scholarly journals Synthesis and Biological Evaluation of Novel 5,7-Dichloro-1,3-benzoxazole Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
N. D. Jayanna ◽  
H. M. Vagdevi ◽  
J. C. Dharshan ◽  
T. R. Prashith Kekuda ◽  
B. C. Hanumanthappa ◽  
...  
Keyword(s):  
Enzyme Inhibitors ◽  
Heterocyclic Ring ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
H Nmr ◽  
New Class ◽  
Synthesis And Biological Evaluation ◽  
Active Methylene ◽  
C Nmr

A new class of 5,7-dichloro-1,3-benzoxazole derivatives4–11were synthesized by fusing 5,7-dichloro-2-hydrazino-1,3-benzoxazole3nucleus with aliphatic acids, active methylene compounds, and with selected esters to form heterocyclic ring systems like 1,2,4-triazoles, pyrazoles, and triazine moieties. The compound3on diazotization reaction affords the tetrazole compound. The synthesized compounds were characterized by1H NMR, IR, Mass, and13C NMR spectral data and screened for cytotoxic, antimicrobial, antioxidant, and antilipase activities. The compounds4,5, and8have shown significant antimicrobial activities, whereas compounds6and8have been emerged as leading cytotoxic agents. The compounds9,10, and11were found to be strong enzyme inhibitors.

scholarly journals Synthesis and biological evaluation of new Benzimidazole derivatives

2018 ◽  
Vol 29 (1) ◽  
pp. 107 ◽  
Author(s):  
Hadeel Majed ◽  
Firyal W. Askar
Keyword(s):  
Schiff Bases ◽  
Nmr Spectra ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
H Nmr ◽  
Bacteria And Fungi ◽  
Synthesis And Biological Evaluation

Agroup of benzimidazole derivatives bearing different heterocyclic moieties such as Schiff bases, 2-azetidinone and  4-thiazolidinone were efficiently prepared. The structures of the newly compounds were characterized by FTIRand ¹H NMR spectra. The synthesized compounds were evaluated for their antimicrobial activities against gram-positive and gram negative bacteria and fungi using the microdilution procedure.

scholarly journals Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Long Tang ◽  
Jianchun Jiang ◽  
Guoqiang Song ◽  
Yajing Wang ◽  
Ziheng Zhuang ◽  
...  
Keyword(s):  
Small Molecules ◽  
Inhibitory Activity ◽  
Structural Modification ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
H Nmr ◽  
Lead Compounds ◽  
Activity Test ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

AbstractA series of urolithins derivatives were designed and synthesized, and their structures have been confirmed by 1H NMR, 13C NMR, and HR-MS. The inhibitory activity of these derivatives on phosphodiesterase II (PDE2) was thoroughly studied with 3-hydroxy-8-methyl-6H-benzo[C]chromen-6-one and 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[C] chromen-6-one as the lead compounds. The biological activity test showed that compound 2e had the best inhibitory activity on PDE2 with an IC50 of 33.95 μM. This study provides a foundation for further structural modification and transformation of urolithins to obtain PDE2 inhibitor small molecules with better inhibitory activity.

Design, Synthesis, Molecular Docking and Biological Evaluation of Bromo-Pyridyl Containing 3-Chloro 2-Azetidinone Derivatives as Potential Antimycobacterial Agents

2021 ◽  
Author(s):  
Rakesh V. Kusurkar ◽  
Rahul H. Rayani ◽  
Anand G. Vala ◽  
Deepa R. Parmar ◽  
Manoj N Bhoi ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antitubercular Activity ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Dynamics Simulation ◽  
Design Synthesis ◽  
H Nmr ◽  
New Class ◽  
Lactam Ring ◽  
C Nmr

Abstract A new class of β-lactam pharmacophore series of 2-Bromo-N-[4-(2-{[2-(substituted phenyl)-3-chloro-4-oxoazetidin-1-yl] amino}-2-oxoethyl) phenyl] pyridine-4-carboxamide derivatives were designed, prepared, and screened for their antimycobacterial activities. The hydrazone derivatives were first synthesized via conventional and microwave methods, and then the β-lactam ring could be constructed via a [2+2] ketenimine cycloaddition. The structure of all synthesized compounds was characterized by FTIR, 1H NMR, 13C NMR, and Mass spectroscopy techniques. All the newly synthesized derivatives were found to be effective in inhibiting M. tuberculosis H37RV strain infection at concentrations of 12.5, 25.0, and 50.0 µg/mL using the MABA method. Amongst, the compound (6e) was found to be good potent antitubercular activity at 12.5 mg/mL concentration in comparison with the rest of the compounds using the standard therapeutic agent Streptomycin. Molecular dynamics simulation studies and Molecular docking studies have been performed against mycobacterial InhA enzyme to gain an insight into the possible mechanistic action in search of good potent antitubercular candidates.

scholarly journals Synthesis and Biological Evaluation of Coumarinyl Sydnone Derivatives

2011 ◽  
Vol 8 (1) ◽  
pp. 113-118 ◽  
Author(s):  
Keshav C. Patel ◽  
Himanshu D. Patel
Keyword(s):  
Antimicrobial Activity ◽  
Melting Point ◽  
Thin Layer ◽  
Biological Evaluation ◽  
Physical Methods ◽  
H Nmr ◽  
Antimicrobial Evaluation ◽  
Layer Chromatography ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

A novel series of compounds containing coumarinyl sydnone derivatives from 4-methyl-7-hydroxy-8-nitro coumarin were synthesized. The formed compounds have been evaluated by physical methods (melting point, thin layer chromatography, elemental analysis) and by spectral data (IR,1H-NMR &13C NMR). The antimicrobial evaluation of the compounds showed that some of them revealed promising antimicrobial activity.

scholarly journals Design, Synthesis and Biological Evaluation of N-((2-phenyloxazol-4-yl)methyl) Pyrimidine Carboxamide Derivatives as Potential Fungicidal Agents

2020 ◽  
Vol 26 (1) ◽  
pp. 185-191
Author(s):  
Danling Huang ◽  
Shumin Zheng ◽  
Yong-Xian Cheng
Keyword(s):  
Sclerotinia Sclerotiorum ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
H Nmr ◽  
Structure Activity ◽  
Colletotrichum Fragariae ◽  
New Compounds ◽  
Synthesis And Biological Evaluation ◽  
Commercial Fungicide ◽  
C Nmr

Abstract Twelve N-((2-phenyloxazol-4-yl)methyl) pyrimidine carboxamide derivatives were designed, synthesized, and characterized by 1H NMR, 13C NMR, and HRMS. The fungicidal activities of these new compounds against Sclerotinia sclerotiorum, Botrytis cinereal, and Colletotrichum fragariae were evaluated. The results indicated that compounds 5b, 5f, and 5g displayed potential fungicidal activities against tested fungi, especially 5f exhibited IC50 value of 28.9 mg/L against S. sclerotiorum. Moreover, the compounds 5f and 5g showed IC50 values of 54.8 mg/L and 62.2 mg/L against C. fragariae respectively, which shows that they were more active than the commercial fungicide hymexazol. The superficial structure-activity relationships were discussed, which may be of benefit for the development of fungicides and discovery of novel fungicides.

Synthesis and biological evaluation of a new class of quinazolinoneazoles as potential antimicrobial agents and their interactions with calf thymus DNA and human serum albumin

MedChemComm ◽  
2015 ◽  
Vol 6 (1) ◽  
pp. 222-229 ◽  
Author(s):  
Li-Ping Peng ◽  
Sangaraiah Nagarajan ◽  
Syed Rasheed ◽  
Cheng-He Zhou
Keyword(s):  
Human Serum Albumin ◽  
Serum Albumin ◽  
Human Serum ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Calf Thymus Dna ◽  
New Class ◽  
Calf Thymus ◽  
Synthesis And Biological Evaluation

A series of quinazolinone azoles were synthesized and screened for their antimicrobial activities, and further studies of their binding behaviors with calf thymus DNA and human serum albumin were investigated.

scholarly journals Synthesis and Biological Evaluation of S-Substituted Perhalo-2-nitrobuta-1,3-dienes as Novel Xanthine Oxidase, Tyrosinase, Elastase, and Neuraminidase Inhibitors

2018 ◽  
Vol 2018 ◽  
pp. 1-11 ◽  
Author(s):  
Nihal Onul ◽  
Onur Ertik ◽  
Neşe Mermer ◽  
Refiye Yanardag
Keyword(s):  
Carbon Tetrachloride ◽  
Xanthine Oxidase ◽  
Spectroscopic Data ◽  
Biological Evaluation ◽  
Neuraminidase Inhibitors ◽  
H Nmr ◽  
Allyl Mercaptan ◽  
New Compounds ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

S-substituted perhalo-2-nitrobuta-1,3-dienes 3a, b were synthesized by the reaction of polyhalo-2-nitrobuta-1,3-dienes 1a, b with allyl mercaptan. 1-(2,3-Dibromopropanethio)-4-bromo-1,3,4-trichloro-2-nitrobuta-1,3-diene 4 was obtained from the addition of bromine to S-substituted polyhalo-2-nitrobuta-1,3-diene 3b in carbon tetrachloride. Sulfoxides 5a, b, and 6 were obtained from the reaction of thiosubstituted polyhalonitrobutadienes 3a, b, and 4 with m-CPBA in CHCl3. The structures of the new compounds were determined by spectroscopic data (FTIR, 1H NMR, 13C NMR, MS). These compounds exhibited antixanthine oxidase, antityrosinase, antielastase, and antineuraminidase activities.

scholarly journals Synthesis and Biological Evaluation of Novel Piperazine Containing Hydrazone Derivatives

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Betül Kaya ◽  
Yusuf Özkay ◽  
Halide Edip Temel ◽  
Zafer Asım Kaplancıklı
Keyword(s):  
Aromatic Aldehydes ◽  
Biological Evaluation ◽  
Standard Drug ◽  
H Nmr ◽  
Chemical Structures ◽  
Ft Ir ◽  
Inhibition Potency ◽  
New Compounds ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

Some hydrazone derivatives were synthesized and their potential anticholinesterase activities were examined. A series of eleven new compounds of N′-(2,4-disubstitutedbenzylidene)-2-(4-(4-nitrophenyl)piperazin-1-yl)acetohydrazide derivatives were obtained via reaction of 2-[4-(4-nitrophenyl)piperazin-1-yl]acetohydrazide with aromatic aldehydes. The chemical structures of the compounds were enlightened by FT-IR,1H-NMR,13C-NMR, and HRMS (ESI) spectral data. The inhibition potency of the compounds3a–kagainst AChE and BuChE was measured and evaluated using a modification of Ellman’s spectrophotometric method. Among the tested compounds, compound3cwas assigned to be the most active derivative. Galantamine was used as a standard drug.

scholarly journals Synthesis and Biological Evaluation of 2-aroyl-4-phenyl-5- hydroxybenzofurans as a New Class of Antitubulin Agents

2008 ◽  
Vol 4 (6) ◽  
pp. 558-564 ◽  
Author(s):  
Romeo Romagnoli ◽  
Pier Baraldi ◽  
Taradas Sarkar ◽  
Carlota Cara ◽  
Olga Lopez ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
New Class ◽  
Synthesis And Biological Evaluation

Novel C-9, 9'-O-acyl Esters of (-)-Carinol as Free-radical Scavengers and Xanthine Oxidase Enzyme Inhibitors: Synthesis and Biological Evaluation

2013 ◽  
Vol 9 (1) ◽  
pp. 100-103 ◽  
Author(s):  
Praveen Kumar Suryadevara ◽  
Hari Babu Tatipaka ◽  
Rama Subba Rao Vidadala ◽  
Ashok k Tiwari ◽  
Janaswamy Madhusudana Rao ◽  
...  
Keyword(s):  
Free Radical ◽  
Xanthine Oxidase ◽  
Enzyme Inhibitors ◽  
Biological Evaluation ◽  
Free Radical Scavengers ◽  
Radical Scavengers ◽  
Oxidase Enzyme ◽  
Synthesis And Biological Evaluation
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