Shivaji Nivrutti Thore

Deogiri College · Department of Chemistry

A series of novel trans-3-substituted aminomethyl-5-(4-(4-chlorophenyl)cyclohexyl)-1,3,4-oxadiazole-2(3H)-thiones was synthesized successfully from achiral trans-4-(4-chlorophenyl)cyclohexane-1-carboxylic acid. To investigate their potential binding interactions with proteins at the active site, molecular docking studies were conducted using CDOCKE...

Herein, we report an efficient method to access difluoromethyl ethers of thiols and phenols using ethyl bromodifluoroacetate and K2CO3. This method demonstrates chemoselective difluoromethylation of thiols and phenols in the presence of amines. The current method also discloses the synthesis of bis(aryloxy)fluoromethane compounds which are least re...

Anhydrous copper sulfate is identified as a promoter for Knoevenagel condensation with surprising activity and excellent isolated yields. Low cost, easy availability and convenient to handle anhydrous copper sulfate was used to enhance the Knoevenagel condensation reaction by acting as a strong dehydrating agent. The developed protocol demonstrated...

An effective approach toward conversion of phenols to their benzene sulfonate esters by using N-fluorobenzenesufonimide (NFSI) and catalytic potassium fluoride is demonstrated. Mild reaction conditions, shorter reaction time, excellent yield and easy-to-handle reagents are the key features of the methodology. Mild reaction conditions have conferred...

Coronavirus disease 2019 (Covid-19) is caused by the Severe Acute Respiratory Syndrome-Corona Virus-2 (SARS-CoV-2) was firstly identified in the city of Wuhan of China in December 2019, which was spread and become a global issue due to its high transmission rate. To date, the outbreak of COVID-19 has resulted in infection to 150,356,672 people and...

A new series of thiazole compounds are synthesized and theirs anticancer activity was tested against breast cancer cells MCF7. The starting ethyl 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylate was alkylated by alkyl bromides in DMF. The resulted ethyl 4-methyl-2-(4-(alkyloxy)phenyl)thiazole-5-carboxylate compounds were refluxed with hydrazine h...

A one pot protocol for the transformation of aryl TBDMS ethers to corresponding benzene sulfonate esters using NFSI (N-flurobenzenesulfonimide)/KF is described. In situ generation of benzenesulfonyl fluoride directs chemoselective cleavage of aryl silyl ethers over alkyl silyl ethers. Electron withdrawing substituent’s on aryl ring provided better...

The adsorption behaviour of Acid red 1 onto Parthenium hysterophorus L from aqueous solution was investigated. Adsorption kinetics, equilibrium, and thermodynamics were investigated as a function of initial concentration and temperature. Three kinetic models-the pseudo first-order, second order and Elovich were used to investigate the adsorption me...

Synthesis of 2,4,5-trisubstituted imidazole compounds from an aromatic aldehyde, benzil and ammonium acetate is demonstrated using biodegradable lactic acid at 160 °C. This method is a simple, environmentally benign, and works for aromatic aldehyde containing electron donating and electron withdrawing groups. Graphic abstract Open image in new win...

One pot synthesis of 4-amino pyraneshave been achieved using ammoinium carbonate in aqueous ethanol system. The describe method is useful for the synthesis of pyranes using aromatic aldehydes, malononitrile and dimedone as three component reaction using conventional heating as well as microwave. The method provides simple and easy way for the synth...

Triethanolamine is an efficient and green catalyst for the synthesis of 6-amino-1, 4-dihydro-4-substituted-3-methylpyrano-[2, 3-c] pyrazole-5-carbonitrile in aqueous medium reflux conditions. The procedure is easier, eco friendly, simple with easy workup affording good yield of the corresponding products.

Knoevenagel condensation of pyrazole aldehydes with malononitrile is selectively carried out using ammonium carbonate as a mild, cheap, efficient and selective catalyst, in aqueous media at ambient temperature under sonication. This method is green and providing an expeditious way for Knoevenagel condensation of pyrazole aldehyde.

In the present work 4-aryl-6-(4-(pyrrolidin-1-yl)phenyl)pyrimidin-2-amine were synthesized by reacting chalcones with guanidine hydrochloride. The synthesized compounds were tested for antibacterial and antifungal activity.

4-(pyrrolidin-1-yl)benzaldehyde(1) was condensed with acetophenone to give chalcones (3a-3i) which are further cyclized with hydrazine hydrate to afford pyrazolines (4a-4i) by conventional and non-conventional route. The synthesized compounds were evaluated for antifungal and antibacterial activities.

Efflux inhibition is proven bacterial machinery responsible for removal of bacterial wastage including antibiotics. Recently, efflux inhibitors (EI) have been tested with encouraging results as an adjuvant therapy for treatment of tuberculosis (TB). Although, EI have emerged as innovative approach of treatment for multi drug resistant (MDR) & exten...

Triazolo[4,3-a]tetrahydrobenzo(b)thieno[3,2-e]pyrimidine-5(4H)-ones (5a-m) were synthesized and characterized by spectral analysis. All 13 derivatives were evaluated for central nervous system (CNS) depressant and skeletal muscle relaxant activities in Swiss albino mice. All the activities were compared with diazepam as a standard drug at a dose of...

In present work, adsorption experiments were carried out for the removal of Benzo Fast Scarlet from aqueous solutions using Parthenium L. The results have shown that, the amount of dye adsorption increases with increasing the initial concentration of the dye and temperature. The adsorption kinetic data were analysed by using various kinetic models....

A series of novel 3-aryl-2(4-(pyrrolidin-1-yl) phenyl) thiazolidin-4-ones has been synthesized and screened for antibacterial activity. From the synthesized compounds 4a, 4d and 4f show moderate antibacterial activity.

In this work we have synthesis Schiff bases and α-amino phosphonates by conventional and non-conventional methods. The one pot synthesis of α-amino phosphonates were also carried out by both the methods.

A practical and convenient procedure for the synthesis of 2-Aryl Benzimidazoles has been developed by reacting o-phenylenediamine with aromatic aldehydes in presence of 10 mol% sodium dodecyl sulphate in aqueous medium at room temperature in open air atmospheric condition with and without use of sonication

Ammonium nickel sulphate [(NH4)2SO4.NiSO4.6H2O] was found as a new catalyst to synthesis 2-aryl benzimidazole, 2-aryl benzothiazole and 2-aryl benzoxazole in aqueous media under sonication irradiation. The procedure is an eco-friendly, efficient and provides simple workup and good yield.

In the present study adsorption behavior of methylene blue and rhodamine B from aqueous solution using adsorbent prepared from “Hyptis suaveolens” (Vilayti Tulsi) was investigated as a function of parameters such as initial concentration, adsorbent dose, pH, contact time and temperature. The adsorption process was pH dependent. The thermodynamic pa...

A series of novel 5-methyl-2-phenylthiazole-4-substituted-heteroazole derivatives (6–15) have been synthesized. The structures of these compounds were established by IR, 1HNMR, Mass spectral data and elemental analyses. Compounds were evaluated for their anti-inflammatory and analgesic activities as well as gastric ulcerogenic effects. Derivatives...

A series of substituted thiazole derivatives (6–16) were synthesized to obtain new compounds with potential anti-inflammatory and analgesic activities. At equimolar oral doses, compounds 3-(piperidin-1-yl-methyl)-1, 3, 4-oxadiazol-2-thione (14), 5-amino-4-ethyl ester pyrazole (15), and 5-amino-3-phenylpyrazole derivatives (16) displayed anti-inflam...

A series of novel ethyl-5-amino-3-methylthio-1H-pyrazole-4-carboxylates 3a–j were synthesized from condensation of various hydrazides 2a–j with ketene dithioacetal. The synthesized compounds were screened for in vivo analgesic and anti-inflammatory activities using acetic acid writhing test in mice and carrageenan-induced paw edema test in rat, res...

Boric acid (10 mmol%) with TBAB (10 mmol%) in water was used as a catalyst for the synthesis of 2-arylsubstituted benzimidazoles efficiently. Simple and convenient procedure, easy purification and shorter reaction time are the advantageous features of this method.

A new series of 2-acetylphenyl 3,5-diflurobenzoates, 1-(3,5-difluorophenyl) -3-(2-hydroxyphenyl) propane-1,3-diones, 2-(3,5-difluorophenyl)-4H-chromen-4- ones and 2-(5-(3,5-difluorophenyl)-1H-pyrazol-3-yl) phenols have been synthesized and screened as antibacterial agents. In the series 3a, 4a, 4b, 4f, 4h exhibited moderate antibacterial activity a...

With the aim of developing potential H1-antihistaminic agents, a series of novel 2-substituted-3-carboxamido-4-oxo-4H-pyrimido[2,1-b][1,3]benzothiazole (8a–g) and 2-substituted-3-carboxamido-8-chloro-4-oxo-4H-pyrimido[2,1-b][1,3]benzothiazole (9a–g) were synthesized and evaluated in vitro for H1-antihistaminic activity on guinea pig ileum preparati...

Oxadiazoles (Ia), (Ib) and tetrazole derivatives (II) exhibit significant antiinflammatory activity.

This article explains an elementary concepts of wave function based quantum chemistry. First part devotes, the molecular Hamiltonian is specified and the Born Oppenheimer approximation is made. Later, the most important properties of electronic wave functions are discussed such as normalization, antisymmetry and inclusion of the electronic spin. Th...

The lithium bromide mediated condensation of 1-amino-2-heteroaryl substrates with ethyl cyanoformate, to obtain versatile alkylcarbamate protected benzoheteroazolones was studied. This unprecedented reaction could be used to furnish different azolones like 2-benzimidazolones, 2-benooxazolones and 2-amino-thiazoles in good yields. 2011 Bentham Scien...

A series of 4,5-dihydro-1,5-diaryl-1H-pyrazole-3-substituted-heteroazoles were designed and synthesized in order to obtain new compounds with potential anti-inflammatory activity. The title compounds were screened for in vivo anti-inflammatory activity by using Carrageenan induced rat paw edema method. Diclofenac sodium was used as a standard drug...

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

The first successful lithium bromide mediated solvent free condensation of arylenediamine and esters to obtain 2-substituted benzimidazole and imidazopyridine in good to excellent yields is described.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Various fluorine containing (42)-2-(4-fluorophenyl)-4-[(1 -phenyl-1Hoyrazol-4-yl)methylidene]5-(trifluoromethyl)-2,4-dihydro-3H-pyrazol-3- one 3a-e, (4E)-2-(4-fluorophenyl)-4-((4-oxo-3,4-dihydro2Hohromerh3-yl) methylidene]-5-(trifluoromethyl)-2,4-dihydro-3H-pyrazol-3-one 5a-e and (4E)-4-[(2chloroquinolin-3-yl)methylidene]-2-(4-fluorophenyl)-5-(trif...

The acid catalyzed cyclization of β-diketones gave chromones 6. The key step is esterification of acrylic acid with 2-hydroxyacetophenone to give ester 4. The structures of the products were confirmed by NMR, IR and mass spectral data.

Condensation of acetophenone with pyrazole aldehyde gave new series of fluorine and chlorine containing chalcones 3. Several pyrazolyl compounds were obtained using compounds 3. The structures of the compounds 3-7 were confirmed by NMR, IR and mass spectroscopy.

Different aryl isothiocyanates on reaction with acid hydrazides gave thiosemicarbazides. These thiosemicarbazides on treatment with conc H(2)SO(4) gave thiadiazoles. Their structures were confirmed by spectral analysis. The compounds synthesized were screened for their antibacterial activity against seven different organisms by using Agar Diffusion...

MgBr2 performs as a novel catalyst for the synthesis of various 1,5-benzodiazepine derivatives from wide range of substituted o-phenylenediamines and various ketones in good to excellent isolated yields (93–98%) using water as solvent at ambient temperature. Several solvents were examined for this reaction; however, in terms of reaction yield and t...

A series of triazolo[4,3-a]tetrahydrobenzo(b)thieno[3,2-e]pyrimidine-5(4H)-ones (12a-n) were synthesized and evaluated for CNS depressant, skeletal muscle relaxant and anticonvulsant activities by photoactometer, Rotarod and pentylenetetrazole induced the convulsions method respectively in Swiss albino mice. Diazepam was used as standard drug. The...

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Glyoxylic acid (5 mol%) performs as a novel highly water-soluble catalyst for the synthesis of 2-aryl-1-arylmethyl-1H-benzimidazoles from a wide range of substituted o-phenylenediamines and various substituted aldehydes in good to excellent isolated yields (85–95%) using water as solvent at ambient temperature. The remarkable advantages offered by...

magnified image A novel approach for the Aza‐Michael addition reactions between various amines and α,β‐unsaturated esters, nitriles and ketones using N‐donor Ligand catalyst (3 mol %) is described. The reactions are carried out in aqueous media at an ambient temperature to afford the products in excellent yields.

PdCl2, N-donor ligand and base mediated Suzuki coupling reaction of aryl halides and arylboronic acid in water are described. The corresponding Suzuki products were obtained in good to excellent yields.

The first successful Pd(OAc)2, N-donor ligand and base mediated Heck coupling reaction of aryl halides and alkenes in water is described. The corresponding Heck products were obtained in good to excellent yields.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.

Alum (KAl(SO4)2·12H2O) performs as a novel catalyst for the synthesis of 2-arylbenzothiazoles and 2-arylbenzoxazole from o-aminothiophenol and o-aminophenol with various substituted aldehydes in good to excellent isolated yields (85–95%) using water as a solvent at ambient temperature. Several solvents were examined for this reaction; however, in t...

Pyrimidine derivatives have received attention due to their applications in physiology(1,2) and derivatives of pyrimidine like phenobarbital, mysoline, etc. are well known in pharmacology. Various aminopyrimidmes were found effective as antimalarial(3) agents. Dihydropyridines(4) are known to exhibit anti hypertensive(5,6) properties. These finding...

A highly efficient, environmental friendly, palladium (11) catalyzed ligand promoted Suzuki reaction in aqueous phase was developed in short reaction time (4 - 5 h) at room temperature. The key for such a successful catalytic system was the use of suitable amount of co-solvent in the aqueous phase and reuse of palladium catalyst.

2,4-Bis-anilino-6-(2′-acetyl 4′-chlorophenyl phenyloxy)triazines have been converted into chalcones by condensing with aromatic aldehydes. These chalcones on treatment with hydrazine hydrate and hydroxyl amine hydrochloride give pyrazolines and isoxazolines respectively. The synthesized compounds have been tested for their antimicrobial activity.

The Mannich bases of the benzimidazoles were prepared by using formaldehyde and amino benzothiazoles in the presence of traces of conc. HCl. These prepared compounds were tested for their antibacterial activity against gram(+ve) and gram(-ve) bacteria. Some of the compounds show remarkable activity.

The benzimidazolin-2-thione and formaldehyde stirred and added substituted-2-amino. benzothiazole in presence of traces of conc. HCl and refluxed for 1 h. to give 1,3-bis-[substituted amino benzothiazolyl]-methyl benzimidazolin-2-thione(III) by Mannich reaction. The antiviral screenings of all compounds were studied against tobacco mosaic virus (TM...

Hydrazides of substituted 1,4-dihydropyridines have been synthesised by condensing substituted dihydropyridine dicarboxylic acid ester with hydrazine hydrate. The hydrazides on condensing with β-diketones and CS2/KOH give pyrazoles and oxadiazole 5-thiones respectively. The synthesised compounds were screened for antimicobial activity.

Hydrazides of substituted 1,4-dihydropyridines have been synthesised by condensing substituted dihydropyridine dicarboxylic acid ester with hydrazine hydrate. Hydrazides were condensed with different aromatic aldehydes to give different Schiff bases. These schiff bases on treatment with chloroacetyl chloride gave azitidinones. Teh synthesised compo...

The Cyanuric chloride when treated with substituted 1,4-dihydropyridines at different temperature conditions give 2,4,6-(substituted dihydropyridinyl)-S-triazines. These synthesised compounds were screened for their antimicrobial activity against gram +ve and gram -Ve bacteria has been described.