ChemInform Abstract: Studies on Arylfuran Derivatives. Part 11. Synthesis, Characterization and Biological Studies on Some Mannich Bases Carrying 2,4‐Dichlorophenylfurfural Moiety.

Holla, B. Shivarama; Rao, B. Sooryanarayana; Shridhara, K.; Akberali, P. M.

doi:10.1002/chin.200046157

Cited by 9 publications

(9 citation statements)

References 1 publication

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“…Antibacterial, antifungal, antitubercular, antitumor and anticancer activities of some Schiff bases have been reported, and they are active against a wide range of organisms [19]. Some Schiff bases bearing aryl groups or heterocyclic residues possessing excellent biological activities have attracted the attention of many researchers in recent years [20]. The Schiff bases formed from aromatic aldehydes, ketones and their derivatives are quite stable.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Antimicrobial, Antitubercular and Cheminformatic Studies of 2-(1-Benzofuran-2-Yl)-N'-[(3z)-2-Oxo-1, 2-Dihydro-3h-Indol-3-Ylidene] Quinoline-4-Carbohydrazide and Its Derivatives

Santoshkumar

Satyanarayana

Anantacharya

et al. 2017

Int J Pharm Pharm Sci

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Objective: Synthesis of novel 2-(1-benzofuran-2-yl)-N'-[(3Z)-2-oxo-1, 2-dihydro-3H-indol-3-ylidene] quinoline-4-carbohydrazide and its derivatives for antimicrobial and antitubercular activity.Methods: Synthesis was carried out using the general method and the structures were confirmed by IR, 1 Results:The results revealed that at 25 mg/ml concentration, compounds 3a and 5a showed good antibacterial activity at 3.5±0.1, 3.8±0.3, 3.6±0.2 respectively against E. coli, K. pneumonia and S. typhimurium, when compared with drug streptomycin with similar concentration. The percentage of inhibition found at 50 µg/ml concentration, compounds 2b and 6a exhibited good antifungal activity at 53±1.15, 57±1.52 against A. flavus and C. neoformans, compared with standard drug fluconazole. The increase in activity was found to be dose dependent. The analogue 2a showed good antitubercular activity at 12.5±0.5 µg/ml, compounds 2b, 3a, 4a-b, 5a-b and 6a-b exhibited significant activity at 25±0.57 µg/ml and compound 3b showed moderate activity at 50±0.57 µg/ml. The mean value of P<0.05 were considered to be statistically significant. The absorption, distribution, metabolism, excretion and toxicity studies of the entitled molecules were analyzed and found to be in acceptable range.H-NMR, [13]C-NMR and mass spectral analysis. The antibacterial activity was carried by agar well diffusion method, antifungal activity was performed by poison food technique and antitubercular activity was carried out by Microplate Alamar Blue Assay (MABA) method with the help of H37Rv. In silico absorption, distribution, metabolism, excretion, toxicity (ADMET) study of the drug, likeliness was carried out in ACD/lab-2. Conclusion:The study reveals that compounds containing benzofuran coupled nitrogen heterocycles are essential for activity as they possess excellent drug-like characteristics, suggesting to be potentially best inhibitor of H37Rv strain. The in silico ADME analysis also revealed that all the compounds were in acceptable range to obey the pharmacokinetic parameters.

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Section: Introductionmentioning

confidence: 99%

Synthesis, Antimicrobial, Antitubercular and Cheminformatic Studies of 2-(1-Benzofuran-2-Yl)-N'-[(3z)-2-Oxo-1, 2-Dihydro-3h-Indol-3-Ylidene] Quinoline-4-Carbohydrazide and Its Derivatives

Santoshkumar

Satyanarayana

Anantacharya

et al. 2017

Int J Pharm Pharm Sci

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“…Antibacterial, antifungal, antitumor, and anticancer activities of some Schiff bases have been reported, and they are active against a wide range of organisms (Sari et al, 2003). Some Schiff bases bearing aryl groups or heterocyclic residues possessing excellent biological activities have attracted the attention of many researchers in recent years (Holla et al, 2000). The Schiff bases formed from aromatic aldehydes, ketones, and their derivatives are quite stable.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and biological activities of Schiff bases of gabapentin with different aldehydes and ketones: a structure–activity relationship study

2010

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A series of novel gabapentin derivatives 6a-k and 7a-f were synthesized, and their biological activities were determined. The chemical structures were confirmed by elemental analyses, UV-visible, FT-IR, and 1 H NMR spectral studies. The structure-activity relationships (SAR) for anticonvulsant and antioxidant activities were discussed.Compounds 7a-f were evaluated for their possible anticonvulsant activity by Maximal Electroshock Seizure (MES) test, and their neurotoxic effects were determined by rotorod test. Majority of the compounds were active in MES tests. Compounds 7b and 7e showed good protective effect from seizure when compared to standard drug, phenytoin (100 mg/kg). The same compounds showed no neurotoxicity at the maximum dose administered (100 mg/kg). Most of the novel compounds showed DPPH radical scavenging activity, where compounds 6f, 6j, and 7a were the best radical scavengers (IC 50 was about 60 lg/ml).

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“…It is well established that the activity of such nitroheterocycles is mainly due to the metabolic reduction of their nitro functionality by nitroreductase enzyme [24]. Moreover, a number of other furan derivatives have also exhibited antibacterial activity [25,26]. Therefore, in view of these findings, we have designed some new bisindoles by employing a new methodology.…”

Section: Introductionmentioning

confidence: 99%

An efficient synthesis of bis(indolyl)methanes and evaluation of their antimicrobial activities

Kamal

Khan

Reddy

et al. 2009

Journal of Enzyme Inhibition and Medicinal Chemistry

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ChemInform Abstract: Studies on Arylfuran Derivatives. Part 11. Synthesis, Characterization and Biological Studies on Some Mannich Bases Carrying 2,4‐Dichlorophenylfurfural Moiety.

Cited by 9 publications

References 1 publication

Synthesis, Antimicrobial, Antitubercular and Cheminformatic Studies of 2-(1-Benzofuran-2-Yl)-N'-[(3z)-2-Oxo-1, 2-Dihydro-3h-Indol-3-Ylidene] Quinoline-4-Carbohydrazide and Its Derivatives

Synthesis, Antimicrobial, Antitubercular and Cheminformatic Studies of 2-(1-Benzofuran-2-Yl)-N'-[(3z)-2-Oxo-1, 2-Dihydro-3h-Indol-3-Ylidene] Quinoline-4-Carbohydrazide and Its Derivatives

Synthesis and biological activities of Schiff bases of gabapentin with different aldehydes and ketones: a structure–activity relationship study

An efficient synthesis of bis(indolyl)methanes and evaluation of their antimicrobial activities

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