An Insight into the Synthesis and SAR of 2,4-Thiazolidinediones (2,4-TZD) as Multifunctional Scaffold: A Review

2020 ◽  
Vol 20 (4) ◽  
pp. 308-330 ◽  
Author(s):  
Navjot Singh Sethi ◽  
Deo Nandan Prasad ◽  
Rajesh Kumar Singh
Keyword(s):  
Antioxidant Activities ◽  
Structural Information ◽  
Biological Activities ◽  
Low Cost ◽  
Pharmacological Activities ◽  
Strategic Design ◽  
Lead Compounds ◽  
Privileged Scaffold ◽  
Synthetic Routes ◽  
Insight Into

2,4-Thiazolidinedione (2,4-TZD) is a versatile pharmacophore, a privileged scaffold, and a remarkable sulphur-containing heterocyclic compound with diverse pharmacological activities. The multifarious biological activities, due to different mechanisms of action, low cost, and easy availability of 2,4-TZD impressed medicinal chemists to integrate this moiety to develop various lead compounds with diverse therapeutic actions. This resulted in the swift development in the last decade for generating different new potential molecules bearing 2,4-TZD. In this review, the authors attempt to shape and present the latest investigations (2012 onwards) going on in generating promising 2,4-TZD containing lead compounds. The data has been collected and analyzed to develop the structure-activity relationship (SAR). The SAR and active pharmacophores of various leads accountable for antidiabetic, anticancer, antimicrobial, and antioxidant activities have also been illustrated. This review also highlighted some of the important chemical synthetic routes for the preparation of various 2,4-TZD derivatives. This review will definitely serve as a useful source of structural information to medicinal chemists and may be utilized for the strategic design of potent 2,4-TZD derivatives in the future.

scholarly journals Potential of Steroidal Alkaloids in Cancer: Perspective Insight Into Structure–Activity Relationships

2021 ◽  
Vol 11 ◽  
Author(s):  
Ying Huang ◽  
Gen Li ◽  
Chong Hong ◽  
Xia Zheng ◽  
Haiyang Yu ◽  
...  
Keyword(s):  
Chemical Structure ◽  
Structural Modification ◽  
Biological Activities ◽  
Chemical Properties ◽  
Steroidal Alkaloids ◽  
Pharmacological Activities ◽  
Structure Activity Relationships ◽  
Lead Compounds ◽  
Structure Activity ◽  
Insight Into

Steroidal alkaloids contain both steroidal and alkaloid properties in terms of chemical properties and pharmacological activities. Due to outstanding biological activities such as alkaloids and similar pharmacological effects to other steroids, steroidal alkaloids have received special attention in anticancer activity recently. Substituted groups in chemical structure play markedly important roles in biological activities. Therefore, the effective way to obtain lead compounds quickly is structural modification, which is guided by structure–activity relationships (SARs). This review presents the SAR of steroidal alkaloids and anticancer, including pregnane alkaloids, cyclopregnane alkaloids, cholestane alkaloids, C-nor-D-homosteroidal alkaloids, and bis-steroidal pyrazine. A summary of SAR can powerfully help to design and synthesize more lead compounds.

scholarly journals Chemical Diversity and Biological Activity of Secondary Metabolites from Soft Coral Genus Sinularia since 2013

Marine Drugs ◽  
2021 ◽  
Vol 19 (6) ◽  
pp. 335
Author(s):  
Xia Yan ◽  
Jing Liu ◽  
Xue Leng ◽  
Han Ouyang
Keyword(s):  
Biological Activity ◽  
Secondary Metabolites ◽  
Coral Species ◽  
Soft Coral ◽  
Biological Activities ◽  
Vital Role ◽  
Chemical Diversity ◽  
Pharmacological Activities ◽  
Lead Compounds ◽  
Coral Genus

Sinularia is one of the conspicuous soft coral species widely distributed in the world’s oceans at a depth of about 12 m. Secondary metabolites from the genus Sinularia show great chemical diversity. More than 700 secondary metabolites have been reported to date, including terpenoids, norterpenoids, steroids/steroidal glycosides, and other types. They showed a broad range of potent biological activities. There were detailed reviews on the terpenoids from Sinularia in 2013, and now, it still plays a vital role in the innovation of lead compounds for drug development. The structures, names, and pharmacological activities of compounds isolated from the genus Sinularia from 2013 to March 2021 are summarized in this review.

scholarly journals A Mini-Review on the Phytochemistry and Biological Activities of Selected Apocynaceae Plants

2019 ◽  
Author(s):  
Abiche Ekalu ◽  
Rachael Gbekele-Oluwa Ayo ◽  
Habila D. James ◽  
Ibrahim Hamisu
Keyword(s):  
Cardiac Glycosides ◽  
Biological Activities ◽  
Nerium Oleander ◽  
Pharmacological Activities ◽  
Alstonia Scholaris ◽  
Thevetia Peruviana ◽  
Carissa Carandas ◽  
Wrightia Tinctoria ◽  
Insight Into

This review aims at studying the phytochemistry and biological activities of some selected Apocynaceae plants. Eleven members of this family were reviewed for their phytochemistry and biological activities. Interestingly, the commonly isolated compounds reported from Mondia whitei (Hook.f.) Skeels, Secondatia floribunda A. DC, Carissa carandas, Tabernaemontana divaricate, Nerium oleander, Wrightia tinctoria, T. divaricate, Alstonia scholaris, Carrisa spinarum Linn, Thevetia peruviana and Caralluma lasiantha were triterpenoids, flavonoids, phytosterols, cardiac glycosides and lignans. All of them exhibited remarkable biological activities, mostly similar to each other. This review provides a detailed insight into the pharmacological activities of these selected members of this family.

Benzofuran: A Key Heterocycle - Ring Closure And Beyond

2020 ◽  
Vol 17 (3) ◽  
pp. 224-276
Author(s):  
Andiappan Lavanya ◽  
Kilambi Narasimhan ◽  
Vediappen Padmini
Keyword(s):  
Biological Activities ◽  
Extraction Process ◽  
Ring Closure ◽  
Pharmacological Activities ◽  
Naturally Occurring ◽  
Synthetic Materials ◽  
Privileged Scaffold ◽  
Medicinal Properties ◽  
Anti Inflammatory ◽  
Anti Hiv

: The benzofuranyl motif present in compounds exhibits various medicinal properties and non-drug applications. These derivatives are naturally occurring compounds or synthetic materials, which cover a broad spectrum of pharmacological activities like anti-inflammatory, anti-diabetic, anti- depressant, anti-HIV, anti-microbial, anti-proliferative, anti-convulsant, cytotoxic, analgesic, etc. Few of the commercially interesting compounds from this class are, ailanthoidol (anti-inflammatory), amiodarone, dronedarone, celivarone (anti-arrhythmic), bufuralol (muscular airways relaxant), morphine, 5-(2-aminopropyl)benzofuran; 5-APB, 6-(2-aminopropyl)benzofuran; 6-APB (CNS), rifampicin (antibiotic), etc., whereas, some of the non-drug applications are in perfumery industry (bergapten) and as tannin activators in sunscreen preparations (psoralen, 8-methoxypsoralen, and angelicin). Considering these interesting biological activities and commercial utilities, a review on the synthetic aspects of this privileged scaffold was attempted. For the benefit of natural product-based drug discovery, available sources of these derivatives, extraction process and reported biological activities have also been outlined in this review.

Hydroxycinnamic Acids and Their Related Synthetic Analogs: An Update of Pharmacological Activities

2021 ◽  
Vol 21 ◽  
Author(s):  
Ayyoub Selka ◽  
Fanta J. Ndongou Moutombi ◽  
Jacques Jean-François ◽  
Mohamed Touaibia
Keyword(s):  
Antioxidant Activities ◽  
Biological Activities ◽  
Hydroxycinnamic Acid ◽  
Hydroxycinnamic Acids ◽  
Pharmacological Activities ◽  
Synthetic Analogs ◽  
Anti Cancer ◽  
Anti Inflammatory

: The hydroxycinnamic acid scaffold is extremely versatile with various biological activities. This review will highlight the progress of the biological activities of hydroxycinnamic acids and their related synthetic analogs, including recently reported anti-cancer, anti-inflammatory, and antioxidant activities.

Recent Advances in Transition Metal Free Synthetic Protocols for Quinoline Derivatives

2020 ◽  
Vol 24 (16) ◽  
pp. 1815-1852
Author(s):  
Rukhsana Tabassum ◽  
Muhammad Ashfaq ◽  
Hiroyuki Oku
Keyword(s):  
Transition Metal ◽  
Heterocyclic Compounds ◽  
Pharmaceutical Chemistry ◽  
Quinoline Derivatives ◽  
Metal Free ◽  
Substituted Quinolines ◽  
Privileged Scaffold ◽  
Synthetic Routes ◽  
Therapeutic Activities ◽  
Insight Into

The quinoline moiety is a privileged scaffold among heterocyclic compounds that is an important construction motif in the fields of pharmaceutical chemistry. Quinoline molecule possesses a variety of therapeutic activities like antiviral, antimalarial, antibacterial, antitumor, anticancer, antioxidant antihypertensive, antifungal, anthelmintic, cardiotonic, anticonvulsant and anti-inflammatory. This review provides an insight into recent development in transition metal free novel and modified conventional synthetic routes to yield a wide variety of substituted quinolines.

Recent Applications of Benzimidazole as a Privileged Scaffold in Drug Discovery

2020 ◽  
Vol 20 ◽  
Author(s):  
Yongzhen Guo ◽  
Xuben Hou ◽  
Hao Fang
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Anticancer Agents ◽  
Medicinal Chemistry ◽  
Biological Activities ◽  
Great Influence ◽  
Parasitic Infections ◽  
Peptic Ulcers ◽  
Lead Compounds ◽  
Privileged Scaffold

: Benzimidazole is an aromatic bicyclic heterocycle that is regarded as a valuable privileged scaffold in medicinal chemistry. Many marketed drugs and natural products containing benzimidazole scaffolds exert great influence in fighting various diseases, such as hypertension, peptic ulcers, parasitic infections, and cancer. In this review, we introduce the pharmacological applications of some marketed drugs and lead compounds with a focus on anticancer agents, reporting the corresponding data to show the biological activities at their targets. The publications in this review encompass those from 2014 to 2019.

Recent Advances in Transition Metal Mediated Synthetic Approaches to Quinoline Derivatives

2020 ◽  
Vol 17 ◽  
Author(s):  
Rukhsana Tabassum ◽  
Muhammad Ashfaq ◽  
Hiroyuki Oku
Keyword(s):  
Transition Metal ◽  
Heterocyclic Compounds ◽  
Therapeutic Agent ◽  
Biological Activities ◽  
Quinoline Derivatives ◽  
Quinoline Ring ◽  
Pharmacological Activities ◽  
Synthetic Routes ◽  
Synthetic Approaches ◽  
Significant Attention

Abstract:: Synthesis of heterocyclic compounds containing quinoline scaffold attracted a significant attention of organic chemists due to their importance as therapeutic agent in pharmaceutical industry. Quinolone molecule exhibit extensive biological activities a few of which are antiviral, anti-inflammatory antibacterial, antifungal, antiproliferative, anthelmintic and anticonvulsant. A variety of synthetic routes has been developed for construction compounds bearing quinoline nucleus due to its broad spectrum of pharmacological activities. This review describes recent development in transition metal mediated synthetic protocols of these important heterocycles by formation of quinoline ring or by substitution of quinoline rings including both modified conventional name reactions and novel routes with highly functionalized quinoline products.

scholarly journals Therapeutic potential of oxadiazole or furadiazole containing compounds

BMC Chemistry ◽  
2020 ◽  
Vol 14 (1) ◽  
Author(s):  
Ankit Siwach ◽  
Prabhakar Kumar Verma
Keyword(s):  
Therapeutic Potential ◽  
Biological Activities ◽  
Antiviral Drug ◽  
Biological Properties ◽  
New Drugs ◽  
Pharmacological Activities ◽  
Methylene Groups ◽  
Synthetic Routes ◽  
Azole Ring ◽  
Derivatives Of

AbstractAs we know that, Oxadiazole or furadi azole ring containing derivatives are an important class of heterocyclic compounds. A heterocyclic five-membered ring that possesses two carbons, one oxygen atom, two nitrogen atoms, and two double bonds is known as oxadiazole. They are derived from furan by the replacement of two methylene groups (= CH) with two nitrogen (-N =) atoms. The aromaticity was reduced with the replacement of these groups in the furan ring to such an extent that it shows conjugated diene character. Four different known isomers of oxadiazole were existed such as 1,2,4-oxadiazole, 1,2,3-oxadiazole, 1,2,5-oxadiazole & 1,3,4-oxadiazole. Among them, 1,3,4-oxadiazoles & 1,2,4-oxadiazoles are better known and more widely studied by the researchers due to their broad range of chemical and biological properties. 1,3,4-oxadiazoles have become important synthons in the development of new drugs. The derivatives of the oxadiazole nucleus (1,3,4-oxadiazoles) show various biological activities such as antibacterial, anti-mycobacterial, antitumor, anti-viral and antioxidant activity, etc. as reported in the literature. There are different examples of commercially available drugs which consist of 1,3,4-oxadiazole ring such as nitrofuran derivative (Furamizole) which has strong antibacterial activity, Raltegravir as an antiviral drug and Nesapidil drug is used in anti-arrhythmic therapy. This present review summarized some pharmacological activities and various kinds of synthetic routes for 2, 5-disubstituted 1,3,4-oxadiazole, and their derived products.

scholarly journals A mini-review on the phytochemistry and biological activities of selected Apocynaceae plants

2019 ◽  
Vol 8 (4) ◽  
pp. 269-273 ◽  
Author(s):  
Abiche Ekalu ◽  
Rachael Gbekele-Oluwa Ayo ◽  
James Dama Habila ◽  
Ibrahim Hamisu
Keyword(s):  
Cardiac Glycosides ◽  
Biological Activities ◽  
Nerium Oleander ◽  
Pharmacological Activities ◽  
Alstonia Scholaris ◽  
Thevetia Peruviana ◽  
Carissa Carandas ◽  
Wrightia Tinctoria ◽  
Insight Into

This review aims at studying the phytochemistry and biological activities of some selected Apocynaceae plants. Eleven members of this family were reviewed for their phytochemistry and biological activities. Interestingly, the commonly isolated compounds reported from Mondia whitei (Hook.f.) Skeels, Secondatia floribunda A. DC, Carissa carandas, Tabernaemontana divaricate, Nerium oleander, Wrightia tinctoria, Tabernaemontana divaricate, Alstonia scholaris, Carrisa spinarum Linn, Thevetia peruviana and Caralluma lasiantha were triterpenoids, flavonoids, phytosterols, cardiac glycosides and lignans. All of them exhibited remarkable biological activities, mostly similar to each other. This review provides a detailed insight into the pharmacological activities of these selected members of this family.

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