The outbreak of novel coronavirus disease (COVID-19) caused by SARS-CoV-2 poses a serious threat to human health and world economic activity. There is no specific drug for the treatment COVID-19 patients at this moment. Traditionally, people have been using spices like ginger, fenugreek onion, etc. remedy common cold. This work identifies potential inhibitors main protease (Mpro) spike (S) receptor from 10 readily available spices. These two proteins, S Mpro, play an important role during...

Abstract Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) is highly pathogenic to humans and has created health care threats worldwide. This urgent situation focused the researchers worldwide towards development of novel vaccine or small molecule therapeutics for SARS-CoV-2. Although several vaccines have already been discovered are in use masses, no therapeutic medication yet approved by FDA treatment COVID-19. Keeping this view, present study, we identified promising hits...

Nitrogen heterocycles are widespread in nature and their applications bioactive pharmaceuticals, agrochemicals functional materials well known. A number of protocols have been developed for syntheses. This review article covers an updated (published during 2005-2008) summary transition metal-catalyzed approaches the syntheses five- six-membered ring with one nitrogen atom via carbon-nitrogen bond forming reactions. The five-membered include pyrroles, pyrrolidines, indoles, oxindoles,...

Abstract In this work an efficient tandem process transforming N ‐substituted amidines into secondary amides has been described. The involves ‐acylurea formation by reaction of the substrate with bis(acyloxy)(phenyl)‐λ 3 ‐iodane followed isocyanate elimination. periodinane reagents are obtained from commercially available phenyliodine(III) diacetate [PhI(OAc) 2 , (PIDA)] ligand exchange carboxylic acids. amidine substrates easily synthesized readily nitriles. method is applicable for amide...

Coronavirus disease 2019 (COVID-19) has created a global human health crisis and economic setbacks. Lack of specific therapeutics limited treatment options against COVID-19 become new challenge to identify potential hits in order develop therapeutics. One the crucial life cycle enzymes SARS-CoV-2 is main protease (Mpro), which plays major role mediating viral replication, makes it an attractive drug target. Virtual screening three times repeated 100 ns molecular dynamics simulation best were...

This review describes the synthesis of five-and six-membered oxygen heterocycles through carbon-oxygen bond formation by metal catalyzed heterocyclization published during 2005 to 2008.CONTENTS Pd(CF 3 CO 2 ) (10 mol%) BQ (4 equiv), L-1-(20 MeOH, 60 0 C, 24 h L-1 67-92%, 53-98% ee: OMe

The recently emerged 2019 Novel Coronavirus (SARS-CoV-2) and associated COVID-19 disease cause serious or even fatal respiratory tract infection. Observing the spread, illness death caused by COVID-19, World Health Organization (WHO) declared a pandemic. To date, there is no approved therapeutics effective treatment available to combat outbreak. This urgent situation pressing world respond with development of novel vaccine small molecule for SARS-CoV-2. In line these efforts, structure...

Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) is highly pathogenic to humans and has created an unprecedented global health care threat. Globally, intense efforts are going on discover a vaccine or new drug molecules control the COVID-19. However, till today, there no effective therapeutics treatment available for In this study, we aim find out potential small molecule inhibitors SARS-CoV-2 main protease (Mpro) from known DrugBank database version 5.1.8. We applied...

Intramolecular CH arylation of pyrone, pyridone, uracil, imidazole, and benzimidazole derivatives are carried out in the presence a Pd catalyst to form potentially bioactive fused heterocyclic compounds, whereas n-Bu 3 SnH-mediated aryl radical cyclization precursors afforded mainly halogen-reduced uncyclized products.Key words: Pd(0) catalyst, arylation, intramolecular cyclization, regioselectivity.

: C-N bond formation reactions are the most important transformations in (bio)organic chemistry because of widespread occurrence amines pharmaceuticals, natural products, and biologically active compounds. The Hofmann rearrangement is a well-known method used for preparation primary from amides. But, traditional version often gave relatively poor yields due to over-oxidation or solubility some amides aqueous base, created an enormous amount waste products. Developments over last two decades,...

The preparation of a variety tetracyclic ring systems by palladium(0)-catalyzed cyclization 2-bromobenzyloxy-substituted coumarins and quinolones is described. process has been found to be viable method for regioselective synthesis the corresponding products in very good excellent yield.

Abstract The article describes the use of a fullerene (C 60 )‐β‐cyclodextrin conjugate, synthesized via 1,3 ‐ dipolar cycloaddition, for ultrasensitive electrochemical detection p‐ nitrophenol. This conjugate was successfully immobilized on surface glassy carbon electrode and developed device showed high activity towards nitrophenol due to synergetic effect C , latter becoming highly conductive upon reduction. determination performed by using square wave voltammetry over concentration range...

Background: Amide bond formation reactions are the most important transformations in (bio)organic chemistry because of widespread occurrence amides pharmaceuticals, natural products and biologically active compounds. The Beckmann rearrangement is a well-known method used for preparation secondary from ketoximes. But, traditional protocols create enormous amount wastes. Thus, atom economical synthesis has got high priority among chemists. However, under classical conditions, aldoximes do not...

Heterocyclic compounds are versatile building blocks in organic synthesis. These important part various natural products and bioactive compounds. Several methodologies have been developed to synthesize these heterocyclic This review article covers an updated (published during 2005 2008) summary of transition-metal catalyzed approaches for the syntheses commonring heterocycles containing more than one heteroatom via selective formation carbon-heteroatom bonds. The five-membered ring with two...

Abstract Fused pyrimidines scaffolds such as pyrimidopyrimidines, purines and xanthines are important structural motifs found in various natural products drug molecules. They used anticancer, antiviral, antibacterial, antifungal, antioxidant, antitumor, anti‐diabetic, adenosine potentiating, hepatoprotective agents. Due to their diverse biological applications, the synthesis of has gained great importance among researchers recent years. Thus, present study aims review synthetic methodologies...

A new efficient route to the synthesis of benzannulated pyranoquinolines has been accomplished via palladium-catalyzed intramolecular aryl-aryl cross-coupling reactions. The coupling reactions proceeded smoothly under ligand-free conditions with catalytic system Pd(OAc)2/Cs2CO3/TBAB in high yields. Halogen-reduced product was not obtained optimum reaction conditions. Regioselective 5,6-dihydro-4H,8H-pyrido[3,2,1-de]phenanthridine is also described. In latter case, a pronounced effect base...

Abstract A novel and concise route towards the synthesis of pyrimido[4,5‐ d ]pyrimidines via a direct annulation reaction N ‐uracil amidines with benzaldehydes under transition metal free conditions has been described. The requisite precursors are obtained S AE on 6‐chlorouracil amidines. series synthesized in good to excellent yields by using Cs 2 CO 3 as base molecular oxygen oxidant t BuOH at 100 0 C. This synthetic protocol number advantages such as‐ operational simplicity, use green...