scholarly journals Synthesis and Antimicrobial Studies of New [Tetrakis (1, 2, 4-Triazole / 1, 3, 4-Oxadiazole / 1, 3, 4-Thiadiazole] [Bis-(Benzene-1, 3, 5-Triyl)] Dioxymethylene Compounds

2020 ◽  
pp. 234-245
Author(s):  
Ahmed Neamah Ayyash
Keyword(s):  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Chemical Structure ◽  
Acid Hydrazide ◽  
Basic Medium ◽  
Tosyl Chloride ◽  
Antimicrobial Studies ◽  
Ft Ir ◽  
Concentrated Sulfuric Acid ◽  
Derivatives Of

     Synthesis of new heterocyclic compounds containing four five-membered rings together was the main goal of this work. The new derivatives of [tetrakis (1,2,4-triazole /1,3,4-thiadiazole /1,3,4-oxadiazole][bis-(benzene-1,3,5-triyl)] dioxymethylene A7-A18 were synthesized by the reaction of [bis-(dimethyl 5-yl-isophthalate)] dioxymethylene compound A1 which was previously prepared from the reaction of 1,2-dibromomethan and dimethyl 5-hydroxyisophthalate, then treated with hydrazine hydrate to yield the corresponding acid hydrazide A2. In the next step, compound A2 was refluxed with 4-substituted isothiocyanate to give substituted thiosemicarbazides A3-A6. The treatment of the latter compounds in basic medium of 2M of NaOH afforded 1,2,4-Triazole derivatives A7-A10. Whereas the reaction of the same compounds with concentrated sulfuric acid gave 1,3,4-thiadiazoles  A11-A14. Furthermore, the new derivatives of 1,3,4-oxadiazole A15-A18 were obtained by the reaction of thiosemicarbazides and tosyl chloride in presence of pyridine. (C. H. N.) elemental analysis, FT-IR, and 1HNMR techniques were used to characterize the chemical structure of some of the new synthesized compounds which also exhibited an important biological activity.

Synthesis and Biological Potentials of Quinoline Analogues: A Review of Literature

2019 ◽  
Vol 16 (7) ◽  
pp. 653-688 ◽  
Author(s):  
Leena Kumari ◽  
Salahuddin ◽  
Avijit Mazumder ◽  
Daman Pandey ◽  
Mohammad Shahar Yar ◽  
...  
Keyword(s):  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Building Blocks ◽  
Vital Role ◽  
Review Of Literature ◽  
Drug Discovery Process ◽  
Active Compounds ◽  
Lead Compounds ◽  
Synthetic Approaches ◽  
Derivatives Of

Heterocyclic compounds are well known for their different biological activity. The heterocyclic analogs are the building blocks for synthesis of the pharmaceutical active compounds in the organic chemistry. These derivatives show various type of biological activity like anticancer, antiinflammatory, anti-microbial, anti-convulsant, anti-malarial, anti-hypertensive, etc. From the last decade research showed that the quinoline analogs plays a vital role in the development of newer medicinal active compounds for treating various type of disease. Quinoline reported for their antiviral, anticancer, anti-microbial and anti-inflammatory activity. This review will summarize the various synthetic approaches for synthesis of quinoline derivatives and to check their biological activity. Derivatives of quinoline moiety plays very important role in the development of various types of newer drugs and it can be used as lead compounds for future investigation in the field of drug discovery process.

ChemInform Abstract: SYNTHESIS AND BIOLOGICAL ACTIVITY OF DERIVATIVES OF 2-ARYLAMINONICOTINIC ACID HYDRAZIDE

1981 ◽  
Vol 12 (25) ◽  
Author(s):  
A. I. MIKHALEV ◽  
L. B. FALALEEVA ◽  
N. I. SHRAMM ◽  
L. M. POLUKHINA ◽  
V. S. ZALESOV ◽  
...  
Keyword(s):  
Biological Activity ◽  
Acid Hydrazide ◽  
Derivatives Of

Chemical structure and biological activity ofo-disubstituted derivatives of benzene

1967 ◽  
Vol 23 (12) ◽  
pp. 1038-1038 ◽  
Author(s):  
K. Boček ◽  
J. Kopecký ◽  
M. Krivucová
Keyword(s):  
Biological Activity ◽  
Chemical Structure ◽  
Derivatives Of

scholarly journals Synthesis, Characterization and In-Silico Analysis of New 2-Pyrazolines

2021 ◽  
Vol 13 (1) ◽  
pp. 183-194
Author(s):  
T. Saroja ◽  
R. M. Ezhilarasi ◽  
V. Selvamani ◽  
S. Mahalakshmi
Keyword(s):  
Acetic Acid ◽  
13C Nmr ◽  
Heterocyclic Compounds ◽  
Mass Spectra ◽  
Acid Hydrazide ◽  
In Silico Analysis ◽  
Pharmacological Activities ◽  
Cyclocondensation Reaction ◽  
Ft Ir ◽  
Silico Analysis

Heterocyclic compounds such as pyrazolines, pyrimidines, oxazole and isoxazole exhibit different pharmacological activities. The current study involves synthesis of new 2-pyrazolines. The synthesis involves the cyclocondensation reaction of substituted chalcones with (4-fluorophenylthio)acetic acid hydrazide (FTAH) under reflux. The chalcones (C1-C7 / 1a-1g) were synthesized from the reaction of substituted acetophenone with substituted benzaldehyde and FTAH was prepared from 4-fluro thiophenol. New 2-pyrazolines were obtained in good yields (60-70 %). All the compounds were characterized by FT-IR, 1H, 13C NMR and mass spectra. PASS analysis was carried out for the 2-pyrazolines synthesized (P1-P7 / 3a-3g).

scholarly journals SYNTHESIS CHARACTERIZATION AND ANTIMICROBIAL ACTIVITIES STUDIES OF N-{2-(4-CHLOROPHENYL) ACETYL} AMINO ALCOHOLS DERIVED FROM α-AMINO ACIDS

2020 ◽  
pp. 11-16
Author(s):  
G. Venkateshappa ◽  
G. Shivaraju ◽  
P. Raghavendra Kumar
Keyword(s):  
Amino Acids ◽  
Amino Alcohols ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
Moderate Activity ◽  
E Coli ◽  
Synthetic Drugs ◽  
Antimicrobial Studies ◽  
Ft Ir ◽  
Derivatives Of

Amino acids play important roles in organisms to sustain in living state and perform as body constituents, enzymes and antibodies. At insalubrious situations, use of amino acids derivatives as drugs in the maintenance of normal health is better choice than common unnatural synthetic drugs. This is due to the fact that the amino acids derivatives may be more bio-compatible, biodegradable and eliminate easily than others.  In this sense we have made an effort and report herein the synthesis of N-{2-(4-chlorophenyl) acetyl} amino alcohols synthesised by reduction of N-{2-(4-chlorophenyl)acetyl} derivatives of (S)-amino acids such as (S)-phenylalanine, (S)-alanine, (S)-methionine, (S)-leucine, (S)-tryptophan and (S)-proline. These newly synthesized amino acids derivatives were analysed by proton, carbon-13 NMR and FT-IR spectroscopy. The composition of solid derivatives was determined by elemental analysis. Further, antimicrobial activities of these derivatives were assessed on usual bacteria K. aerogenes, E. coli, S. aureus and P. desmolyticum and fungi A. flavus and C. albicans. The compounds were witnessed moderate activity than authorised antibacterial and fungal agents Ciprofloxacin and Fluconazole respectively. The antimicrobial studies also revealed that, these derivatives could be better antifungal agents than antibacterial agents. Finally we compared the experimental results of antimicrobial activities with docking studies.  

scholarly journals Analysis of the relationship between the predicted biological activity and the chemical structure of S-derivatives of 5-(5-bromofuran-2-yl)-4R-1,2,4-triazole-3-thiols

2021 ◽  
Vol 14 (2) ◽  
pp. 167-172
Author(s):  
O. A. Bigdan
Keyword(s):  
Biological Activity ◽  
Chemical Structure ◽  
Plant Protection ◽  
Hypoxia Inducible Factor ◽  
Polymeric Materials ◽  
Plant Protection Products ◽  
New Drugs ◽  
Antihypoxic Activity ◽  
Oxidation Reactions ◽  
Derivatives Of

1,2,4-Triazole derivatives are actively used as components in the development of new drugs, plant protection products, polymeric materials, anti-corrosion agents and etc. Chemical modeling of substituted 1,2,4-triazoles due to the introduction of different pharmacophores into the structure is very popular among scientists in various fields. Today it is known that some S-derivatives of 5-(5-bromofuran-2-yl)-4R-1,2,4-triazole-3-thiols have antimicrobial activity. The aim of the work is to analyze the relationships between the predicted biological activity and the chemical structure of S-derivatives of 5-(5-bromofuran-2-yl) -4R-1,2,4-triazole-3-thiols. Materials and methods. Virtual screening of compounds was performed using the computer program PASS (Prediction of activity spectra for substances). The results of the forecast were issued in the form of a list of names of probable types of activity with estimates of the probabilities of presence (Pa) and absence of each activity (Pi), which had values from 0 to 1. Results. Analyzing the prediction of biological activity on protein targets from the group of enzymes, we can said that derivatives of 5-(5-bromofuran-2-yl)-4R-1,2,4-triazole-3-thiols were active in the group of oxyreductases (Glutathione reductase, mitochondrial; Cyclooxygenase-2; Hypoxia-inducible factor prolyl hydroxylase 2), which catalyzed oxidation reactions, the transfer of electrons from one molecule (reducer, electron donor) to another (oxidant, electron acceptor). These compounds can demonstrate antioxidant, antihypoxic activity. Conclusions. The conducted forecast of biological activity revealed that derivatives of 5-(5-bromofuran-2-yl)-4R-1,2,4-triazole-3-thiols are the most active and there is a probability to show antitumor, antiviral, antibacterial, diuretic, actoprotective, and antioxidant activity.

Particular Activity of Naphthacene Derivatives as Inducers of Zoxazolamine Hydroxylase Synthesis in Rats

1967 ◽  
Vol 22 (5) ◽  
pp. 532-534 ◽  
Author(s):  
N. P. Buu-Ηοϊ ◽  
Do-Phuoc Hien
Keyword(s):  
Biological Activity ◽  
High Activity ◽  
Chemical Structure ◽  
Structural Analogues ◽  
Derivatives Of

High activity as inducers of microsomal zoxazolamine hydroxylase synthesis in rats has been found to be remarkably frequent in derivatives of the linear tetracyclic hydrocarbon naphthacene and their heterocyclic structural analogues. The relationships between chemical structure and this type of biological activity, which is shown to be independent of carcinogenic properties, are discussed.

Chemical structure and biological activity ofp-disubstituted derivatives of benzene

1964 ◽  
Vol 20 (12) ◽  
pp. 667-668 ◽  
Author(s):  
K. Boček ◽  
J. Kopecký ◽  
M. Krivucová ◽  
D. Vlachová
Keyword(s):  
Biological Activity ◽  
Chemical Structure ◽  
Derivatives Of

scholarly journals Synthesis and Microbiological Activity of Some Newly Synthesized Derivatives of 2-Oxo-2H-chromen-2-one

2011 ◽  
Vol 8 (4) ◽  
pp. 1522-1527 ◽  
Author(s):  
Majlinda Daci-Ajvazi ◽  
Sevdije Govori ◽  
Shuhreta Omeragiq
Keyword(s):  
Staphylococcus Aureus ◽  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Sulfonyl Chloride ◽  
Aeromonas Salmonicida ◽  
Significant Activity ◽  
Microbiological Activity ◽  
Bacillus Spp ◽  
New Compounds ◽  
Derivatives Of

By the action of 2-amino-5-methylthio-1,3,4-thiadiazole, 3-amino-5-methylisoxazole, 2-amino-6-fluorobenzothiazole, 2-amino-5-chloropyridine, respectively, on 4-chloro-2-oxo-2H-chromene-3-sulfonyl chloride, the corresponding 9-methylthio-7,7-dioxo-7,7a-dihydro-5-oxo-7λ6,10-dithia-8,11-diaza-cyclopenta[b] phenantren-6-one, 9-methyl-7,7-dioxo-7H-5,8-dioxa-7λ6-thia-7a,11-diaza-cyclopenta[b] phenantren-6-one, 9-fluoro-7,7-dioxo-7H-5-oxa-7λ6,12-dithia-7a,13-diaza-indeno[1,2-b] phenantren-6-one and 9-Chloro-7,7-dioxo-7H-5-oxa-7λ6-thia-7a,12-diaza-benzo[α]anthracen -6-one were formed and they have been isolated in satisfying yields. Based on the biological activity of chromene-2-ones and heterocyclic compounds condensed in position 3 and 4, we also studied microbiological activity of these new compounds(5-8), againstStaphylococcus aureusATCC 25923,Streptococcus pneumoniae, Aeromonas Salmonicida, Bacillus sppand some of them exhibited significant activity.

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