scholarly journals Synthesis, Structural Elucidation, and Antibacterial Evaluation of Some New Molecules Derived from Coumarin, 1,3,4-Oxadiazole, and Acetamide

2016 ◽  
Vol 2016 ◽  
pp. 1-10 ◽  
Author(s):  
Shahid Rasool ◽  
Aziz-ur-Rehman ◽  
Muhammad Athar Abbasi ◽  
Sabahat Zahra Siddiqui ◽  
Syed Adnan Ali Shah ◽  
...  
Keyword(s):  
Biological Activities ◽  
Basic Medium ◽  
Bacterial Strains ◽  
Alkyl Aryl ◽  
H Nmr ◽  
Intermolecular Cyclization ◽  
Biological Potential ◽  
Aryl Amines ◽  
Spectral Data Analysis ◽  
New Compounds

Because of the reported biological activities of coumarin, 1,3,4-oxadiazole, and acetamides, some new compounds incorporating these moieties were synthesized and evaluated for their biological potential against Gram-positive and Gram-negative bacteria. In the present work, 4-chlororesorcinol (1) and ethyl acetoacetate (2) were mixed in a strong acidic medium to synthesize 6-chloro-7-hydroxy-4-methyl-2-oxo-2H-chromene (3) which was subjected to the intermolecular cyclization after consecutive three steps to synthesize 5-[(6-chloro-4-methyl-2-oxo-2H-chromen-7-yl)oxy]methyl-1,3,4-oxadiazol-2-thiol (6). A series of acetamoyl electrophiles, 8a–o, were synthesized from aralkyl/alkyl/aryl amines, 7a–o, in an aqueous basic medium. The final compounds, 9a–o, were synthesized by the reaction of compounds 6 and 8a–o in DMF/NaH. The synthesized compounds were structurally elucidated by spectral data analysis of IR, 1H-NMR, and EIMS. The most of the synthesized compounds remained moderate to excellent antibacterial agents. The molecules, 9e, 9j, and 9k, were the most efficient ones against all the five bacterial strains taken into account.

scholarly journals Facile Synthesis of Propranolol and Novel Derivatives

2020 ◽  
Vol 2020 ◽  
pp. 1-10
Author(s):  
Vy Anh Tran ◽  
Nguyen Hai Tai Tran ◽  
Long Giang Bach ◽  
Trinh Duy Nguyen ◽  
Thi Thuong Nguyen ◽  
...  
Keyword(s):  
Water Solubility ◽  
Antihypertensive Drugs ◽  
Biological Activities ◽  
Pyridinium Chlorochromate ◽  
Butyl Bromide ◽  
H Nmr ◽  
Oxidation Reduction ◽  
High Yields ◽  
New Compounds ◽  
Layer Chromatography

Propranolol is one of the first medications of the beta-blocker used for antihypertensive drugs. This study reports the facile route for the synthesis of propranolol and its novel derivatives. Herein, propranolol synthesis proceeded from 1-naphthol and isopropylamine under mild and less toxic conditions. Novel propranolol derivatives were designed by reactions of propranolol with benzoyl chloride, pyridinium chlorochromate, and n-butyl bromide through esterification, oxidation reduction, and alkylation, respectively. The isolation and purity of compounds were conducted using column chromatography and thin-layer chromatography. Mass spectrometry and 1H-NMR spectroscopy were applied to identify new compounds structure. Propranolol derivatives from 2-chlorobenzoyl chloride (compound 3), 2-fluorobenzoyl chloride (compound 5), and especially acetic anhydride (compound 6) manifested high yields and significantly increased water solubility. Six semisynthetic propranolol derivatives promise to improve antioxidative and biological activities.

Chemical composition, biological activities, and toxicity study of Carduncellus pinnatus essential oil from west Algeria

2021 ◽  
Vol 17 ◽  
Author(s):  
Mohammed Semaoui ◽  
Mohammed El Amine Dib ◽  
Nassim Djabou ◽  
Jean Costa ◽  
Alain Muselli
Keyword(s):  
Gas Chromatography ◽  
Chemical Composition ◽  
Essential Oil ◽  
Essential Oils ◽  
Biological Activities ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Bacterial Strains ◽  
Biological Potential ◽  
New Findings

Background: Many species have already been examined regarding their biological activities but there are nevertheless many more which merits examination, among them Carduncellus pinnatus (Desf), that is one of the less abundant and the less frequent aromatic plants of Asteraceae species, it is one species widely distributed in the Mediterranean region. In the present investigation, chemical composition of essential oils of Carduncellus pinnatus and their antioxidant, antimicrobial and antifungal activities were investigated for the first time. Methods: The chemical composition of the essential oils of Carduncellus pinnatus was analyzed by gas chromatography (GC) and gas chromatography mass spectroscopy (GC/MS) during its vegetative cycle. The antioxidant properties were evaluated by DPPH-radical scavenging and FRAP methods. The essential oil was tested on two-gram positive bacteria, three-gram negative bacteria, two filamentous fungi and one yeast. The toxicity of this essential oil was evaluated from several experiments on five mice tested in the laboratory. Results: The chemical composition of essential oils studied by GC and GC-MS showed a total of Twenty-seven compounds constituted mainly by Aplotaxene. Harvest time affected quantitatively but not qualitatively the chemical composition of essential oils. The results showed that Carduncellus pinnatus presented interesting antioxidant property. In order to assess the biological activities of Carduncellus pinnatus, all essential oil samples were combined together to produce a collective essential oil (Coll EO). The Coll EO showed activity on all tested bacterial strains based on the inhibition diameters obtained. The most interesting antimicrobial activity has been observed against Salmonella typhi, Escherichia coli and Staphylococcus aureus with IC50s 0.4, 1.2 and 1.2 g/L, but which remains weak compared to the Gentamicin control, respectively). Regarding antifungal activity, largest inhibition was observed against Fusarium solani (IC50= 0.8 g/L). On the other hand, the toxicity test of Coll EO showed no mortality rate to the concentration of 1g/kg injected to the mice. Conclusion: The results presented here constitutes new findings in the field of the chemical characterization and biological potential of Carduncellus pinnatus.

scholarly journals Synthesis and Antibacterial, Antimycobacterial Activity of 7-[4-{5-(2-Oxo-2-p-substituted-phenylethylthio)-1,3,4-thiadiazol-2yl}-3′-methylpiperazinyl] Quinolone Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Kapil M. Agrawal ◽  
Gokul S. Talele
Keyword(s):  
Biological Activities ◽  
Antimycobacterial Activity ◽  
Bacterial Strains ◽  
Mass Spectral ◽  
H Nmr ◽  
Mass Spectral Study ◽  
Weak Activity ◽  
Fluoroquinolone Derivatives ◽  
Quinolone Derivatives ◽  
C Nmr

Currently we screened 9 newer synthesized fluoroquinolone derivatives5(a–i)against two gram positive, two gram negative bacterial strains, and mycobacterium tuberculosis H37Rv. These analogues were confirmed by IR,1H NMR,13C NMR, and elemental analysis. Selected compounds were confirmed by mass spectral study. Compounds5(b–d)showed comparable biological activities and other analogues of the series showed moderate-to-weak activity, as compared to the reference marketed drugs.

Design, Synthesis and Biological Evaluation of of Novel Anticancer Agent tert-butyl 1-phenyl-3,4-dihydro-1H-pyrido[3,4-b]indole-2(9H)-carboxylate

2013 ◽  
Vol 781-784 ◽  
pp. 2211-2214
Author(s):  
Biao Shi ◽  
Yi Qian Wang ◽  
Yao Yang ◽  
Peng Yu ◽  
Kui Lu
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Biological Evaluation ◽  
Nmr Spectrum ◽  
Design Synthesis ◽  
H Nmr ◽  
Growth Inhibitory ◽  
Wide Range ◽  
New Compounds ◽  
Synthesis And Biological Evaluation

Indole and its derivatives extensively exist in nature, which showed a wide range of biological activities. Recently, there is a growing tendency to develop some new methods for the synthesis of novel indole derivatives and to study their biological properties. In this paper, we would like to report the design, synthesis and biological evaluation of a novel series of tricyclic indoles by employing Pictet-Spengler reaction as key step. All the target compounds were synthesized in four steps in 68-78% overall yield, which were characterized by 1H-NMR spectrum. All this new compounds were tested in an MTT assay on HepG2 and K562 and HT-29. Two of them showed tumor cell growth inhibitory good activity.

scholarly journals Novel Aryl Ether Derivatives as Antiinflammatory and Analgesics

2011 ◽  
Vol 8 (3) ◽  
pp. 1401-1407
Author(s):  
P. Rashmi ◽  
Gopal Krishna Rao ◽  
Kshama Devi ◽  
B. G. Shivananda ◽  
G. R. Swetha ◽  
...  
Keyword(s):  
Analgesic Activity ◽  
Mass Spectra ◽  
Biological Activities ◽  
Aryl Ether ◽  
H Nmr ◽  
Diaryl Ether ◽  
Wide Range ◽  
Aryl Ethers ◽  
New Compounds

The diaryl ether moieties have attracted considerable attention of medicinal chemists as they are endowed with a wide range of diverse biological activities. The present study involves synthesis, characterization of some new aryl ethers and evaluation of their antiinflammatory and analgesic activity. A series of new aryl ether derivatives[4(a-h), 5]were prepared by Ullmann’s ether condensation. The structures of new compounds are supported by their IR,1H NMR and Mass spectra. The new derivatives were evaluated for their antiinflammatory and analgesic activity. Among the tested, compound3has shown better antiinflammatory and analgesic activity.

A common mechanism links activities of butyrate in the colon

2017 ◽  
Author(s):  
Mohit S. Verma ◽  
Michael J. Fink ◽  
Gabriel L Salmon ◽  
Nadine Fornelos ◽  
Takahiro E. Ohara ◽  
...  
Keyword(s):  
Stem Cells ◽  
Histone Deacetylases ◽  
Biological Activities ◽  
Short Chain Fatty Acids ◽  
Common Mechanism ◽  
Epithelial Stem Cells ◽  
Degree Of Unsaturation ◽  
Structure Activity ◽  
Starting Point ◽  
New Compounds

Two biological activities of butyrate in the colon (suppression of proliferation of colonic epithelial stem cells and inflammation) correlate with inhibition of histone deacetylases. Cellular and biochemical studies of molecules similar in structure to butyrate, but different in molecular details (functional groups, chain-length, deuteration, oxidation level, fluorination, or degree of unsaturation) demonstrated that these activities were sensitive to molecular structure, and were compatible with the hypothesis that butyrate acts by binding to the Zn<sup>2+</sup> in the catalytic site of histone deacetylases. Structure-activity relationships drawn from a set of 36 compounds offer a starting point for the design of new compounds targeting the inhibition of histone deacetylases. The observation that butyrate was more potent than other short-chain fatty acids is compatible with the hypothesis that crypts evolved (at least in part), to separate stem cells at the base of crypts from butyrate produced by commensal bacteria.

Click Reactions in Chemistry of Triterpenes - Advances Towards Development of Potential Therapeutics

2018 ◽  
Vol 25 (5) ◽  
pp. 636-658 ◽  
Author(s):  
Jan Pokorny ◽  
Lucie Borkova ◽  
Milan Urban
Keyword(s):  
Biological Activities ◽  
Synthetic Approach ◽  
Clinical Use ◽  
New Approach ◽  
Click Reactions ◽  
Drug Candidates ◽  
The Past ◽  
Low Toxicity ◽  
New Compounds ◽  
Potential Therapeutics

Triterpenoids are natural compounds with a large variety of biological activities such as anticancer, antiviral, antibacterial, antifungal, antiparazitic, antiinflammatory and others. Despite their low toxicity and simple availability from the natural resources, their clinical use is still severely limited by their higher IC50 and worse pharmacological properties than in the currently used therapeutics. This fact encouraged a number of researchers to develop new terpenic derivatives more suitable for the potential clinical use. This review summarizes a new approach to improve both, the activity and ADME-Tox properties by connecting active terpenes to another modifying molecules using click reactions. Within the past few years, this synthetic approach was well explored yielding a lot of great improvements of the parent compounds along with some less successful attempts. A large quantity of the new compounds presented here are superior in both activity and ADME-Tox properties to their parents. This review should serve the researchers who need to promote their hit triterpenic structures towards their clinical use and it is intended as a guide for the chemical synthesis of better drug candidates.

scholarly journals Beehive Products as Antibacterial Agents: A Review

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 717
Author(s):  
Rita Abou Nader ◽  
Rawan Mackieh ◽  
Rim Wehbe ◽  
Dany El El Obeid ◽  
Jean Marc Sabatier ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Honey Bee ◽  
Antibacterial Agents ◽  
Royal Jelly ◽  
Biological Activities ◽  
Vital Role ◽  
Bee Venom ◽  
Bacterial Strains ◽  
Wide Range ◽  
Life Threatening

Honeybees are one of the most marvelous and economically beneficial insects. As pollinators, they play a vital role in every aspect of the ecosystem. Beehive products have been used for thousands of years in many cultures for the treatment of various diseases. Their healing properties have been documented in many religious texts like the Noble Quran and the Holy Bible. Honey, bee venom, propolis, pollen and royal jelly all demonstrated a richness in their bioactive compounds which make them effective against a variety of bacterial strains. Furthermore, many studies showed that honey and bee venom work as powerful antibacterial agents against a wide range of bacteria including life-threatening bacteria. Several reports documented the biological activities of honeybee products but none of them emphasized on the antibacterial activity of all beehive products. Therefore, this review aims to highlight the antibacterial activity of honey, bee venom, propolis, pollen and royal jelly, that are produced by honeybees.

Synthesis and characterization of a new series of thiadiazole derivatives as potential anticancer agents

2020 ◽  
Vol 26 (1) ◽  
pp. 6-13 ◽  
Author(s):  
Ulviye Acar Çevik ◽  
Derya Osmaniye ◽  
Serkan Levent ◽  
Begüm Nurpelin Sağlik ◽  
Betül Kaya Çavuşoğlu ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Cancer Cell Line ◽  
Chemotherapeutic Agents ◽  
Anticancer Activities ◽  
Normal Tissues ◽  
H Nmr ◽  
Wide Range ◽  
Thiadiazole Derivatives ◽  
Low Efficiency

AbstractCancer is one of the most common causes of death in the world. Despite the importance of combating cancer in healthcare systems and research centers, toxicity in normal tissues and the low efficiency of anticancer drugs are major problems in chemotherapy. Nowadays the aim of many medical research projects is to discover new safer and more effective anticancer agents. 1,3,4-Thiadiazole compounds are important fragments in medicinal chemistry because of their wide range of biological activities, including anticancer activities. The aim of this study was to determine the capacity of newly synthesized 1,3,4-thiadiazole compounds as chemotherapeutic agents. The structures of the obtained compounds were elucidated using 1H-NMR, 13C-NMR and mass spectrometry. Although the thiadiazole derivatives did not prove to be significantly cytotoxic to the tumour tissue cultures, compound 4i showed activity against the C6 rat brain cancer cell line (IC50 0.097 mM) at the tested concentrations.

scholarly journals Recent Findings in Azaphilone Pigments

2021 ◽  
Vol 7 (7) ◽  
pp. 541
Author(s):  
Lúcia P. S. Pimenta ◽  
Dhionne C. Gomes ◽  
Patrícia G. Cardoso ◽  
Jacqueline A. Takahashi
Keyword(s):  
Water Solubility ◽  
Biological Activities ◽  
Low Cost ◽  
Scale Up ◽  
Structural Diversity ◽  
Downstream Processing ◽  
Global Market ◽  
Yield Improvement ◽  
Potential Applications ◽  
New Compounds

Filamentous fungi are known to biosynthesize an extraordinary range of azaphilones pigments with structural diversity and advantages over vegetal-derived colored natural products such agile and simple cultivation in the lab, acceptance of low-cost substrates, speed yield improvement, and ease of downstream processing. Modern genetic engineering allows industrial production, providing pigments with higher thermostability, water-solubility, and promising bioactivities combined with ecological functions. This review, covering the literature from 2020 onwards, focuses on the state-of-the-art of azaphilone dyes, the global market scenario, new compounds isolated in the period with respective biological activities, and biosynthetic pathways. Furthermore, we discussed the innovations of azaphilone cultivation and extraction techniques, as well as in yield improvement and scale-up. Potential applications in the food, cosmetic, pharmaceutical, and textile industries were also explored.

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