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.

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 Design, Synthesis, and Bioactivity Evaluation of New Thiochromanone Derivatives Containing a Carboxamide Moiety

Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4391
Author(s):  
Lingling Xiao ◽  
Lu Yu ◽  
Pei Li ◽  
Jiyan Chi ◽  
Zhangfei Tang ◽  
...  
Keyword(s):  
Antibacterial Activities ◽  
Xanthomonas Oryzae ◽  
Design Synthesis ◽  
Compound A ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
In Vitro Antibacterial Activity ◽  
Antibacterial And Antifungal ◽  
In Vitro Antifungal Activity

In this study, using the botanical active component thiochromanone as the lead compound, a total of 32 new thiochromanone derivatives containing a carboxamide moiety were designed and synthesized and their in vitro antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo), Xanthomonas oryzae pv. oryzicolaby (Xoc), and Xanthomonas axonopodis pv. citri (Xac) were determined, as well as their in vitro antifungal activities against Botryosphaeria dothidea (B. dothidea), Phomopsis sp., and Botrytis cinerea (B. cinerea). Bioassay results demonstrated that some of the target compounds exhibited moderate to good in vitro antibacterial and antifungal activities. In particular, compound 4e revealed excellent in vitro antibacterial activity against Xoo, Xoc, and Xac, and its EC50 values of 15, 19, and 23 μg/mL, respectively, were superior to those of Bismerthiazol and Thiodiazole copper. Meanwhile, compound 3b revealed moderate in vitro antifungal activity against B. dothidea at 50 μg/mL, and the inhibition rate reached 88%, which was even better than that of Pyrimethanil, however, lower than that of Carbendazim. To the best of our knowledge, this is the first report on the antibacterial and antifungal activities of this series of novel thiochromanone derivatives containing a carboxamide moiety.

scholarly journals Biological Activity of Phenothiazine Sulfonamides

2019 ◽  
Vol 8 (2S6) ◽  
pp. 535-537
Keyword(s):  
Rhizopus Oryzae ◽  
Antibacterial Activities ◽  
Bacillus Sphaericus ◽  
Dilution Method ◽  
Curvularia Lunata ◽  
Gram Negative ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Background: Antibacterial activities in “dimethylsulfoxide (DMSO)” were executed by the broth dilution method utilizing nutrient agar. By using the agar cup bioassay method antifungal activities were calculated with “Clotrimazole” as the standard. The novel compounds 1a-j have been evaluated in vitro for their antibacterial activity by “Gram-positive bacteria namely Bacillus subtilis, Bacillus sphaericus and Staphylococcus aureus and three Gram-negative bacteria Pseudomonas aeruginosa”, “Klebsiella aerogenes and Chromobacterium violaceum”. All ten compounds were analysed for their antifungal activity against five test “organisms Aspergillus niger, Chrysosporium tropicum, Rhizopus oryzae, Fusarium moniliforme and Curvularia lunata”. Among the isolated compounds 1d and 1e evinced dynamic Movement towards both gram certain What's more gram negative microscopic organisms. Mixes 1d Also 1f uncovered useful antifungal action. All the secluded compounds were scrutinized for their antibacterial and antifungal activities and most of the compounds manifested remarkable anti bacterial and anti fungal activity.

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 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>

Synthesis of New Series of Phenyldiazene Based Metal Complexes for Designing Most Active Antibacterial and Antifungal Agents

2021 ◽  
Vol 43 (5) ◽  
pp. 578-578
Author(s):  
Khalil Ahmad Khalil Ahmad ◽  
Habib ur Rehman Shah Habib ur Rehman Shah ◽  
Areeba Ashfaq Areeba Ashfaq ◽  
Muhammad Ashfaq Muhammad Ashfaq ◽  
Muhammad Kashif Muhammad Kashif ◽  
...  
Keyword(s):  
Transition Metal ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Antifungal Agents ◽  
Standard Drug ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Excellent Activity ◽  
Antibacterial And Antifungal

In this study, In Vitro antibacterial and antifungal activities of azo series based on transition metal complexes (Cu2+, Zn2+, Mn2+, Co2+ and Ni2+) with already our reported ligands named as; [(E)-1-(1, 3-dioxolan-2-yl)-2-phenyldiazene] (K-1), [(E)-1-(1, 3-dioxolan-2-yl)-2-(4-methylphenyl)diazene] (K-2), 2-[(E)-phenyl diazenyl]-1H-benzimidazole] (K-3), [(E)-1-(1, 3-dioxolan-2-yl)-2-(4-ethylphenyl)diazene] (K-4), and [(E)-1-(1, 3-dioxolan-2-yl)-2-(2-methylphenyl)-diazene] (K-5) were studied. FTIR 1H-NMR and mass spectrometric techniques were applied for interpretation of synthesized complexes. 4.05-4.07 ppm chemical shift appearance of azo group confirms azo coupling with transition metal complexes. N=N, C-H, C-N and C-O groups are also confirmed by FTIR which exhibited peaks at 1400-1500, 2090-3090, 1100-1180, 1010-1060 and 625-780 cm-1. Furthermore, mass spectroscopic data also gives strong indication for the synthesis of metal complexes. All the newly synthesized complexes were screened for their antibacterial and antifungal activities. Antibacterial and antifungal activity against S. aureus, E.coli and A.niger, A.ustus and C.albican at conc. 250 and#181;g/ml showed excellent activity by K-1 complexes (Co2+, Cu2+, Ni2+), K-5 complexes (Zn2+, Mn2+, Cu2+), K-2 complexes (Co2+, Cu2+, Mn2+) and K-3 (Zn2+, Mn2+, Co2+, Cu2+) as compared to standard drug (Ampicillin). Hence, based on this study, it was concluded that these azo based complexes may act as a platform for designing more active antibacterial and antifungal agents.

In vitro Antibacterial and Antifungal Activities of Ethanolic Extract of Aloe vera Leaf Gel

2006 ◽  
Vol 1 (4) ◽  
pp. 348-355 ◽  
Author(s):  
S. Subramania ◽  
D. Sathish Kumar . ◽  
P. Arulselvan . ◽  
G.P. Senthilkumar .
Keyword(s):  
Aloe Vera ◽  
Ethanolic Extract ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal
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