scholarly journals Synthesis, Characterization, and Antibacterial Activities of Novel Sulfonamides Derived through Condensation of Amino Group Containing Drugs, Amino Acids, and Their Analogs

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Muhammad Abdul Qadir ◽  
Mahmood Ahmed ◽  
Muhammad Iqbal
Keyword(s):  
Amino Acids ◽  
Spectral Analysis ◽  
New Products ◽  
Antibacterial Activities ◽  
Amino Group ◽  
Bacterial Strains ◽  
Zone Of Inhibition ◽  
E Coli ◽  
Ft Ir

Novel sulfonamides were developed and structures of the new products were confirmed by elemental and spectral analysis (FT-IR, ESI-MS,1HNMR, and13CNMR). In vitro, developed compounds were screened for their antibacterial activities against medically important gram (+) and gram (−) bacterial strains, namely,S. aureus,B. subtilis,E. coli, andK. pneumoniae. The antibacterial activities have been determined by measuring MIC values (μg/mL) and zone of inhibitions (mm). Among the tested compounds, it was found that compounds 5a and 9a have most potent activity againstE. coliwith zone of inhibition:31±0.12 mm (MIC: 7.81 μg/mL) and30±0.12 mm (MIC: 7.81 μg/mL), respectively, nearly as active as ciprofloxacin (zone of inhibition:32±0.12 mm). In contrast, all the compounds were totally inactive against the gram (+)B. subtilis.

scholarly journals Amidine Sulfonamides and Benzene Sulfonamides: Synthesis and Their Biological Evaluation

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Muhammad Abdul Qadir ◽  
Mahmood Ahmed ◽  
Hina Aslam ◽  
Sadia Waseem ◽  
Muhammad Imtiaz Shafiq
Keyword(s):  
Spectral Analysis ◽  
New Products ◽  
Biological Evaluation ◽  
Bacterial Strains ◽  
Antifungal Activities ◽  
E Coli ◽  
Antibacterial And Antifungal Activities ◽  
Ft Ir ◽  
Antibacterial And Antifungal

New amidine and benzene sulfonamide derivatives were developed and structures of the new products were confirmed by elemental and spectral analysis (FT-IR, ESI-MS,1HNMR, and13CNMR). In vitro, developed compounds were screened for their antibacterial and antifungal activities against medically important bacterial strains, namely,S. aureus, B. subtilis, andE. coli, and fungi, namely,A. flavus, A. parasiticus, andA.sp. The antibacterial and antifungal activities have been determined by measuring MIC values (μg/mL) and zone of inhibitions (mm). Among the tested compounds, it was found that compounds3b,9a, and9bhave most potent activity againstS. aureus, A. flavus, and A. parasiticus, respectively, and were found to be more active than sulfamethoxazole and itraconazole with MIC values 40 μg/mL. In contrast, all the compounds were totally inactive against theA.sp. except10band15bto show activity to some extent.

scholarly journals Design, Synthesis and Biological Evaluation of Novel Benzothiazole Based [1,2,4]Triazolo[4,3-c]quinazoline Derivatives

2020 ◽  
Vol 32 (3) ◽  
pp. 580-586
Author(s):  
Ranjit V. Gadhave ◽  
Bhanudas S. Kuchekar
Keyword(s):  
Biological Evaluation ◽  
Bacterial Strains ◽  
Active Compounds ◽  
Design Synthesis ◽  
Structural Modifications ◽  
E Coli ◽  
Chemical Structures ◽  
Ft Ir ◽  
Antioxidant Agent

A new series of N-(benzo[d]thiazol-2-yl)-[1,2,4]triazolo[4,3-c]quinazoline-5-carboxamide derivatives were synthesized by condensation of [1,2,4]triazolo[4,3-c]quinazoline-5-carboxylate derivatives with substituted benzothiazoles. The chemical structures of the synthesized compounds were confirmed by FT-IR, MS and 1H NMR spectra. Designed triazoloquinazoline derivatives were docked with oxido-reductase enzyme (PDB Code 4h1j) and DNA gyrase enzyme (PDB Code 3g75). Based on high binding affinity score, the best compound were selected for synthesis and subjected to in vitro antioxidant and antibacterial activity. Compounds 7a and 7d were found to be most active compounds as antioxidant agent among this series when compared with ascorbic acid. Compounds 7a, 7d and 7f were found to be most active compounds as an antibacterial agents among this series when compared with ciprofloxacin against bacterial strains such as S. aureus (ATCC 25923), E. coli (ATCC 25922) and P. aeruginosa (ATCC 27853). Study revealed that the most active compounds after structural modifications can be exploited as lead molecules for other pharmacological activities such as anti-inflammatory, anticancer and antidepressant activities.

scholarly journals Simonkolleite Coating on Poly(Amino Acids) to Improve Osteogenesis and Suppress Osteoclast Formation in Vitro

Polymers ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 1505 ◽  
Author(s):  
Shuyang Li ◽  
Xingtao Chen ◽  
Xiaomei Wang ◽  
Yi Xiong ◽  
Yonggang Yan ◽  
...  
Keyword(s):  
Amino Acids ◽  
Osteoclast Formation ◽  
Mouse Bone Marrow ◽  
Graft Material ◽  
Dependent Manner ◽  
E Coli ◽  
Ft Ir ◽  
Dose Dependent ◽  
Relative Cell Viability

Zinc can enhance osteoblastic bone formation and stimulate osteogenic differentiation, suppress the differentiation of osteoclast precursor cells into osteoclasts, and inhibit pathogenic bacterial growth in a dose-dependent manner. In this study, simonkolleite, as a novel zinc resource, was coated on poly (amino acids) (PAA) via suspending PAA powder in different concentrations of zinc chloride (ZnCl2) solution, and the simonkolleite-coated PAA (Zn–PAA) was characterized by SEM, XRD, FT-IR and XPS. Zinc ions were continuously released from the coating, and the release behavior was dependent on both the concentration of the ZnCl2 immersing solution and the type of soak solutions (SBF, PBS and DMEM). The Zn–PAA was cultured with mouse bone marrow stem cells (BMSCs) through TranswellTM plates, and the results indicated that the relative cell viability, alkaline phosphatase (ALP) activity and mineralization of BMSCs were significantly higher with Zn–PAA as compared to PAA. Moreover, the Zn–PAA was cultured with RAW264.7 cells, and the results suggested an inhibiting effect of Zn–PAA on the cell differentiation into osteoclasts. In addition, Zn–PAA exhibited an antibacterial activity against both S. aureus and E. coli. These findings suggest that simonkolleite coating with certain contents could promote osteogenesis, suppress osteoclast formation and inhibit bacteria, indicating a novel way of enhancing the functionality of synthetic bone graft material and identifying the underline principles for designing zinc-containing bone grafts.

scholarly journals Indole-3-carbaldehyde Semicarbazone Derivatives: Synthesis, Characterization, and Antibacterial Activities

2020 ◽  
Vol 2020 ◽  
pp. 1-9 ◽  
Author(s):  
Fernando Carrasco ◽  
Wilfredo Hernández ◽  
Oscar Chupayo ◽  
Celedonio M. Álvarez ◽  
Sandra Oramas-Royo ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Bacillus Subtilis ◽  
Antibacterial Activities ◽  
Isomeric Form ◽  
Bacterial Strains ◽  
H Nmr ◽  
Nmr Techniques ◽  
Ft Ir ◽  
Liquid Acetone

Four indole-3-carbaldehyde semicarbazone derivatives, 2-((5-bromo-1H-indol-3-yl)methylene)hydrazinecarboxamide (1), 2-((5-chloro-1H-indol-3-yl)methylene)hydrazinecarboxamide (2), 2-((5-methoxy-1H-indol-3-yl)methylene)hydrazinecarboxamide (3), and 2-((4-nitro-1H-indol-3-yl)methylene)hydrazinecarboxamide (4) were synthesized and characterized by ESI-MS and spectroscopic (FT-IR, 1H NMR, and 13C NMR) techniques. The two-dimensional NMR (in acetone-d6) spectral data revealed that the molecules 1 and 2 in solution are in the cisE isomeric form. This evidence is supported by DFT calculations at the B3LYP/6-311++G(d,p) level of theory where it was shown that the corresponding most stable conformers of the synthesized compounds have a cisE geometrical configuration, in both the gas and liquid (acetone and DMSO) phases. The in vitro antibacterial activity of compounds 1–4 was determined against Gram-positive (Staphylococcus aureus and Bacillus subtilis) and Gram-negative (Pseudomonas aeruginosa and Escherichia coli) bacteria. Among all the tested semicarbazones, 1 and 2 exhibited similar inhibitory activities against Staphylococcus aureus (MIC = 100 and 150 μg/mL, respectively) and Bacillus subtilis (MIC = 100 and 150 μg/mL, respectively). On the other hand, 3 and 4 were relatively less active against the tested bacterial strains compared with 1, 2, and tetracycline.

scholarly journals Novel Synthesis and Antimicrobial Activities of Thiazino-Oxazine Derivatives

2018 ◽  
Vol 10 (4) ◽  
Author(s):  
Dr.Pravina B. Piste
Keyword(s):  
Spectral Analysis ◽  
Heterocyclic Compounds ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Plate Method ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli ◽  
Novel Synthesis

In the designing and synthesis of new heterocyclic compounds, containing two different pharmacophores, we have carried out new series of 3-(4-chlorophenyl)-4-methylidene-4,8-dihydro-2H,5H-1,3-thiazino[5,4-e]-1,3-oxazine-2,5,7(3H)-trione derivatives (5a-5k) in good yields from the cyclization of 5-[(1E)-N- (4-chlorophenyl) ethanimidoyl] -4-hydroxy- 2H-1,3- thiazine-2,6(3H)-dione derivatives (4a-4k) with triphosgene. All the synthesized compounds (5a-5k) were confirmed by spectral analysis. The synthesized compounds (5a-5k) were screened in vitro for their antibacterial activities against S. subtilis (gram positive) and E. coli. (gram negative) while antifungal activity against C. albicans by cup plate method. Some of the products of series were found to have quite good activities as compared to the standard drug streptomycin and flucanozole.

scholarly journals Anthraquinones from the Roots of Kniphofia insignis and Evaluation of Their Antimicrobial Activities

2021 ◽  
Vol 2021 ◽  
pp. 1-5
Author(s):  
Asnakew Amare Tadesse ◽  
Negera Abdissa Ayana ◽  
Dele Abdissa Keneni
Keyword(s):  
Antimicrobial Activities ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Zone Of Inhibition ◽  
Fusarium Spp ◽  
E Coli ◽  
Spectroscopic Analyses ◽  
Crude Extracts ◽  
Antimicrobial Assay

Sequential extraction using a cold maceration method and column chromatographic separation of the roots Kniphofia insignis headed to the isolation of three anthraquinones: one monomeric anthraquinone (1) and two dimeric anthraquinones (2 and 3). It was further purified by Sephadex LH-20 and recrystallized. The structures of these compounds were established based on the spectroscopic analyses including NMR (1H-NMR and 13C-NMR and infrared) and comparison with reported literatures. In an in vitro antimicrobial assay of the crude extracts, the isolated compounds were made against four bacterial strains (S. aureus ATCC 25923, B. subtilis ATCC 6633, E. coli ATCC 35218, and P. aeruginosa ATCC 27853) and Fusarium spp. fungal strain. In the crude extracts of chloroform, substantial antimicrobial activity was seen with the highest activity against B. subtilis (16 mm) and E. coli (22 mm). Meanwhile, compound 1 has a better zone of inhibition with 14 mm against P. aeruginosa, whereas compound 2 showed better activity (13 mm) against Fusarium spp. fungal strain.

Copper(II) mixed-ligand complexes containing 1, 10-phenanthroline, adenine and thymine: Synthesis, characterization and antibacterial activities

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Copper Complexes ◽  
Antimicrobial Agents ◽  
Conductivity Measurement ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
Bacterial Strains ◽  
E Coli ◽  
In Vivo Cytotoxicity

New copper complexes, [Cu(phen)2(Thy)]2Cl and [Cu(phen)2(Ad)]2Cl (phen = 1,10-phenantroline, Ad (Adenine, a purine nucleobase) and Thy (Thymine, a pyrimidine nucleobase)), were synthesized and characterized by atomic absorption spectroscopy (AAS), conductivity measurement, UV-visible and infrared (IR) techniques. The complexes were tested for their antimicrobial activity against two gram positive and two gram negative bacterial strains. The results of in vitro antimicrobial activities were compared with the commercially available antimicrobial agents (ciprofloxacin and chloramphenicol). This comparative study has demonstrated that [Cu(phen)2(Thy)]2Cl inhibited the growth of methicillin resistant Staphylococcus aureous (MRSA), Escherichia coli (E. coli) and Klebsiella pneumoniae (K. pneumonia) better than chloramphenicol by 11.25%, 19.41% and 25.35%, respectively. It also showed better activities than ciprofloxacine on MRSA and K. pneumoniae by 2.50% and 12.13%, respectively. Similarly, [Cu(phen)2(Ad)]2Cl demonstrated better inhibitions than chloramphenicol against MRSA, E. coli and K. pneumoniae by 11.24%, 2.48% and 9.06%, respectively. Therefore, after in vivo cytotoxicity investigations, these complexes could be considered as potential antimicrobial agents.

scholarly journals Phytochemical Analysis, Antioxidant and Antimicrobial Screening of Seriphidium Oliverianum Plant Extracts

Dose-Response ◽  
2021 ◽  
Vol 19 (1) ◽  
pp. 155932582110047
Author(s):  
Ali Abbas ◽  
Syed Ali Raza Naqvi ◽  
Muhammad Hidayat Rasool ◽  
Asma Noureen ◽  
Muhammad Samee Mubarik ◽  
...  
Keyword(s):  
Methanol Extract ◽  
Reducing Power ◽  
Antibacterial Activities ◽  
Total Phenolic ◽  
Phytochemical Analysis ◽  
Bacterial Strains ◽  
Zone Of Inhibition ◽  
Dpph Scavenging

The aim of this study was to investigate the phytochemicals using reverse-phase high pressure liquid chromatography (RP-HPLC), antioxidant, antifungal and antibacterial activities of Seriphidium oliverianum stem extracts. The extraction was carried out by conventional shaking process (CSP) and ultrasonic assisted process (UAP). The highest total phenolic contents (97.85 ± 0.735 mg gallic acid equivalent (GAE)/g sample) and flavonoid contents (188.15 ± 0.53 mg catechin equivalent (CE)/g sample) were found in methanol extract obtained by CSP. Antioxidant activity was investigated using DPPH° scavenging assay and reducing power assay. Methanol extract using UAP showed the highest DPPH° scavenging activity (79.95% ± 1.80%) followed by methanol and butanol extracts obtained through CSP. Moreover, methanol extracts using CSP showed highest reducing activity (1.032 ± 0.0205 absorbance). In-vitro antimicrobial activity was studied using most common infection causing fungal and bacterial strains. Anti-fungal activity of methanol extract using CSP showed the highest zone of inhibition (10.5 mm) against F. avenaceum fungal strain, while aqueous extracts obtained through showed the highest antibacterial activity (22 ± 1.32 mm zone of inhibition) against S. aureus. The results showed that the methanol stem extract of S. oliverianum is a valued candidate for further screening and could be processed for in-vivo infection induced animal trials.

scholarly journals Substrate specificities of Escherichia coli ItaT that acetylates aminoacyl-tRNAs

2020 ◽  
Author(s):  
Chuqiao Zhang ◽  
Yuka Yashiro ◽  
Yuriko Sakaguchi ◽  
Tsutomu Suzuki ◽  
Kozo Tomita
Keyword(s):  
Escherichia Coli ◽  
Amino Acids ◽  
Amino Group ◽  
Hydrophobic Pocket ◽  
Hydrophobic Residues ◽  
Substrate Specificities ◽  
E Coli ◽  
Hydrophobic Amino Acids

Abstract Escherichia coli ItaT toxin reportedly acetylates the α-amino group of the aminoacyl-moiety of Ile-tRNAIle specifically, using acetyl-CoA as an acetyl donor, thereby inhibiting protein synthesis. The mechanism of the substrate specificity of ItaT had remained elusive. Here, we present functional and structural analyses of E. coli ItaT, which revealed the mechanism of ItaT recognition of specific aminoacyl-tRNAs for acetylation. In addition to Ile-tRNAIle, aminoacyl-tRNAs charged with hydrophobic residues, such as Val-tRNAVal and Met-tRNAMet, were acetylated by ItaT in vivo. Ile-tRNAIle, Val-tRNAVal and Met-tRNAMet were acetylated by ItaT in vitro, while aminoacyl-tRNAs charged with other hydrophobic residues, such as Ala-tRNAAla, Leu-tRNALeu and Phe-tRNAPhe, were less efficiently acetylated. A comparison of the structures of E. coli ItaT and the protein N-terminal acetyltransferase identified the hydrophobic residues in ItaT that possibly interact with the aminoacyl moiety of aminoacyl-tRNAs. Mutations of the hydrophobic residues of ItaT reduced the acetylation activity of ItaT toward Ile-tRNAIlein vitro, as well as the ItaT toxicity in vivo. Altogether, the size and shape of the hydrophobic pocket of ItaT are suitable for the accommodation of the specific aminoacyl-moieties of aminoacyl-tRNAs, and ItaT has broader specificity toward aminoacyl-tRNAs charged with certain hydrophobic amino acids.

SYNTHESIS, ANTIBACTERIAL EVALUATION AND DOCKING STUDIES OF SOME NOVEL ISATIN DERIVATIVES

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (03) ◽  
pp. 7-12
Author(s):  
N. Venkateshan ◽  
◽  
R Rajapandi ◽  
P. Kaniga
Keyword(s):  
Antibacterial Activities ◽  
Mannich Bases ◽  
Docking Studies ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Binding Model ◽  
Molegro Virtual Docker ◽  
E Coli ◽  
In Vitro Antibacterial Activity

Benzylimino isatin Mannich bases (IS1 & IM1-IM6) were designed manually and synthesized by the simple Mannich reaction. The synthesized compounds were confirmed by means of their spectral evidence (FTIR, 1H NMR and ESI-MS). The antibacterial activities were carried out with Gram +ve as well as Gram -ve bacteria by disc diffusion method. All the compounds showed moderate In vitro antibacterial activity, particularly, compound IM4 (E)-3-(benzylimino)-1-[(4-methylpiperazin-1-yl)methyl]indolin-2 -one showed better activity with 19, 17, 17 and 11 mm zone of inhibition at 100 μg/0.1 mL concentration against Gram +ve bacteria (S. aureus, B. subtilis) and Gram –ve bacteria (P. eruginosa, E. coli) respectively compared to standard fluoroquinolone antibacterial ciprofloxacin, which have 30 mm zone of inhibition at 10 μg/0.1 mL concentration in Gram +ve bacteria (B. Subtilus) as well as Gram -ve bacteria (P. eruginosa). Molecular docking studies were carried out for active compound IM4 with DNA gyrase enzyme (1kzn) protein by Molegro Virtual Docker 2013.1.6 (MVD), in order to determine the probable binding model in to active site of 1kzn with the compound IM4.

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