Nitro- and 6-Amino-Benzothiazoles and Their Corresponding Anthranilic Acid Derivatives against Leishmania infantum and Trichomonas vaginalis

2002 ◽  
Vol 46 (8) ◽  
pp. 2588-2594 ◽  
Author(s):  
Florence Delmas ◽  
Carole Di Giorgio ◽  
Maxime Robin ◽  
Nadine Azas ◽  
Monique Gasquet ◽  
...  
Keyword(s):  
Benzoic Acid ◽  
Anthranilic Acid ◽  
Leishmania Infantum ◽  
Trichomonas Vaginalis ◽  
No Production ◽  
Protective Mechanisms ◽  
Anthranilic Acid Derivatives ◽  
Intracellular Amastigote ◽  
Amino Benzoic Acid

ABSTRACT 6-Nitro- and 6-amino-benzothiazoles bearing different chains in position 2 and their corresponding anthranilic acid derivatives were investigated for their in vitro antiparasitic properties against parasites of the species Leishmania infantum and Trichomonas vaginalis compared to their toxicity towards human monocytes. Biological investigations established that the antiprotozoal properties depended greatly on the chemical structure of the position 2 substitution-bearing group. Compound C1, 2-[(2-chloro-benzothiazol-6-yl) amino] benzoic acid, demonstrated an interesting antiproliferative activity towards parasites of the species T. vaginalis, while compound C11, 2-({2-[(2-hydroxyethyl) amino]-benzothiazol-6-yl} amino) benzoic acid, exhibited a promising activity against parasites of the species L. infantum in their intracellular amastigote form. Additional experiments established that compound C11, which was poorly toxic against the promastigote and the extracellular amastigote forms of the parasite, could improve host-protective mechanisms against Leishmania by preventing parasite internalization by macrophages and stimulating NO production, by means of a mechanism synergistically enhanced by the presence of gamma interferon.

Para-amino benzoic acid (PABA) modulates expression and stability of CDC25A in tumor cells and enhances radiosensitivity in vitro and in vivo

2004 ◽  
Vol 60 (1) ◽  
pp. S360-S361
Author(s):  
S. Xavier ◽  
J. Roth ◽  
M. Caunt ◽  
A. Akalu ◽  
D. Rodriguez ◽  
...  
Keyword(s):  
Benzoic Acid ◽  
Tumor Cells ◽  
Amino Benzoic Acid
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