scholarly journals Synthesis and Evaluation of Important Biologically Active Heterocyclic Compounds: Schiff Bases, Oxadiazole and Pyrazolyl Derivatives

2013 ◽  
Vol 9 (2) ◽  
pp. 1892-1899
Author(s):  
Mona A. Hosny ◽  
Wafaa A. Mokbe ◽  
Emtithal A. El-Sawi
Keyword(s):  
Breast Cancer ◽  
Heterocyclic Compounds ◽  
Biologically Active ◽  
High Antimicrobial Activity ◽  
Pharmacological Activities ◽  
Ic50 Value ◽  
New Compounds ◽  
Value Of It ◽  
Derivatives Of ◽  
Acid Compound

In this work, we prepared an excellent yield of (2-oxo-2H-pyrano[3,2-h] quinolin-4-yl) acetic acid; compound (1) and from the reaction of it with hydrazine hydrate (100%) we obtain 2-(2-oxo-2H-pyrano [3,2-h] quinolin-4-yl) aceto hydrazide (2) which is the starting material for the synthesis of several series of new compounds: such as schiff’s bases (3a-e) and compound (4) in good yields, hydrazide derivatives like compound (5), derivatives of mercapto oxadiazole as compound (6) and derivatives of pyrazolyl as compound (7). All these compounds were found to possess high antimicrobial activity against G+ and G- bacteria and against antifungal as described in scheme (1). Anticancer activity was screened only for compound (1). The IC50 value of it against breast cancer was found = 6.83 µM comparable with that of the drug of doxorubicin which has IC50 = 5.6. As a result these newly compounds from (1) to (7) are considerable as potent compounds for various pharmacological activities. 

Dual Acting Isatin-heterocyclic Hybrids: Recent Highlights as Promising Pharmacological Agents

2018 ◽  
Vol 16 (2) ◽  
pp. 220-236 ◽  
Author(s):  
Srinubabu Maddela ◽  
Githa Elizabeth Mathew ◽  
Della Grace Thomas Parambi ◽  
Fakhria Aljoufi ◽  
Bijo Mathew
Keyword(s):  
Single Molecule ◽  
Heterocyclic Compounds ◽  
Structural Modification ◽  
Drug Efficacy ◽  
Biologically Active ◽  
Synergistic Activity ◽  
Pharmacological Activities ◽  
Pharmacological Agents ◽  
Drug Candidates ◽  
Derivatives Of

Background: For the development of suitable lead molecules to different diseases is a highly challenging task for medicinal chemists. Nowadays, hybrid pharmacophore concept has developed as a useful structural modification tool in the drug design of new drug candidates for different diseases. Hybrid pharmacophore approach consists of combination of two or more pharmacophoric moieties from different biologically active compounds with complementary functions or different mechanisms of action into a single molecule. This often results in synergistic activity or enhanced drug efficacy. Objective: To develop the suitable leads for different diseases there will be a lot of scope to study the substitution of heterocyclic moieties on the different positions of isatin ring. The broad and potent activities of the isatin and their derivatives have been established them as pharmacologically significant scaffolds. In this review, an attempt has been made with specifically emphasizing the hybridization of Isatin with different derivatives of heterocyclic compounds on the different positions of the isatin ring (aryl ring, isatin nitrogen and C2/C3 carbonyl moieties). Conclusion: This review highlighted the recent advances of dual acting isatin-heterocyclic hybrids presenting various pharmacological activities viz., anticancer, antitubercular, anti-inflammatory and antimicrobial.

A REVIEW ON RECENT ADVANCES IN CHEMISTRY, SYNTHESIS AND BIOLOGICAL APPLICATIONS OF ISATIN DERIVATIVES

2018 ◽  
pp. 16-22
Author(s):  
Shukla PK ◽  
Singh MP ◽  
Patel R
Keyword(s):  
Heterocyclic Compounds ◽  
Biologically Active ◽  
Biological Applications ◽  
Plant Origin ◽  
Recent Past ◽  
Pharmacological Activities ◽  
Naturally Occurring ◽  
Recent Advances ◽  
Biological Aspects ◽  
Isatin Derivatives

Indole and its derivatives have engaged a unique place in the chemistry of nitrogen heterocyclic compounds. The recognition of the plant growthhormone, heteroauxin, the significant amino acids, tryptamine & tryptophan and anti-inflammatory drug, indomethacine are the imperativederivatives of indole which have added stimulus to this review work. Isatin (1H-indole-2,3-dione), an indole derivative of plant origin. Althoughit is a naturally occurring compound, but was synthesized by Erdmann and Laurent in 1840 before it was found in nature. Isatin is a versatileprecursor for many biologically active molecules and its diversified nature makes it a versatile substrate for further modifications. It is concernedin many pharmacological activities like anti-malarial, antiviral, anti-allergic, antimicrobial etc; isatin and its derivatives have been also found todemonstrate promising outcomes against various cancer cell lines. This review provides a brief overview on the recent advances and futureperspectives on chemistry and biological aspects of isatin and its derivatives reported in the recent past.

SOME DIRECTIONS IN THE MODIFICATION OF AZOLES

2020 ◽  
Vol 5 (443) ◽  
pp. 85-91
Author(s):  
Ibrayev M.K., ◽  
◽  
Takibayeva A.T., ◽  
Fazylov S.D., ◽  
Rakhimberlinova Zh.B., ◽  
...  
Keyword(s):  
13C Nmr Spectroscopy ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Synthesis Conditions ◽  
Alkaloid Cytisine ◽  
Azole Ring ◽  
Cyclic Compounds ◽  
New Compounds ◽  
Derivatives Of

This article presents studies on the targeted search for new derivatives of azoles, such as benzthiazole, 3,5-dimethylpyrazole, 1,3,4-oxadiazole-2-thione, 1,3,4-thiadiazole. The possibility of combining in one molecule of the azole ring with other cyclic compounds: the alkaloid cytisine, morpholine, furan and some arenes has been studied. To obtain new compounds, the reactions of bromination, acylation, and interaction with isothiocyanates were studied. Optimal synthesis conditions were studied for all reactions. It was found that the reaction of 4-bromo-3,5-dimethylpyrazole with isothiocyanates, in contrast to the previously written derivatives of anilines, takes a longer time and requires heating the reaction mixture. The combination of a pirasol fragment with halide substituents often results in an enhanced therapeutic effect. The synthesized 2-bromine-N-(6-rodanbenzo[d]thiazole-2-yl)acetamide, due to the alkylbromide group, is an important synth in the synthesis of new benzthiazole derivatives. Its derivatives combine in one molecule the rest of rhodanbenzthiazole with alkaloid cytisine and biogenic amine morpholine and are potentially biologically active compounds, since the molecule structure contains several pharmacophoric fragments: benzthiazole and alkaloid (amine) heterocycles, rhodane and urea groups. The mechanism of formation of 1,3,4-oxadiazole-2-tyons from hydrazides under action on them by carbon disulfide was studied and assumed. It was shown that dithiocarbamates in acidic medium decompose with the release of hydrogen sulfide and the formation of highly reactive isothiocyanate group. Then, intra-molecular cyclization occurs, with the formation of end products - 1,3,4-oxadiazole-2-thions. The structures of the synthesized compounds were studied by 1H and 13C NMR spectroscopy. All synthesized substances are potentially biologically active compounds, since they contain several pharmacophore fragments in their structure.

scholarly journals A Short Review on Heterocyclic Compounds Showing Anti-Breast Cancer Activity

2021 ◽  
Vol 13 (3) ◽  
pp. 1075-1098
Author(s):  
R. Ayana ◽  
B. Vijayakumar ◽  
P. Athulya ◽  
V. S. Anjana ◽  
K. V. Vismaya ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Heterocyclic Compounds ◽  
Drug Users ◽  
Short Review ◽  
Inadequate Response ◽  
Tumor Resistance ◽  
Model Data ◽  
Common Cancer ◽  
Interesting Possibility ◽  
New Compounds

Breast cancer (BC) is the most common cancer for females, and its incidence tends to increase year by year. Currently, the backbone of therapy for BC is mainly chemotherapy; however, its toxicity in normal cells and acquired tumor resistance to the drug users are considered the main barriers. Therefore, there is still an urgent need for the development of more effective and safer anti-BC agents. Based on previous reference documents in recent years, this review covers the work reported on the anti-BC compounds classified according to the structures. This review summarized significant anti-BC compounds organized by functional groups according to the animal model data, although there would be some limitations. This review highlights the properties of new compounds having promising anti-BC properties, which may be proven to be more effective and selective, and possibly free of unwanted side effects. The reviewed compounds represent an interesting possibility of overcoming BC and reducing the percentage of patients with an inadequate response to drug therapy.

Synthesis and Reactions of Perimidines and Their Fused Systems

2020 ◽  
Vol 24 (15) ◽  
pp. 1669-1716 ◽  
Author(s):  
Thoraya A. Farghaly ◽  
Sami A. Al-Hussain ◽  
Zeinab A. Muhammad ◽  
Magda A. Abdallah ◽  
Magdi E. A. Zaki
Keyword(s):  
Chemical Reactions ◽  
Heterocyclic Compounds ◽  
Antifungal Agents ◽  
Biological Activities ◽  
Lone Pair ◽  
Pharmacological Activities ◽  
Synthetic Analogs ◽  
Interesting Class ◽  
Derivatives Of

Perimidines are peri-naphtho-fused derivatives of pyrimidine. They are of particular interest as they are a rare example of an azine in which the lone pair of electrons of pyrrole-like nitrogen participates in the π-system of the molecule. Perimidine is an interesting class of heterocyclic compounds. Various synthetic analogs of perimidines have been prepared and evaluated for many pharmacological activities in different models with desired findings. They exhibit biological activities as antitumor, antiulcer, antimicrobial, and antifungal agents. This review is an attempt to organize the synthesis and chemical reactions of perimidine analogs reported to date systematically since 1955. It should be noted that this review is the first one that includes the preparation and reactions of the perimidine ring.

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.

scholarly journals Synthesis and physicochemical properties 4-((R))amino)-5-methyl-4H-1,2,4-triazole-3-thiols

2018 ◽  
pp. 55-59
Author(s):  
T. V. Kravchenko ◽  
O. I. Panasenko ◽  
Ye. G. Knysh
Keyword(s):  
Physicochemical Properties ◽  
High Efficiency ◽  
Chemical Compounds ◽  
Biological Properties ◽  
Biologically Active ◽  
Physical Chemical ◽  
Medical University ◽  
New Compounds ◽  
Instrumental Methods ◽  
Derivatives Of

Purposeful synthesis of derivatives of 1,2,4-triazole is one of the most important branches of modern pharmaceutical science Modern pharmaceutical market of domestic medicines requires constant updates of existing range. It makes possible the synthesis of new compounds with a predicted biological activity. The main advantage of derivatives of 1,2,4-triazole is high efficiency and low toxic. That is promising factor for creation of new chemical compounds. Analysis of literary data of past few years has showed that there is not enough information about synthesis, physical, chemical and biological properties of derivatives of 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol in the literature. So synthesis and further research of derivatives of 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol is topical. The research took place at the Department of toxicological and inorganic Chemistry of Zaporizhzhia State Medical University (the head of the department – professor O. I. Panasenko). During the work the research were the physicochemical properties of newly synthesized of compounds in accordance with the methods described in the State Pharmacopoeia of Ukraine. As starting substance was used 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol obtained by cyclization of of potassium 2-atsetilgidrazinkarboditioata in the medium hydrazine hydrate. It is planned to research of the compounds obtained in the antimicrobial, act-protective, antioxidative and hypolipidemic activity. 9 new compounds of ylidene derivatives of 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol were synthesized in a research. The structure of the new synthesized of substances was confirmed by with by means of modern of instrumental methods analysis (1H-PMR-spectroscopy, chromato-mass-spectrometry, elemental analysis). The obtained data is possible to use in purposeful synthesis for the further research of biologically active compounds.

scholarly journals Synthesis and structural features of 5-(4-(tert-butyl) phenyl)-4-((R)amino)-4H-1,2,4-triazole-3-thiols

2018 ◽  
pp. 60-65
Author(s):  
I. I. Aksyonova-Seliuk ◽  
O. I. Panasenko ◽  
E. G. Knysh
Keyword(s):  
Chemical Structure ◽  
Chemical Properties ◽  
Biologically Active ◽  
Physical And Chemical Properties ◽  
Tert Butyl ◽  
New Compounds ◽  
Physical And Chemical ◽  
Derivatives Of ◽  
Active Substances ◽  
And Chemical Properties

Chemistry of heterocyclic compounds is one of the most popular sector in organic chemistry. Scientists allocate among them a class of derivatives of 1,2,4-triazole. This class of compounds attracts attention his broad spectrum of biological activity. There are antiviral, anti-inflammatory, anti-tubercular, antimicrobial, antioxidant, actoprotective, anti-cancer and other activities. The derivatives of 1,2,4-triazole have one more important advantage. It is low toxicity. This properties do this class of derivatives promising for researches their chemical structure and biological activity and purposeful search of biologically active substances. The purpose of the work is synthesis of 5-(4-(tert-butyl)phenyl)-4-((R)amino)-4H-1,2,4-triazoles-3-thiols from appropriate ylidene derivatives of 4-amino-5-(4 (tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol and research of their physical and chemical properties. The objects of research were 10 new compounds, derivatives of 4-amino-5-(4-(tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol. These compounds are the crystal substances which are odorless, insoluble in water and soluble in organic solvents. Investigation of the physical and chemical properties of this compounds was carried out according to the methods listed in the State Pharmacopoeia of Ukraine. The melting temperature of synthesized compounds was determined by device OptiMelt Stanford Research Systems MPA100. The structure of the compound was confirmed by 1H-NMR spectroscopy (Mercury 400) and gas chromatography-mass spectrometry (Agilent 1260 Infinity HPLC). 10 new compounds, derivatives of 4-amino-5-(4-(tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol, were synthesized in a study. The chemical structure of the new compounds was confirmed by modern instrumental methods of analysis. Results of the done work can be use in the future search of biologically active substances.

Evaluation of Acetylcholinesterase and Prolyl Oligopeptidase Inhibition of Novel Amino acid-functionalized Stigmasterol and Ursolic Acid Derivatives

2019 ◽  
Vol 23 (19) ◽  
pp. 2131-2140
Author(s):  
Nalin Seixas ◽  
Ionara I. Dalcol ◽  
Bruno Ravanello ◽  
Keiti Alessio ◽  
Fábio A. Duarte ◽  
...  
Keyword(s):  
Amino Acid ◽  
Ursolic Acid ◽  
Prolyl Oligopeptidase ◽  
Pharmacological Activities ◽  
Natural Sources ◽  
Structural Modifications ◽  
Ic50 Value ◽  
Ic50 Values ◽  
Pharmacological Potential ◽  
New Compounds

Triterpenes and phytosterols are classes of natural compounds widespread in plants possessing a great number of pharmacological activities. In our continued search for new compounds from natural sources with pharmacological potential, we prepared a series of novel stigmasterol and ursolic acid (UA) derivatives by coupling with L-proline, L-cysteine and L-glutamic acid. Unlike stigmasterol, the eight derivatives obtained showed good inhibitory capacity against acetylcholinesterase (AChE) or prolyl oligopeptidase (POP). Among these derivatives, we highlight 3 and 5 with IC50 values of 99.0 ± 8.8 and 97.5 ± 5.0 µM against AChE, respectively, and derivative 8 with a POP IC50 value of 75.7 ± 6.3 µM. The ursolic acid derivative 19 was the most promising compound of its class, with IC50 against AChE of 98.3 ± 7.7 µM. These results demonstrate that simple structural modifications on triterpenes and phytosterols can enhance their performance as enzymatic inhibitors.

A Mini-Review on Pharmacological Importance of Benzothiazole Scaffold

2020 ◽  
Vol 17 ◽  
Author(s):  
Mohammad Asif ◽  
Mohd. Imran
Keyword(s):  
Heterocyclic Compounds ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Pharmacological Activities ◽  
Structural Alterations ◽  
Benzothiazole Derivatives ◽  
Drug Molecules ◽  
Anti Inflammatory ◽  
Almost All

: Heterocyclic compounds are important because they have almost all types of pharmacological properties. Due to these properties of heterocyclic compounds, they attracted the researchers for the development of more effective newer drug molecules. In this review, we are focused on benzothiazole and its derivatives, which are used for the synthesis of various biologically active molecules. Benzothiazole derivatives have been possessed the various type of pharmacological activities like antimicrobial, anti-inflammatory, analgesic, anticonvulsant, antiviral, anthelmintic, antioxidant, anticancer, and other anticipated activities. Hence, structural alterations have resulted in different benzothiazole derivatives that illustrated a wide variety of pharmacological activities.

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