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 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 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.

Infrared, 1H-NMR Spectral Studies of some Methyl 6-O-Myristoyl-α-D-Glucopyranoside Derivatives: Assessment of Antimicrobial Effects

2015 ◽  
Vol 58 ◽  
pp. 122-136 ◽  
Author(s):  
Sarkar M.A. Kawsar ◽  
Khaleda Mymona ◽  
Refat Asma ◽  
Mohammad A. Manchur ◽  
Yasuhiro Koide ◽  
...  
Keyword(s):  
Pathogenic Fungi ◽  
Spectral Studies ◽  
Bacterial Strains ◽  
Substitution Product ◽  
Antifungal Activities ◽  
H Nmr ◽  
Antibacterial And Antifungal Activities ◽  
Fungal Phytopathogens ◽  
Antibacterial And Antifungal

This study was carried out to regioselective myristoylation of methyl α-D-glucopyranoside (1) using the direct acylation method gave the corresponding methyl 6-O-myristoyl-α-D-glucopyranoside (2) in fair yield. A number of 2,3,4-tri-O-acyl derivatives (3-15) of this 6-O-substitution product using a wide variety of acylating agents were also prepared in order to obtain newer derivatives of synthetic and biological importance. The reaction conditions are reasonably simple and yields were very good. The structures of the title compounds (2-15) were established by using analytical, physicochemical techniques and spectroscopic data (IR and 1H-NMR). All the synthesized compounds were employed as test chemicals for in vitro antimicrobial functionality test against Gram-positive Bacillus subtilis, Staphylococcus aureus, Gram-negative Escherichia coli, Pseudomonas aeruginosa bacteria and plant pathogenic fungi Aspergillus niger and Candida albicans. For comparative studies, antimicrobial activity of standard antibiotics, Ampicillin and Nystatin were also carried out against these microorganisms. The study revealed that the tested samples exhibited moderate to good antibacterial and antifungal activities. It was also observed that the test substances were more effective against fungal phytopathogens than those of the human bacterial strains. Encouragingly, a number of tested chemicals showed nearest antibacterial and antifungal activities with the standard antibiotics employed.

scholarly journals Biological evaluation of some octanoyl derivatives of methyl 4,6-O-cyclohexylidene-α-D-glucopyranoside

2013 ◽  
pp. 53-64 ◽  
Author(s):  
Abul KMS Kabir ◽  
Sarkar MA Kawsar ◽  
Mohammad MR Bhuiyan ◽  
Md Safiqur Rahman ◽  
Bilkiss Banu
Keyword(s):  
Pathogenic Bacteria ◽  
Biological Evaluation ◽  
Phytopathogenic Fungi ◽  
Bacterial Strains ◽  
Antibacterial And Antifungal Activities ◽  
Inhibition Concentration ◽  
Fungal Phytopathogens ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

Some acylated derivatives of methyl 4,6-O-cyclohexylidene-?-D-glucopyranoside, including the precursor, were employed as test compounds for in vitro antimicrobial functionality test against ten human pathogenic bacteria and six phytopathogenic fungi. For comparative studies, biological activity of standard antibiotics, Ampicillin and Nystatin were also carried out against these microorganisms. The study revealed that the tested samples exhibited moderate to good antibacterial and antifungal activities. It was also observed that the test substances were more effective against fungal phytopathogens than those of the bacterial strains. Encouragingly, a good number of test compounds exhibited better antimicrobial activity than the standard antibiotics employed. Minimum Inhibition Concentration (MIC) test of methyl 4,6-O-cyclohexylidene-3-Odecanoyl- 2-O-octanoyl-?-D-glucopyranoside was conducted against INABA ET (Vibrio) and MIC was found to be 12.5 ?g/disc. DOI: http://dx.doi.org/10.3329/cujbs.v3i1.13406 The Chittagong Univ. J. B. Sci.,Vol. 3(1&2):53-64, 2008

scholarly journals Synthesis and antimicrobial evaluation of some 1-(4-arylthiazol-2-yl)-1′-(aryl/heteroaryl)-3,3′-dimethyl-[4,5′-bi-1H-pyrazol]-5-ols

2017 ◽  
Vol 82 (2) ◽  
pp. 127-139 ◽  
Author(s):  
Satbir Mor ◽  
Rajni Mohil ◽  
Savita Nagoria ◽  
Ashwani Kumar
Keyword(s):  
Antibacterial Activities ◽  
Bacterial Strains ◽  
Antifungal Activities ◽  
Docking Simulations ◽  
Antibacterial And Antifungal Activities ◽  
Dehydroacetic Acid ◽  
Antimicrobial Evaluation ◽  
High Yields ◽  
Antibacterial And Antifungal

A series of sixteen 1-(4-arylthiazol-2-yl)-1?-(aryl/heteroaryl)-3,3?-dimethyl-[ 4,5?-bi-1H-pyrazol]-5-ols (7a?p) was synthesized starting from dehydroacetic acid (DHA, 1) via the stepwise formation of thiosemicarbazone (2), 3-(1-(2-(4-arylthiazol-2-yl)hydrazono)ethyl)-4-hydroxy-6-methyl-2H-pyran- -2-ones (4a?d) and 1-(1-(4-arylthiazol-2-yl)-5-hydroxy-3-methyl-1H-pyrazol- -4-yl)butane-1,3-diones (5a?d) in high yields. The in vitro antibacterial and antifungal activities of the synthesized bipyrazoles 7a?p were investigated against two Gram-positive bacterial strains, viz. Bacillus subtilis (MTCC 441) and Staphylococcus aureus (MTCC 7443), one Gram-negative bacterial strain, viz. Escherichia coli (MTCC 42), and two fungal strains, viz. Candida albicans (MTCC 183) and Aspergillus niger (MTCC 282). The compounds 7a and 7e were found to exhibit better inhibitory activity against A. niger than the reference fluconazole. Moreover, the antifungal activities of the title compounds were more prolific than their antibacterial activities. Furthermore, in order to study binding interactions, docking simulations of compounds 7a, 7m and 7o were performed into the active site of S. aureus 1,4-dihydroxy-2-naphthoyl- -CoA synthase. Keywords: bipyrazoles; antibacterial; antifungal; docking simulations.

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3-FORMYL INDOLE BASED SCHIFF BASES

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.

Substituted 4-Formyl-2H-chromen-2-ones: Their Reaction with N-(2,3,4,6-Tetra-Oacetyl- β-D-galactopyranosyl)thiosemicarbazide, Antibacterial and Antifungal Activity of Their Thiosemicarbazone Products

2020 ◽  
Vol 24 (19) ◽  
pp. 2272-2282
Author(s):  
Vu Ngoc Toan ◽  
Nguyen Minh Tri ◽  
Nguyen Dinh Thanh
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Selenium Dioxide ◽  
Antibacterial And Antifungal Activity ◽  
E Coli ◽  
Antibacterial And Antifungal Activities ◽  
Alkyl Ethers ◽  
Antibacterial And Antifungal

Several 6- and 7-alkoxy-2-oxo-2H-chromene-4-carbaldehydes were prepared from corresponding alkyl ethers of 6- and 7-hydroxy-4-methyl-2-oxo-2H-chromen-2-ones by oxidation using selenium dioxide. 6- and 7-Alkoxy-4-methyl-2H-chromenes were obtained with yields of 57-85%. Corresponding 4-carbaldehyde derivatives were prepared with yields of 41-67%. Thiosemicarbazones of these aldehydes with D-galactose moiety were synthesized by reaction of these aldehydes with N-(2,3,4,6-tetra-O-acetyl-β-Dgalactopyranosyl) thiosemicarbazide with yields of 62-74%. These thiosemicarbazones were screened for their antibacterial and antifungal activities in vitro against bacteria, such as Staphylococcus aureus, Escherichia coli, and fungi, such as Aspergillus niger, Candida albicans. Several compounds exhibited strong inhibitory activity with MIC values of 0.78- 1.56 μM, including 8a (against S. aureus, E. coli, and C. albicans), 8d (against E. coli and A. niger), 9a (against S. aureus), and 9c (against S. aureus and C. albicans).

scholarly journals Phytochemical investigation and in vitro antimicrobial activity of Richardia scabra

2016 ◽  
Vol 11 (2) ◽  
pp. 248 ◽  
Author(s):  
Kathirvel Poonkodi ◽  
Subban Ravi
Keyword(s):  
Antimicrobial Activity ◽  
Diffusion Method ◽  
Bacterial Strains ◽  
Weed Species ◽  
Antibacterial And Antifungal Activities ◽  
Agar Plug ◽  
Phytochemical Investigation ◽  
Antibacterial And Antifungal ◽  
Simple Sugar

<p class="Abstract">The present study was aimed to evaluate the phytochemical screening and antimicrobial activity of the petroleum ether and methanol extracts from the mature leaves of <em>Richardia scabra</em> from India. Disc diffusion method was used to determine the zone inhibition of the tested samples for antibacterial and agar plug method was used to determine the antifungal activity, while the microtube-dilution technique was used to determine the minimum inhibitory concentration. Both extracts showed significant antibacterial and antifungal activities when tested against 10 bacterial and four fungal strains. The minimum inhibitory concentrations of the methanol extract of<em> R. scabra</em> ranged between 12.5–100 μg/mL for bacterial strains. Alkaloids, steroids, flavonoids, fatty acids, terpenoids and simple sugar were detected as phytoconstituents of extracts. To the best of our knowledge, this is the first report against antimicrobial activity of common weed species <em>R. scabra</em> found in India.</p><p> </p>

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