scholarly journals SYNTHESIS AND BIOLOGICAL EVALUATION OF NICOTINIC ACID PEPTIDE DERIVATIVES

2019 ◽  
Vol 8 (4) ◽  
Author(s):  
Nisha Dhir ◽  
Gagan Preet Kaur
Keyword(s):  
Antimicrobial Activity ◽  
Nicotinic Acid ◽  
Biological Activities ◽  
Methyl Esters ◽  
Biological Evaluation ◽  
E Coli ◽  
Peptide Derivatives ◽  
Rf Values ◽  
Antibacterial And Antifungal ◽  
Synthesis And Biological Evaluation

The present study deals with the synthesis of nicotinic acid peptide derivatives and comparative evaluation of biological activities, such as antibacterial and antifungal. Among hetrocyclic aromatic compounds, pyridine nucleus is found in many bioactive products and incorporation of amino acids and peptides into the hetrocyclic aromatic congeners have resulted in compounds with potent activities. All the compounds were synthesized by coupling of nicotinic acids with amino acid methyl esters/dipeptides/tripeptides/tetrapeptides in presence of DCC as coupling agent and NMM as base under continuous stirring for 36 hrs. All synthesized peptide derivatives were identified on the basis of melting point range, Rf values, solubility studies, IR and 1H NMR spectral data. The antimicrobial activity of synthesized compounds was determined against bacterial strainsviz. E. Coli and S. Aureus and fungal strains viz. C. albicans and A. Niger using ciprofloxacin and fluconazole as standard respectively. All the synthesized compounds showed good to moderate antimicrobial activity at 40, 80 and 160 μg/ml. The comparative studies showed the following order of activity profile: nicotinic acid <nicotinic acid methylesters>dipeptide >tripeptide>tetrapeptide. Keywords: Nicotinic acid, Peptides, Antimicrobial activity.

scholarly journals Synthesis, spectral studies and biological activity of 2, 3-disubstituted imidazo [2, 1-b] benzothiazole derivatives

2018 ◽  
Vol 6 (01) ◽  
pp. 01-08
Author(s):  
Yashveer Singh ◽  
Baljeet Kaur ◽  
Amandeep Kaur ◽  
Vivek Kumar Gupta ◽  
Monika Gupta
Keyword(s):  
Antimicrobial Activity ◽  
Catalytic Domain ◽  
Biological Evaluation ◽  
Spectral Studies ◽  
Thiazole Ring ◽  
Standard Drug ◽  
Atp Binding Site ◽  
Benzothiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
Synthesis And Biological Evaluation

Benzothiazole is a heterocyclic compound formed by the fusion of benzene and thiazole ring. The moiety had been reported to act via competing with ATP binding site at the catalytic domain of tyrosine kinase. The present work involves the synthesis and biological evaluation of 4, 5 disubstituted imidazo [2, 1-b] benzothiazole derivatives. The antimicrobial activity of the synthesized derivatives was carried out against Gram + ve bacteria Staphylococcus aureus (MTCC 3160) and Gram –ve bacteria Bordetella bronchiseptica (MTCC 6838), Pseudomonas aeruginosa (T11) and fungal strains Candida albicans (MTCC 1637). Ciprofloxacin and Fluconazole were used as standard drug for antibacterial and antifungal activity respectively. The compounds 6a1, 6a2, 6a3, 6b1 and 8a1 exhibited good antimicrobial activity against all the strains. The derivative 8a1 was further screened for anticancer activity against MCF-7 cell line using Doxorubicin as standard. The structures of the synthesized compounds were established by IR and NMR spectral studies.

scholarly journals Synthesis and Biological Evaluation of 2-(3-Methyl-2-oxoquinoxalin-1(2H)-yl)-N'-(substituted phenyl-methyledene/ethylidene)acetohydrazides

2010 ◽  
Vol 7 (4) ◽  
pp. 1435-1439 ◽  
Author(s):  
Gopal Krishna Rao ◽  
R. B. Kotnal ◽  
P. N. Sanjay Pai
Keyword(s):  
Antimicrobial Activity ◽  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Aromatic Aldehydes ◽  
Biological Evaluation ◽  
Spectral Studies ◽  
Antibacterial And Antifungal Activities ◽  
Quinoxaline Derivatives ◽  
Antibacterial And Antifungal ◽  
Synthesis And Biological Evaluation

A series of quinoxaline derivatives was prepared and evaluated for antitubercular, antibacterial and antifungal activities. The title compounds were prepared by condensation of substituted aromatic aldehydes and substituted acetophenones with 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl) acetohydrazide. Structures of all these compounds were confirmed by their spectral studies. Among synthesized compounds (4r, 4t, 4u, 4wand4x) have shown good anti tubercular activity (25 µg mL-1) when compared to reference drugs pyrazinamide (10 µg mL-1) and streptomycin (7.5 µg mL-1). In this study, few derivatives showed broad spectrum of antimicrobial activity at low concentration. The MICs (Minimum inhibitory concentration) of some compounds are 2-4 µg mL-1.

scholarly journals Synthesis and Biological Evaluation of 4-(3-Hydroxy-benzofuran-2-yl)coumarins

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Puttaraju Boregowda ◽  
Shivashankar Kalegowda ◽  
Vijaykumar Pandurang Rasal ◽  
Jagadeeshreddy Eluru ◽  
Ebenezer Koyye
Keyword(s):  
Staphylococcus Aureus ◽  
Antimicrobial Activity ◽  
Microwave Irradiation ◽  
Methyl Salicylate ◽  
Methyl Esters ◽  
Biological Evaluation ◽  
Cell Cytotoxicity ◽  
Acid Methyl ◽  
Synthesis And Biological Evaluation

Various 4-bromomethylcoumarins (1a-k) were reacted with methyl salicylate to yield 2-(2-oxo-2H-chromen-4-ylmethoxy)-benzoic acid methyl esters (2a-k). Formations of (3a-k) were achieved by using DBU under microwave irradiation. Structures of all the compounds were established on the basis of their spectral data. All the compounds were tested in vitro for their antimicrobial activity and cell cytotoxicity. All the tested compounds (2b-k) and (3a-k) were shown to be better activity against Staphylococcus aureus than the standard Ciprofloxacin. The compound (3k) (R = 6-OMe) was found to be more potent cytotoxic than the standard 5-fluorouracil.

Synthesis and Biological Evaluation of Chalconyl Incorporated Schiff’s Bases of Sulphonamides

2017 ◽  
Vol 8 (03) ◽  
Author(s):  
Neeraj Kumar ◽  
Dhruti Bhatt ◽  
Chandra Shekhar Sharma ◽  
Hamendra Pratap Singh ◽  
Harshda Pandiya ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Biological Evaluation ◽  
Antibacterial And Antifungal Activity ◽  
Schiff’S Bases ◽  
E Coli ◽  
Schiff's Bases ◽  
Microbial Strains ◽  
Antibacterial And Antifungal ◽  
Synthesis And Biological Evaluation

A series of of Chalconyl Incorporated Schiff’s Bases of Sulphonamides was synthesized by reacting substituted chalcone derivatives with Sulphacetamide sodium in methanol. All the title compounds synthesized (2a-2d) were tested for antibacterial and antifungal activity using E. coli, P. aeruginosa, S. aureus, S. pyogenus and C. albicans, A. niger and A. clavatus respectively as microbial strains and Sulphacetamide sodium as standard. The compound 2d showed significant antibacterial activity and 2a showed moderate antifungal activity as compared with Sulphacetamide Sodium.

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 6,7-dimethoxy-5-oxo-2,3,5,9b-tetrahydrothiazolo[2,3-a]isoindole- 3-1,1-dioxide Derivatives with Antimicrobial Activity and Docking Assisted Prediction of the Mechanism of their Antibacterial and Antifungal Properties

2020 ◽  
Vol 20 (29) ◽  
pp. 2681-2691
Author(s):  
Athina Geronikaki ◽  
Victor Kartsev ◽  
Phaedra Eleftheriou ◽  
Anthi Petrou ◽  
Jasmina Glamočlija ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Drug Targets ◽  
Bacterial Species ◽  
Pharmaceutical Research ◽  
Docking Studies ◽  
Fungal Species ◽  
Docking Analysis ◽  
E Coli ◽  
Antibacterial And Antifungal

Background: Although a great number of the targets of antimicrobial therapy have been achieved, it remains among the first fields of pharmaceutical research, mainly because of the development of resistant strains. Docking analysis may be an important tool in the research for the development of more effective agents against specific drug targets or multi-target agents 1-3. Methods: In the present study, based on docking analysis, ten tetrahydrothiazolo[2,3-a]isoindole derivatives were chosen for the evaluation of the antimicrobial activity. Results: All compounds showed antibacterial activity against eight Gram-positive and Gram-negative bacterial species being, in some cases, more potent than ampicillin and streptomycin against all species. The most sensitive bacteria appeared to be S. aureus and En. Cloacae, while M. flavus, E. coli and P. aeruginosa were the most resistant ones. The compounds were also tested for their antifungal activity against eight fungal species. All compounds exhibited good antifungal activity better than reference drugs bifonazole (1.4 – 41 folds) and ketoconazole (1.1 – 406 folds) against all fungal species. In order to elucidate the mechanism of action, docking studies on different antimicrobial targets were performed. Conclusion: According to docking analysis, the antifungal activity can be explained by the inhibition of the CYP51 enzyme for most compounds with a better correlation of the results obtained for the P.v.c. strain (linear regression between estimated binding Energy and log(1/MIC) with R 2 =0.867 and p=0.000091 or R 2 = 0.924, p= 0.000036, when compound 3 is excluded.

scholarly journals Xylochemical Synthesis and Biological Evaluation of Shancigusin C and Bletistrin G

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3224
Author(s):  
Leander Geske ◽  
Ulrich Kauhl ◽  
Mohamed E. M. Saeed ◽  
Anja Schüffler ◽  
Eckhard Thines ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Aromatic Substitution ◽  
Substitution Reactions ◽  
Total Syntheses ◽  
Wittig Olefination ◽  
Starting Point ◽  
Perkin Reaction ◽  
Synthesis And Biological Evaluation

The biological activities of shancigusin C (1) and bletistrin G (2), natural products isolated from orchids, are reported along with their first total syntheses. The total synthesis of shancigusin C (1) was conducted by employing the Perkin reaction to forge the central stilbene core, whereas the synthesis of bletistrin G (2) was achieved by the Wittig olefination followed by several regioselective aromatic substitution reactions. Both syntheses were completed by applying only renewable starting materials according to the principles of xylochemistry. The cytotoxic properties of shancigusin C (1) and bletistrin G (2) against tumor cells suggest suitability as a starting point for further structural variation.

scholarly journals Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva
Keyword(s):  
Antimicrobial Activity ◽  
Diclofenac Sodium ◽  
Biological Evaluation ◽  
Ring System ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Pyrimidine Moiety ◽  
Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

scholarly journals Betalains in Edible Fruits of Three Cactaceae Taxa—Epiphyllum, Hylocereus, and Opuntia—Their LC-MS/MS and FTIR Identification and Biological Activities Evaluation

Plants ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 2669
Author(s):  
Michaela Barkociová ◽  
Jaroslav Tóth ◽  
Katarzyna Sutor ◽  
Natalia Drobnicka ◽  
Slawomir Wybraniec ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antioxidant Activity ◽  
Food Industry ◽  
Biological Activities ◽  
Ornamental Plants ◽  
Reducing Power ◽  
Activity Assay ◽  
Natural Pigment ◽  
E Coli ◽  
Ft Ir

Epiphyllum, Hylocereus, and Opuntia plants belong to the Cactaceae family. They are mostly known as ornamental plants but also for their edible fruits, which can potentially be sources of betalains, such as betanin, a natural pigment used in the food industry, e.g., under the European label code E 162. The aim of this work was the identification of betalains (using LC-MS/MS), evaluation of total betalain content (spectrophotometrically), analysis of functional groups (using FT-IR), evaluation of antioxidant activity (using DPPH, ABTS, FRAP, DCFH-DA, and reducing power methods) and evaluation of antimicrobial activity (S. aureus, E. coli, and C. albicans) in fruits of Epiphyllum, Hylocereus, and Opuntia taxa. A total of 20 betalains were identified in the studied Cactaceae fruits. The Epiphyllum pink hybrid had the highest values of total betalains amongst all samples. The highest antioxidant activity was observed in the Epiphyllum pink hybrid, in Opuntia zacuapanensis and O. humifusa fruits. The antimicrobial activity assay showed that cacti fruits were not able to effectively inhibit the growth of E. coli, S. aureus, or C. albicans. Our results prove that these fruits are good sources of natural pigments—betalains. They do not contain toxic compounds in significant amounts and they exhibit antioxidant activity.

scholarly journals Design, Synthesis and Biological Evaluation of Novel 1, 3, 4-Oxadiazole Bearing Pyridine Moiety

2019 ◽  
pp. 300-307
Author(s):  
Asma D. Ambekari ◽  
Shrinivas K. Mohite
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectra ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Pyridine Moiety ◽  
Anti Inflammatory ◽  
Physicochemical Data ◽  
Synthesis And Biological Evaluation

Series of novel substituted Synthesis of N-{[5-(substituted)-1,3,4-oxadiazole-2-yl] carbamothioyl} derivatives containing 1,3,4-oxadiazole moiety were synthesized by microwave as a green chemistry method and conventional method by using pyridine 3- carboxylic acid as a starting material. The structures of the synthesized compounds were characterized by physicochemical data, IR, Mass spectra and 1HNMR. All the newly synthesized compound screened for their antimicrobial and In-vivo and In-vitro Anti-inflammatory studies. Anti-inflammatory studies revealed that compound 4f showed significant in-vivo and in-vitro anti-inflammatory activity as well potent antimicrobial activity.

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