SYNTHESIS OF 1,3-THIAZOLE DERIVATIVES

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (01) ◽  
pp. 7-19
Author(s):  
Rebaz Omar ◽  
◽  
Pelin Koparir ◽  
Metin Koparir ◽  
Keyword(s):  
Nitrogen Atom ◽  
Drug Design ◽  
Drug Development ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Thiazole Derivatives ◽  
Anti Cancer ◽  
Drug Synthesis ◽  
Anti Oxidant ◽  
Anti Hiv

Many heterocyclic compounds containing nitrogen atom are used in drug development. Thiazole is one of the most important heterocyclic compounds in drug design, which contains sulfur and nitrogen atom. Different site reactions in thiazole compounds extend to new drug synthesis and plays an important role in medicinal chemistry. Thiazole and derivatives are found to possess widely biological activities such as anti-inflammatory, anti-diabetic, anti-microbial, anti-cancer, anti-consulsant, anti-HIV, anti-hypertensive, anti-Alzheimer, anti-oxidant and anthelmintic. The aim of this review is to corroborate procedures which are available for the synthesis 1,3-thiazole derivatives

N-heterocycles: Recent advances in biological applications

2021 ◽  
Vol 19 ◽  
Author(s):  
Monica Dinodia
Keyword(s):  
Structural Design ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Review Article ◽  
Biological Applications ◽  
Pharmacological Activities ◽  
Physiological Properties ◽  
Anti Cancer ◽  
Anti Hiv ◽  
Depth View

Abstract: Nitrogen based heterocycles display an impressive repertoire of biological activities, including antioxidant, antimicrobial, anti-tuberculosis, analgesic, anti-inflammatory, anti-viral, anti-HIV, anti-cancer, anti-helminthic, and other pharmacological activities. Numerous novel nitrogen-based heterocycles have been synthesized, which showed various physiological properties, and their application in medicinal chemistry is ever-growing. The present review will provide an in-depth view of N-heterocyclic compounds that showed biological activities in the last 5 years (2017-2021). This review article will be helpful for the structural design of effective and sustainable N-heterocyclic drugs against diseases with minimal side effects.

1,4-Dihydropyridine: A Dependable Heterocyclic Ring with the Promising and the Most Anticipable Therapeutic Effects

2019 ◽  
Vol 19 (15) ◽  
pp. 1219-1254 ◽  
Author(s):  
Abhinav Prasoon Mishra ◽  
Ankit Bajpai ◽  
Awani Kumar Rai
Keyword(s):  
Calcium Ion ◽  
Heterocyclic Compounds ◽  
Channel Blocker ◽  
Heterocyclic Ring ◽  
Therapeutic Effects ◽  
Voltage Gated ◽  
Therapeutic Benefits ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Synthetic Medicinal

: Nowadays, heterocyclic compounds act as a scaffold and are the backbone of medicinal chemistry. Among all of the heterocyclic scaffolds, 1,4-Dihydropyridine (1,4-DHP) is one of the most important heterocyclic rings that possess prominent therapeutic effects in a very versatile manner and plays an important role in synthetic, medicinal, and bioorganic chemistry. The main aim of the study is to review and encompass relevant studies related to 1,4-DHP and excellent therapeutic benefits of its derivatives. An extensive review of Pubmed-Medline, Embase and Lancet’s published articles was done to find all relevant studies on the activity of 1,4-DHP and its derivatives. 1,4-DHP is a potent Voltage-Gated Calcium Channel (VGCC) antagonist derivative which acts as an anti-hypertensive, anti- anginal, anti-tumor, anti-inflammatory, anti-tubercular, anti-cancer, anti-hyperplasia, anti-mutagenic, anti-dyslipidemic, and anti-ulcer agent. From the inferences of the study, it can be concluded that the basic nucleus, 1,4-DHP which is a voltage-gated calcium ion channel blocker, acts as a base for its derivatives that possess different important therapeutic effects. There is a need of further research of this basic nucleus as it is a multifunctional moiety, on which addition of different groups can yield a better drug for its other activities such as anti-convulsant, anti-oxidant, anti-mutagenic, and anti-microbial. This review would be significant for further researches in the development of several kinds of drugs by representing successful matrix for the medicinal agents.

A review on phyto-pharmacology of Oxalis corniculata

2021 ◽  
Vol 24 ◽  
Author(s):  
Iqra Sarfraz ◽  
Azhar Rasul ◽  
Ghulam Hussain ◽  
Muhammad Ajmal Shah ◽  
Bushra Nageen ◽  
...  
Keyword(s):  
Clinical Trials ◽  
Biological Activities ◽  
Chemical Constituents ◽  
Current Effort ◽  
Isolation And Characterization ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Anti Fungal ◽  
Warm Temperate

: Oxalis corniculata (Oxalidaceae) is a small decumbent and delicate appearing medicinal herb flourishing in warm temperate and tropical domains such as Pakistan and India. Main bioactive chemical constituents of Oxalis plant include several alkaloids, flavonoids, terpenoids, cardiac glycosides, saponins, phlobatannins along with steroids. Due to its polyphenolic, glycosides and flavonoid profile, it is proved to be protective in numerous ailments and exhibit various biological activities such as anti-fungal, anti-cancer, anti-oxidant, anti-bacterial, anti-diabetic, and cardioprotective. Moreover, bioactive phytochemicals from this plant possess significant wound healing potential. Our current effort intends to emphasize on the immense significance of this plant species, which have not been the subject matter of clinical trials and effective pharmacological studies, even though its favored usage has been stated. This review proposes that Oxalis corniculata possess potential for the cure of various diseases, however, further researches on isolation and characterization of bioactive compounds along with pre-clinical trials are compulsory to figure out its pharmacological applications.

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.

scholarly journals REVIEW: Organosulphure compound of garlic (Allium sativum L.) and its biological activities

2003 ◽  
Vol 1 (2) ◽  
pp. 65-76 ◽  
Author(s):  
UDHI EKO HERNAWAN ◽  
AHMAD DWI SETYAWAN
Keyword(s):  
Platelet Aggregation ◽  
Side Effects ◽  
Allium Sativum ◽  
Urinary Infection ◽  
Biological Activities ◽  
Bioactive Compound ◽  
Traditional Medicines ◽  
Anti Cancer ◽  
Long Time ◽  
Anti Oxidant

Garlic has been used a long time ago as traditional medicines. The valuable bulb is used to treat hypertension, respiratory infection, headache, hemorrhoids, constipation, bruised injury or slice, insomnia, cholesterol, influenza, urinary infection, etc. Garlic bulbs can be used as anti-diabetic, anti-hypertension, anti-cholesterol, anti-atheroschlerosis, anti-oxidant, anti-cell platelet aggregation, fibrinolyse spur, anti-viral, anti-microbial, and anti-cancer. The ultimate bioactive compound of garlic is organo-sulphure components, i.e. alliin, allicin, ajoene, allyl sulphide groups, and allyl cystein. There was not any report of any side effects or toxicity of garlic.

An Introduction to the Basic Concepts in QSAR-Aided Drug Design

2015 ◽  
pp. 1-47 ◽  
Author(s):  
Maryam Hamzeh-Mivehroud ◽  
Babak Sokouti ◽  
Siavoush Dastmalchi
Keyword(s):  
Drug Design ◽  
Drug Development ◽  
Biological Activities ◽  
Model Development ◽  
Quantitative Structure Activity Relationship ◽  
Molecular Structures ◽  
New Drugs ◽  
Qsar Modeling ◽  
Qsar Studies ◽  
Modern Drug

The need for the development of new drugs to combat existing and newly identified conditions is unavoidable. One of the important tools used in the advanced drug development pipeline is computer-aided drug design. Traditionally, to find a drug many ligands were synthesized and evaluated for their effectiveness using suitable bioassays and if all other drug-likeness features were met, the candidate(s) would possibly reach the market. Although this approach is still in use in advanced format, computational methods are an indispensable component of modern drug development projects. One of the methods used from very early days of rationalizing the drug design approaches is Quantitative Structure-Activity Relationship (QSAR). This chapter overviews QSAR modeling steps by introducing molecular descriptors, mathematical model development for relating biological activities to molecular structures, and model validation. At the end, several successful cases where QSAR studies were used extensively are presented.

An Introduction to the Basic Concepts in QSAR-Aided Drug Design

Oncology ◽  
2017 ◽  
pp. 20-66
Author(s):  
Maryam Hamzeh-Mivehroud ◽  
Babak Sokouti ◽  
Siavoush Dastmalchi
Keyword(s):  
Drug Design ◽  
Drug Development ◽  
Biological Activities ◽  
Model Development ◽  
Quantitative Structure Activity Relationship ◽  
Molecular Structures ◽  
New Drugs ◽  
Qsar Modeling ◽  
Qsar Studies ◽  
Modern Drug

The need for the development of new drugs to combat existing and newly identified conditions is unavoidable. One of the important tools used in the advanced drug development pipeline is computer-aided drug design. Traditionally, to find a drug many ligands were synthesized and evaluated for their effectiveness using suitable bioassays and if all other drug-likeness features were met, the candidate(s) would possibly reach the market. Although this approach is still in use in advanced format, computational methods are an indispensable component of modern drug development projects. One of the methods used from very early days of rationalizing the drug design approaches is Quantitative Structure-Activity Relationship (QSAR). This chapter overviews QSAR modeling steps by introducing molecular descriptors, mathematical model development for relating biological activities to molecular structures, and model validation. At the end, several successful cases where QSAR studies were used extensively are presented.

Phytochemical and pharmacological aspects of Nothapodytes nimmoniana. An overview

2013 ◽  
Vol 59 (1) ◽  
pp. 53-66 ◽  
Author(s):  
Nazeerullah Khan ◽  
Ennus Tajuddin Tamboli ◽  
V.K. Sharma ◽  
Sunil Kumar
Keyword(s):  
Wide Spectrum ◽  
Pharmacological Activities ◽  
Nothapodytes Nimmoniana ◽  
Jammu And Kashmir ◽  
Medicinal Uses ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Anti Fungal ◽  
Anti Hiv ◽  
Important Medicinal Plant

Summary Nothapodytes nimmoniana (J. Graham) (Icacinaceae), commonly known as Amruta is found in India particularly in Maharashtra, Goa, Kerala, Assam, Jammu and Kashmir as well as Tamilnadu areas. It is an important medicinal plant, the major source of a potent alkaloid, namely camptothecin, of a wide spectrum of pharmacological activities like anti-cancer, anti-HIV, antimalarial, antibacterial, anti-oxidant, anti-inflammatory, anti-fungal and also applied in the treatment of anaemia. Camptothecin is still not synthesized, therefore, its production entirely depends on natural sources. N. nimmoniana is one such plant which yields contain camptothecin in significantly high amount. The plant is gaining international recognition due to its diversified medicinal uses. It is subjected to excessive harvest. It has been categorized as a vulnerable and endangered plant. The present review encompasses the phytochemical, analytical, pharmacological, biotechnological, and other specific aspects of N. nimmoniana.

scholarly journals Biological Potential and Chemical Properties of Pyridine and Piperidine Fused Pyridazine Compounds: Pyridopyridazine a Versatile Nucleus

2016 ◽  
Vol 1 (1) ◽  
pp. 29 ◽  
Author(s):  
Mohammad Asif
Keyword(s):  
Nitrogen Atom ◽  
Structural Feature ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Chemical Properties ◽  
Pharmacological Properties ◽  
Drug Molecules ◽  
Biological Potential ◽  
Different Types ◽  
And Chemical Properties

Pyridopyridazine compounds are important nitrogen atom containing heterocyclic compounds due to their pharmacological versatility. This heterocycle system characterized a structural feature for different types of bioactive compounds that exhibiting various types of biological activities which make it an attractive scaffold for the design and development of new drug molecules. This article provided information about the pharmacological properties of pyridopyridazines derivatives.

An Overview on Pyranocoumarins: Synthesis and Biological Activities

2020 ◽  
Vol 23 (24) ◽  
pp. 2679-2721 ◽  
Author(s):  
Evangelia-Eirini N. Vlachou ◽  
Konstantinos E. Litinas
Keyword(s):  
Organic Compounds ◽  
Antifungal Agents ◽  
Biological Activities ◽  
Biological Properties ◽  
Pyran Ring ◽  
Naturally Occurring ◽  
Anti Cancer ◽  
Anti Inflammatory ◽  
Antibacterial And Antifungal ◽  
Anti Hiv

Pyrano- and dipyranocoumarins are classes of naturally occurring organic compounds with very interesting biological activities. This review focuses on the synthetic strategies for the synthesis of pyranocoumarins and dipyranocoumarins and the biological properties of those compounds. The synthesis involves the formation of the pyran ring, at first, from a coumarin or the formation of pyranone moiety from an existing pyran. Pyranocoumarins and dipyranocoumarins present anti-HIV, anti-cancer, neuroprotective, antidiabetic, antibacterial, antifungal, anti-inflammatory activities. Especially khellactones and calanolides are usually potent and selective in anti-HIV activity. Decursin and decursinol derivatives are effective as anticancer, neuroprotective, antidiabetic, antibacterial, and antifungal agents.

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