scholarly journals PYRIMIDINES AS POTENT CYTOTOXIC AND ANTI-INFLAMMATORY AGENTS

2017 ◽  
Vol 10 (6) ◽  
pp. 237 ◽  
Author(s):  
Ishwar Bhat K ◽  
Abhishek Kumar
Keyword(s):  
Acetic Acid ◽  
Cytotoxic Activity ◽  
Glacial Acetic Acid ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Anti Inflammatory ◽  
Derivatives Of

Objective: Many derivatives of pyrimidine are known for the broad-spectrum biological activities such as antimicrobial, antitumor, antibacterial, antitubercular, anti-inflammatory, and cytotoxic activity. Chalcones with an enone group show potent pharmacological activities such as antiinflammatory, antibacterial, antifungal, and antimalarial activity. A series of pyrimidines from chalcones have been synthesized and screened for anti-inflammatory and cytotoxic activity studies.Methods: Chalcones [1-(4-nitrophenyl)-3-substituted-phenylprop-2-en-1-one] were synthesized from various substituted aldehydes with 4-nitroacetophenone and cyclized with urea and glacial acetic acid to give pyrimidine derivatives [4-(4-nitrophenyl)-6-substituted-phenylpyrimidin-2-ol].Results: Anti-inflammatory and cytotoxic activity studies revealed that some of the synthesized compounds have shown significant activity.Conclusion: The observed results proved that pyrimidines are found to be interesting lead molecules for the synthesis of anti-inflammatory and cytotoxic agents

scholarly journals Synthesis and Prognosis of Anti-inflammatory Activity of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3h)-one

2021 ◽  
Vol 7 (12) ◽  
pp. 25-33
Author(s):  
A. Chiriapkin ◽  
I. Kodonidi ◽  
A. Ivchenko ◽  
L. Smirnova
Keyword(s):  
Acetic Acid ◽  
Biological Activity ◽  
Dimethyl Sulfoxide ◽  
In Silico ◽  
Glacial Acetic Acid ◽  
Inflammatory Activity ◽  
Modified Method ◽  
Anti Inflammatory ◽  
Catalytic Addition ◽  
Derivatives Of

The article presents a modified method for the synthesis of 2-substituted 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine-4(3H)-one and the predict of their anti-inflammatory activity. The proposed method for obtaining tetrahydrothienopyrimidine derivatives is preparatively effective and simple. Their synthesis was carried out by heterocyclization of azomethine derivatives of 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide in the medium of glacial acetic acid with the catalytic addition of dimethyl sulfoxide. Preliminary prognosis of anti-inflammatory activity in silico method allowed us to identify the most promising compounds. Of these, the 4b structure containing a 2-hydroxyphenyl fragment in the second position of pyrimidine-4(3H)-one may be of the greatest interest. It seems appropriate to further study the spectrum of biological activity of the studied compounds.

scholarly journals PYRAZOLINES AS POTENT ANTITUBERCULAR AND CYTOTOXIC AGENTS

2017 ◽  
Vol 10 (6) ◽  
pp. 247 ◽  
Author(s):  
Ishwar Bhat K ◽  
Abhishek Kumar
Keyword(s):  
Cytotoxic Activity ◽  
Hydrazine Hydrate ◽  
Antimalarial Activity ◽  
Cytotoxic Agents ◽  
Pharmacological Properties ◽  
Aromatic Rings ◽  
Pharmacological Activities

Objective: Pyrazolines are known to exhibit different biological and pharmacological properties such as anticancer, antibacterial, antifungal and antitubercular activities. Chalcones with an enone group between two aromatic rings exhibit remarkable pharmacological activities such as antiinflammatory, antibacterial, antitumor, antifungal, and antimalarial activity. A series of pyrazolines from chalcones have been synthesized and evaluated for antitubercular and cytotoxic activity studies.Methods: Chalcones [3-substituted phenyl-1-(p-tolyl)prop-2-en-1-one] were synthesized from various substituted aldehydes and 4-methyl acetophenone and cyclized into pyrazolines [5-substituted phenyl-3-(p-tolyl)-4,5-dihydro-1H-pyrazole] using hydrazine hydrate. Antitubercular and cytotoxic activity studies were carried out.Results: Antitubercular and cytotoxic activity studies of synthesized pyrazoline revealed that some compounds have showed promising activity.Conclusion: The observed results proved that pyrazolines are found to be interesting lead molecules for further synthesis as antitubercular and cytotoxic agents.

scholarly journals Review Article: Various Biological Activities of Coumarin and Oxadiazole Derivatives.

2017 ◽  
Vol 10 (7) ◽  
pp. 38 ◽  
Author(s):  
Sunny Jalhan
Keyword(s):  
Biological Activities ◽  
Biochemical Properties ◽  
Review Article ◽  
Pharmacological Activities ◽  
Wide Range ◽  
Methylene Groups ◽  
Anti Oxidant ◽  
Oxadiazole Derivatives ◽  
Anti Inflammatory ◽  
Derivatives Of

In this review article data is collected regarding the various derivatives of coumarin and oxadiazole as both these have wide range of biological activities and they can be further modified to synthesize more effective and potent drugs. Coumarin class of organic compounds consists of 1,2-benzopyrone ring system as a basic parent scaffold. These benzopyrones are subdivided into alpha-benzopyrones and gamma benzopyrones; with coumarin class of compounds belonging to alpha-benzopyrones. Since the last few years, coumarins were synthesized in many of their derivative forms. Their pharmacological, therapeutic and biochemical properties depend upon their pattern of substitution. Coumarins exhibit a wide range of pharmacological activities, which includes anti-diabetic, anti-viral, anti-microbial, anticancer, anti-oxidant, anti-parasitic, anti-helminthic, anti-proliferative, anti-convulsant, anti-inflammatory and antihypertensive activities. 1,3,4-Oxadiazole is a heterocyclic compound containing an oxygen atom and two nitrogen atoms in a five-membered ring. It is derived from furan by substitution of two methylene groups (=CH) with two pyridine type nitrogens (-N=). There are three known isomers: 1,2,4-oxadiazole, 1,2,3-oxadiazole and 1,2,5- oxadiazole. Oxadiazole moiety shows antimicrobial, anticancer and anti-inflammatory activity and suitably substituted 1,3,4-oxadiazole having biological activities like antimicrobial, anticancer and other biological activities.

scholarly journals RECENT STRATEGIES FOR EFFICIENT SYNTHESIS AND BIOLOGICAL ACTIVITIES OF COUMARIN-CHALCONE DERIVATIVES

2020 ◽  
pp. 28-37
Author(s):  
SATHISH KUMAR KONIDALA ◽  
VIJAY KOTRA
Keyword(s):  
Antimalarial Activity ◽  
Biological Activities ◽  
Clinical Applications ◽  
Biologically Active ◽  
Efficient Synthesis ◽  
Huge Number ◽  
Pharmacological Activities ◽  
Chalcone Derivatives ◽  
Naturally Occurring ◽  
Anti Inflammatory

Coumarins and chalcones are potential pharmacological and biologically active molecules obtained from natural source. Coumarins have predominant pharmacological activities such as antidiabetic, antitumor, and anti-inflammatory activity. Chalcones are also one of the naturally occurring pharmacologically vital molecules with different activities such as anti-inflammatory, antitumor, antimicrobial, and antimalarial activity. Literature reveals that a huge number of coumarinyl chalcone derivatives have various pharmacological activities. Coumarinyl chalcone derivatives gained more prominence due to their significant biological activities. This work explains the current information about synthesis techniques, pharmacological importance, and clinical applications of coumarinyl chalcone derivatives.

scholarly journals Synthesis and Biological Activities of Some Pyrimidine Derivatives: A Review

2020 ◽  
Vol 36 (6) ◽  
pp. 1001-1015
Author(s):  
Nadia Ali Ahmed Elkanzi
Keyword(s):  
Nitrogen Atom ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Heterocyclic Ring ◽  
Ring System ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Cardiovascular Agents ◽  
Anti Hiv ◽  
Biological And Pharmacological Activities

Nitrogen containing synthetically and biologically important heterocyclic ring system namely pyrimidine possess both biological and pharmacological activities, and defend as aromatic six heterocyclic with 1and 3 nitrogen atom in ring. Preparation of pyrimidine via different methods offer its importance in fields of medicinal chemistry and Chemistry. Pyrimidines and their derivatives act as anti-inflammatory, anti-malaria, anti-tumor, cardiovascular agents, anti-neoplastic, anti-tubercular, anti- HIV, diuretic ,anti-viral, anti-microbial, ,analgesic .This review give light up on biological and pharmacological activities of pyrimidine nucleus.

Synthesis, Characterization and Evaluation of some newer Pyrimidine derivatives as Anti-inflammatory Agents

2021 ◽  
pp. 2529-2534
Author(s):  
Kalpana Divekar ◽  
Rekha. S ◽  
Murugan. Vedigounder ◽  
Shivaprakash. H
Keyword(s):  
Biological Activities ◽  
Diclofenac Sodium ◽  
Pyrimidine Derivative ◽  
Inflammatory Activity ◽  
Paw Edema ◽  
Pyrimidine Derivatives ◽  
Anti Inflammatory ◽  
1Hnmr Spectroscopy ◽  
Hydrolysis Of ◽  
Antiparasitic Agents

Pyrimidine is an important baseone of the base formed by hydrolysis of nucleosides. It is an interesting molecule in the medicinal chemistry because of its diversified biological activities. Alloxan which is an oxidation product of Uric acid is also a pyrimidine derivative of interest to a medicinal chemist. Several pyrimidines are reported as antimicrobial, analegesic, anti-inflammatory, antibacterial, and antiparasitic agents. Pyrimidine scaffold is considered as an interesting one due to its various pharmacological properties. In this scheme, an attempt is made to carry out synthesis of some new pyrimidine derivatives. The Starting material Chalcone is synthesized by condensation of various aromatic aldehyde and aromatic ketone. Chalcone is then treated with thiourea and KOH in presence of ethanol to yield pyrimidine derivatives. Then those pyrimidine derivatives were subjected to alkylation and acetylation. The synthesized compounds were characterized and confirmed by IR and 1HNMR spectroscopy and then evaluated for their anti-inflammatory activity. The anti-inflammatory activity of newly synthesized pyrimidine derivatives were carried out by the carrageenan induced rat hind paw edema method by taking Diclofenac sodium as standard.

scholarly journals Evaluation of Analgesic and Anti-inflammatory Activities of Polyalthia simiarum (Hook. F. &Thomson)

2019 ◽  
Vol 5 (1) ◽  
pp. 18-23
Author(s):  
Selina Kabir ◽  
Ronok Zahan ◽  
Abdullah Mohammad Sarwaruddin Chowdhury ◽  
Choudhury Mahmood Hasan ◽  
Mohammad Abdur Rashid
Keyword(s):  
Acetic Acid ◽  
Analgesic Activity ◽  
Biological Activities ◽  
Dependent Manner ◽  
Paw Edema ◽  
Immersion Method ◽  
Ongoing Research ◽  
Tail Immersion ◽  
Anti Inflammatory ◽  
Dose Dependent

Background: Polyalthia simiarum (Hook. F. &Thomson) exhibits different effects in human body. Objective: As a part of ongoing research on medicinal plants of Bangladesh, the present study is focused to investigate the analgesic and anti-inflammatory activities of stem bark of Polyalthia simiarum (Annonaceae). Methodology: The ethyl acetate (EA) and petroleum ether (PE) extracts were subjected to qualitative chemical investigation for the identification of different phytoconstituents. The analgesic activity was determined for its central and peripheral pharmacological actions using tail immersion method and acetic acid-induced writhing test. The anti-inflammatory activity was evaluated by carrageenan induced paw edema in rats. Analgesic and anti-inflammatory data were evaluated statistically analysed by Dunnett’s-T test. Result: Both extracts at the dose of 50- and 100 mg/kg b.w., produced significant increase in pain threshold in tail immersion method whereas significantly reduced the writhing caused by acetic acid in a dose dependent manner. The EA and PE extracts showed anti-inflammatory activities at 50- and 100 mg/kg body weight. Among all the extracts, the EA extract showed a dose dependent and comparable analgesic activity in all the tested methods and also reduced the paw edema considerably (27.5% and 39.1% inhibition after 4h), in dose dependent manner when compared to carrageenan induced control rat. Conclusion: Therefore, the EA and PE extracts of Polyalthia simiarum were capable to exhibit moderate analgesic and anti-inflammatory activities. This is the first report of analgesic and anti-inflammatory potential of Polyalthia simiarum and can be further investigated to isolate the active compounds responsible for the biological activities. Journal of National Institute of Neurosciences Bangladesh, 2019;5(1): 18-23

scholarly journals Biochemistry, Safety, Pharmacological Activities, and Clinical Applications of Turmeric: A Mechanistic Review

2020 ◽  
Vol 2020 ◽  
pp. 1-14 ◽  
Author(s):  
Rabia Shabir Ahmad ◽  
Muhammad Bilal Hussain ◽  
Muhammad Tauseef Sultan ◽  
Muhammad Sajid Arshad ◽  
Marwa Waheed ◽  
...  
Keyword(s):  
Clinical Research ◽  
Biological Activities ◽  
Curcuma Longa ◽  
Clinical Applications ◽  
Pharmacological Activities ◽  
Neuroprotective Effects ◽  
Wide Range ◽  
Different Types ◽  
Safety And Toxicity ◽  
Anti Inflammatory

Turmeric (Curcuma longa L.) is a popular natural drug, traditionally used for the treatment of a wide range of diseases. Its root, as its most popular part used for medicinal purposes, contains different types of phytochemicals and minerals. This review summarizes what is currently known on biochemistry, safety, pharmacological activities (mechanistically), and clinical applications of turmeric. In short, curcumin is considered as the fundamental constituent in ground turmeric rhizome. Turmeric possesses several biological activities including anti-inflammatory, antioxidant, anticancer, antimutagenic, antimicrobial, antiobesity, hypolipidemic, cardioprotective, and neuroprotective effects. These reported pharmacologic activities make turmeric an important option for further clinical research. Also, there is a discussion on its safety and toxicity.

scholarly journals Analgesic and Anti-Inflammatory Activities of Resveratrol through Classic Models in Mice and Rats

2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Guangxi Wang ◽  
Zhiqiang Hu ◽  
Xu Song ◽  
Qiankun Cui ◽  
Qiuting Fu ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Biological Activities ◽  
Drug Candidate ◽  
Hot Plate ◽  
Sod Activity ◽  
Analgesic Effects ◽  
Mouse Ear ◽  
Anti Inflammatory ◽  
Ear Oedema

Background. Inflammation and pain are closely related to humans’ and animals’ health.Resveratrol(RSV) is a natural compound with various biological activities. The current study is aimed to evaluate the analgesic and anti-inflammatory activities of RSV in vivo. Materials and Methods. The analgesic effects were assessed by the acetic acid-induced writhing and hot plate tests. The anti-inflammatory effects were determined using the xylene-induced mouse ear oedema, the acetic acid-induced rat pleurisy, and carrageenan-induced rat synovitis tests, respectively.Results. The analgesic results showed that RSV could significantly inhibit the number of writhes and improve the time and pain threshold of mice standing on hot plate. The anti-inflammatory results showed that RSV could inhibit the ear oedema of mice. In acetic acid-induced pleurisy test, RSV could significantly inhibit the WBC and pleurisy exudates, could decrease the production of NO, and elevate the activity of SOD in serum. In carrageenan-induced synovitis test, RSV could reduce the content of MDA and elevate the T-SOD activity in serum; RSV could inhibit the expressions of TP, PGE2, NO, and MDA.Conclusion. Shortly, these results indicated that RSV had potent analgesic and anti-inflammatory activities and could be a potential new drug candidate for the treatment of inflammation and pain.

scholarly journals SYNTHESIS OF SOME PYRIMIDINE DERIVATIVES OF EXPECTED BIOLOGICAL ACTIVITIES

2005 ◽  
Vol 28 (1) ◽  
pp. 17-25 ◽  
Author(s):  
Wafaa Zaghary ◽  
Aida El-Azzouny ◽  
Mohammed Motaleb ◽  
Mohammed Kedr
Keyword(s):  
Biological Activities ◽  
Pyrimidine Derivatives ◽  
Derivatives Of
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