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 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 Synthesis, Spectral Studies and Antimicrobial Activity of imidazo[2,1-b][1,3,4]thiadiazole derivatives

2017 ◽  
Vol 5 (04) ◽  
pp. 34-38
Author(s):  
Monika Gupta ◽  
Baljeet Kaur ◽  
Shailender Pratap Singh ◽  
Vivek Kumar Gupta
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Spectral Studies ◽  
Standard Drug ◽  
Mass Spectral ◽  
Good Antibacterial Activity ◽  
Thiadiazole Ring ◽  
Thiadiazole Derivatives ◽  
Antibacterial And Antifungal

Thiadiazole is a heterocyclic compound containg both two nitrogen atom and one sulfur atom as a part of the aromatic five-membered ring. The imidazo [2,1-b]-1,3,4-thiadiazole ring system is the core skeleton of well known immunomodulator levamisole. The synthesis and antimicrobial activity of nine 6-Phenyl-2- substituted imidazo [2,1-b]-1,3,4-thiadiazole derivatives were reported against Gram +ve bacteria Bacillius subtilis (MTCC 121), Staphyloccus aureus (MTCC 87), Gram –ve bacteria Pseudomonas aeruginosa (MTCC 424), Escherichia coli (MTCC 40), and fungal strains Candida albicans (MTCC 183), Fusarium solani (MTCC 2935), Fusarium oxyporium (MTCC 2840). Ciprofloxacin and Fluconazole were used as standard drug for antibacterial and antifungal activity respectively. The synthesized compound (6) and (5b) had moderate antibacterial activity especially with Gram negative Escherichia coli (MTCC 40) where (5a) and (5f) had good antibacterial activity. The structures of the synthesized compounds were established by IR, NMR and Mass spectral studies.

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.

ChemInform Abstract: Synthesis and Biological Evaluation of 2-Mercapto-1,3-benzothiazole Derivatives with Potential Antimicrobial Activity.

ChemInform ◽  
2010 ◽  
Vol 41 (6) ◽  
Author(s):  
Carlo Franchini ◽  
Marilena Muraglia ◽  
Filomena Corbo ◽  
Marco Antonio Florio ◽  
Antonia Di Mola ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Biological Evaluation ◽  
Benzothiazole Derivatives ◽  
Synthesis And Biological Evaluation ◽  
Potential Antimicrobial Activity

Synthesis and Biological Evaluation of 2-Mercapto-1,3-benzothiazole Derivatives with Potential Antimicrobial Activity

2009 ◽  
Vol 342 (10) ◽  
pp. 605-613 ◽  
Author(s):  
Carlo Franchini ◽  
Marilena Muraglia ◽  
Filomena Corbo ◽  
Marco Antonio Florio ◽  
Antonia Di Mola ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Biological Evaluation ◽  
Benzothiazole Derivatives ◽  
Synthesis And Biological Evaluation ◽  
Potential Antimicrobial Activity

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.

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.

Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents

2005 ◽  
Vol 15 (14) ◽  
pp. 3328-3332 ◽  
Author(s):  
Masao Yoshida ◽  
Ichiro Hayakawa ◽  
Noriyuki Hayashi ◽  
Toshinori Agatsuma ◽  
Youko Oda ◽  
...  
Keyword(s):  
Antitumor Agents ◽  
Biological Evaluation ◽  
Benzothiazole Derivatives ◽  
Synthesis And Biological Evaluation
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