Recent Advancements in Biological Activities of Oxadiazole and their Derivatives: A Review

2020 ◽  
Vol 17 (6) ◽  
pp. 409-429
Author(s):  
Arun Kumar Mishra ◽  
Arvind Kumar ◽  
Jagdish K. Sahu
Keyword(s):  
In Silico ◽  
Biological Activities ◽  
Therapeutic Agents ◽  
Isomeric Form ◽  
Molecular Formula ◽  
Synthetic Analogues ◽  
Oxadiazole Derivatives ◽  
In Silico Models ◽  
Anti Hiv Agents ◽  
Anti Hiv

Oxadiazole moiety, which is one of the heterocyclic aromatic groups of the azole family; with the molecular formula C2H2N2O, exists in four isomeric form; out of which, 1,2,4-oxadiazole; 1,2,5-oxadiazole and 1,3,4-oxadiazole are common isomers. The stable isomeric forms of oxadiazoles are observed in a variety of pharmaceutical important potent drugs including raltegravir, butalamine, fasiplon, oxolamine and pleconaril. An attempt has been made to emphasize the chemistry and pharmacology associated with oxadiazole and its derivatives. A number of oxadiazole derivatives are very popular and common in use as potential therapeutic agents. However, a number of researchers are working and have worked to find out more synthetic analogues for anticancer and antifungal, anti-HIV agents using biological and in-silico models.

Synthetic and Biological Attributes of Pyrimidine Derivatives: A Recent update

2021 ◽  
Vol 18 ◽  
Author(s):  
Meenu Devi ◽  
Shivangi Jaiswal ◽  
Sonika Jain ◽  
Navjeet Kaur ◽  
Jaya Dwivedi
Keyword(s):  
Biological Activities ◽  
Structural Diversity ◽  
Therapeutic Agents ◽  
Pyrimidine Derivatives ◽  
Diverse Range ◽  
Biological Attributes ◽  
Synthetic Approaches ◽  
High Degree ◽  
Therapeutic Activities ◽  
Anti Hiv

: Nitrogen-containing heterocycles attract the attention of chemists due to their multifarious activities. Amongst all, pyrimidine plays a central role and exhibits a broad spectrum of biological activities. Literature is replete with the various aspects of synthetic development in pyrimidine chemistry for a wide array of applications. It aroused our interest to compile various novel and efficient synthetic approaches towards the synthesis of pyrimidine and its derivatives. Pyrimidine derivatives are broadly useful as therapeutic agents, owing to their high degree of structural diversity. They have been recorded to possess a diverse range of therapeutic activities, viz. anticancer, anti-inflammatory, anti-HIV etc.

In silico studies on new oxathiadiazoles as potential anti-HIV agents

Gene Reports ◽  
2019 ◽  
Vol 14 ◽  
pp. 87-93 ◽  
Author(s):  
Madhu Yadav ◽  
Ritika Srivastava ◽  
Farha Naaz ◽  
Anuradha Singh ◽  
Rajesh Verma ◽  
...  
Keyword(s):  
In Silico ◽  
In Silico Studies ◽  
Anti Hiv Agents ◽  
Anti Hiv

Synthesis and Antiviral Activity of 1,3-Disubstituted Uracils against HIV-1 and HCMV

2003 ◽  
Vol 14 (5) ◽  
pp. 271-279 ◽  
Author(s):  
Tokumi Maruyama ◽  
Shigetada Kozai ◽  
Tetsuo Yamasaki ◽  
Myriam Witvrouw ◽  
Christophe Pannecouque ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Antiviral Activity ◽  
Human Cytomegalovirus ◽  
Therapeutic Agents ◽  
Reverse Transcriptase Inhibitors ◽  
Uracil Derivatives ◽  
Immunodeficiency Virus ◽  
Anti Hiv Agents ◽  
Anti Hiv ◽  
Hiv 1

The development of new non-nucleoside reverse transcriptase inhibitors (NNRTIs) is an efficient strategy for finding new therapeutic agents against human immunodeficiency virus (HIV). A large number of 6-substituted uracil derivatives have been prepared in order to explore new NNRTIs. However, there are few approaches to anti-HIV agents from 1,3-disubstituted uracil derivatives. Therefore, we tried to prepare several 1,3-disubstituted uracils, which were easily obtainable from uracil by preparation under alkali and Mitsunobu conditions, and examined their antiviral activity against HIV-1 and human cytomegalovirus (HCMV). We found that 1-benzyl-3-(3,5-dimethylbenzyl)uracil and 1-cyanomethyl-3-(3,5-dimethylbenzyl)-4-thiouracil showed powerful inhibition against HCMV and HIV-1, respectively.

Biological Profiling of Anti-HIV Agents and Insight into CCR5 Antagonist Binding Using in silico Techniques

ChemMedChem ◽  
2009 ◽  
Vol 4 (7) ◽  
pp. 1153-1163 ◽  
Author(s):  
Antonio Carrieri ◽  
Violeta I. Pérez-Nueno ◽  
Alessandra Fano ◽  
Carlo Pistone ◽  
David W. Ritchie ◽  
...  
Keyword(s):  
In Silico ◽  
Ccr5 Antagonist ◽  
Antagonist Binding ◽  
Anti Hiv Agents ◽  
Anti Hiv ◽  
Insight Into

scholarly journals Synthesis, In Silico and In Vitro Evaluation for Acetylcholinesterase and BACE-1 Inhibitory Activity of Some N-Substituted-4-Phenothiazine-Chalcones

Molecules ◽  
2020 ◽  
Vol 25 (17) ◽  
pp. 3916
Author(s):  
Thai-Son Tran ◽  
Minh-Tri Le ◽  
Thi-Cam-Vi Nguyen ◽  
The-Huan Tran ◽  
Thanh-Dao Tran ◽  
...  
Keyword(s):  
Molecular Docking ◽  
In Silico ◽  
Biological Activities ◽  
Quantitative Structure Activity Relationship ◽  
2D Qsar ◽  
Study Results ◽  
High Yields ◽  
In Silico Models ◽  
Bace 1

Acetylcholinesterase (AChE) and beta-secretase (BACE-1) are two attractive targets in the discovery of novel substances that could control multiple aspects of Alzheimer’s disease (AD). Chalcones are the flavonoid derivatives with diverse bioactivities, including AChE and BACE-1 inhibition. In this study, a series of N-substituted-4-phenothiazine-chalcones was synthesized and tested for AChE and BACE-1 inhibitory activities. In silico models, including two-dimensional quantitative structure–activity relationship (2D-QSAR) for AChE and BACE-1 inhibitors, and molecular docking investigation, were developed to elucidate the experimental process. The results indicated that 13 chalcone derivatives were synthesized with relatively high yields (39–81%). The bioactivities of these substances were examined with pIC50 3.73–5.96 (AChE) and 5.20–6.81 (BACE-1). Eleven of synthesized chalcones had completely new structures. Two substances AC4 and AC12 exhibited the highest biological activities on both AChE and BACE-1. These substances could be employed for further researches. In addition to this, the present study results suggested that, by using a combination of two types of predictive models, 2D-QSAR and molecular docking, it was possible to estimate the biological activities of the prepared compounds with relatively high accuracy.

scholarly journals Glycosylated Flavonoids from Psidium guineense as Major Inhibitors of HIV-1 Replication in vitro

2017 ◽  
Vol 12 (7) ◽  
pp. 1934578X1701200
Author(s):  
Joseph T Ortega ◽  
Omar Estrada ◽  
Maria L Serrano ◽  
Whendy Contreras ◽  
Giovannina Orsini ◽  
...  
Keyword(s):  
Antiviral Activity ◽  
Reverse Transcriptase ◽  
In Silico ◽  
Biological Activities ◽  
In Silico Prediction ◽  
Flavonoid Quercetin ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Hiv 1

Flavonoids are present in practically all plants and many biological activities have been described for them. The flavonoid quercetin is a common molecule for which anti-HIV activity has been demonstrated. Avicularin and guajaverin are derivatives of quercetin with a glycoside substituent in their structure. In this work, a mixture of both derivatives was purified from an extract of Psidium guinense. The mixture exhibited activity against HIV-1 in vitro, with an IC50 of approximately 8.5 μg/mL, which compares favorably with the IC50 of 53 μg/mL of quercetin. The mixture also inhibited HIV-1 reverse transcriptase (RT), with an IC50 of 7.2 μM, compared to 0.6 μM for quercetin. These results are in agreement with the in silico prediction for the interaction of these flavonoids with RT and suggest that the glycosylic moiety could favor the transport of the compound into the cell. However, the glycosidic moiety might be cleaved intracellularly, being the resultant quercetin responsible for the antiviral activity.

Extraction, isolation and characterization of Bauhinia variegata flower

2020 ◽  
pp. 9-12
Author(s):  
Akanksha Gupta ◽  
Abhishek K Tripathi ◽  
Pushpraj S Gupta
Keyword(s):  
Biological Activities ◽  
Molecular Formula ◽  
Native Plant ◽  
Compound A ◽  
Active Constituents ◽  
Chromatographic Techniques ◽  
Isolation And Characterization ◽  
Soxhlet Apparatus ◽  
Bauhinia Variegata

Background: Bauhinia variegata Linn. is a native plant of Asia and China. B. variegata is found in tropical regions of the world. It belongs to family Leguminosae. It is used for diarrhea, hemorrhoids, constipation, piles, edema, leprosy, wounds, tumors, etc.  Objective: The objective of the present study was to perform extraction of B. variegata flower and isolation of active constituents from the extract. Materials and Methods: The ethanolic extraction of B. variegata flower was performed using the Soxhlet apparatus. The isolation of active constituents from the extract was performed using chromatographic techniques. In column chromatographic studies, n-hexane- [dichloromethane (DCM)] (2:8) was used as an eluting system and further purified through thin layer chromatography (TLC). Compound A and B were isolated through chromatographic techniques, then the molecular formula and characterization of these compounds were carried out with mass and infrared (IR) spectral analysis. Results and Discussion: The percentage yield of B. variegata ethanolic extract (BVE) was found to be 20.8% w/w. The different fractions were F1 having 12.5 grams with n-hexane, F2 (17.1 grams) with CH2Cl2, F3 (21.2 grams) with EtOAc, and F4 (13.4 grams) with EtOH. Compound A and B were isolated from the solvent fractions of n-hexane-DCM (2:8) and EtOAc-DCM (1:9), respectively. The compound A was characterized as 3-hydroxy-6-methoxy-2-phenyl-4H-chromen-4-one. The compound B was characterized as 3-hydroxy-6-methyl-2-phenyl-4H-chromen-4-one. Conclusion: Thus, B. variegata flowers possess active components that need to identify their biological activities.

Synthesis, characterization and biological activities of 1,3,4-oxadiazole derivatives of nalidixic acid and their copper complexes

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Nalidixic Acid ◽  
Copper Complexes ◽  
Biological Activities ◽  
Bidentate Coordination ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Oxadiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
Derivatives Of ◽  
Substituted 1

A series of novel 1, 3, 4-oxadiazole analogues was synthesized from cyclization of hydrazones of substituted 1-ethyl-1,4-dihydro-7-methyl-4-oxo-1,8-naphthyridine-3-carbohydrazides were prepared from nalidixic acid. The structures of synthesized oxadiazole derivatives and their copper complexes were elucidated on the basis of FTIR, elemental analyses, 1H-NMR and atomic absorption spectral analysis. It was observed from spectral data that metal ligand ratio was 1:1 in all copper complexes and they were bidentate, coordination was found to be done through oxygen of 4-oxo group and nitrogen of oxadiazole ring. The synthesized compounds were further evaluated with biological activities and compared with parent hydrazones. Copper complexes possess antibacterial and antifungal activities better than the oxadiazoles while they have better antioxidant activity then copper complexes. Parent hydrazones were better in all biological activities than synthesized oxadiazoles.

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