Murlidhar S. Shingare

Synthesis, in vitro antibacterial and antifungal evaluations of new α-hydroxyphosphonate and new α-acetoxyphosphonate derivatives of tetrazolo [1, 5-a] quinoline

A series of new alpha-hydroxyphosphonate and alpha-acetoxyphosphonate derivatives have been synthesized for the first time of tetrazolo [1, 5-a] quinoline derivatives. Elemental analysis, IR, (1)H NMR, (13)C NMR and mass spectral data elucidated the structures of the all newly synthesized compounds. In vitro antimicrobial activities of the synthesized compounds were investigated against Gram-positive Bacillus subtilis, Gram-negative Escherichia coli and fungi Candida albicans and Aspergillus niger. Some of the tested compounds showed significant antimicrobial activity.

Knoevenagel condensation reactions in an ionic liquid

The condensation reaction of 4-oxo-(4H)-1-benzopyran-3-carbaldehydes and of aromatic aldehydes with 3-methyl-1-phenylpyrazolin-5-(4H)-one were carried out in an ionic liquid, ethylammonium nitrate, at room temperature in shorter times with higher yields of 78–92 and 70–75%, respectively, than found using conventional procedures.

Synthesis and biological evaluation of new 2-chloro-3-((4-phenyl-1H-1,2,3-triazol-1-yl)methyl)quinoline derivatives via click chemistry approach.

Synthesis of new 2-chloro-3-((4-phenyl-1H-1,2,3-triazol-1-yl)methyl)quinoline derivatives (4a-h) using 1,3-dipolar cycloaddition (click chemistry) reaction of 3-(azidomethyl)-2-chloro-quinoline derivatives (3a-h) with phenyl acetylene in the presence of Cu(I) catalyst has been achieved in very high yield. These molecules were evaluated in vitro for their antifungal and antibacterial activity. Most of the compounds exhibited significant antifungal and antibacterial activity against all the tested strains.

Ionic liquid promoted synthesis of bis(indolyl) methanes

Abstract1-benzyl-3-methyl imidazolium hydrogen sulphate [bnmim][HSO4] was found to be an effective catalyst for the condensation reaction of indoles and derivatives with benzaldehydes in microwave irradiation with lower reaction time and higher yields to give bis(indolyl) methanes.

Substituted 3-((Z)-2-(4-nitrophenyl)-2-(1H-tetrazol-5-yl) vinyl)-4H-chromen-4-ones as novel anti-MRSA agents: synthesis, SAR, and in-vitro assessment.

In search for a new antibacterial agent with improved antimicrobial spectrum and potency, we designed and synthesized a series of novel 3-((Z)-2-(4-nitrophenyl)-2-(1H-tetrazol-5-yl) vinyl)-4H-chromen-4-ones 7a-h by convergent synthesis approach. All the synthesized compounds were assayed for their in-vitro antibacterial activities against gram-negative and gram-positive bacteria. The preliminary structure-activity relationship, to elucidate the essential structure requirements for the antimicrobial activity that results into anti-MRSA (methicillin-resistant S. aureus) potential, has been described. Amongst the synthesized compounds 7d, 7e, 7f and 7h were found to possess activity against methicillin-resistant S. aureus in addition to the activity against other bacterial strains such as E. faecalis, S. pneumoniae, and E. coli.

Synthesis and anti-inflammatory activity of some new 4,5-dihydro-1,5-diaryl-1H-pyrazole-3-substituted-heteroazole derivatives

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 for comparison. Out of the 30 compounds tested, compound 19a, 19b, 25a, 25b exhibited significant anti-inflammatory activity. Selected compounds were also screened for in vitro COX-2 inhibition assay and analgesic activity in the acetic acid induced writhing model.

Surfactant catalyzed convenient and greener synthesis of tetrahydrobenzo[a]xanthene-11-ones at ambient temperature

Summary An efficient and greener protocol for the synthesis of 12-aryl-8,9,10,12-tetrahydrobenzo[a]xanthen-11-one using tetradecyltrimethylammonium bromide (TTAB) at room temperature in water is described.

Water mediated uncatalyzed facile synthesis ofylidenenitriles of 4-oxo-(4H)-1-benzopyran-3-carbaldehyde

A simple, efficient and environment ecofriendly route has been developed for the synthesis of ylidenenitriles of 4-oxo-(4H)-1-benzopyran-3-carbaldehyde by the condensation of 4-oxo-(4H)-1-benzopyran-3-carbaldehyde with active methylene compounds viz. malononitrile, cyanoacetic acid and cyanoacetamide in distilled water without catalyst at 90 °C for 1–2 h with quantitative yields and higher selectivity.

An Efficient Synthesis and Antibacterial Screening of Novel Oxazepine α-Aminophosphonates by Ultrasound Approach

An efficient synthesis of novel α-aminophosphonates by the reaction of quino[2,3-b][1,5]benzoxazepines with triethyl phosphite in the presence of the easily available, inexpensive, and nontoxic catalyst p-toluene sulphonic acid (p-TSA). This method affords the α-aminophosphonates under the influence of ultrasound irradiation in solvent-free conditions, in short reaction times (4–6 min), high yields (80–90%), with improved purity. The synthesized α-aminophosphonates show antibacterial activity against Gram-positive and Gram-negative bacteria. Supplemental materials are available for this article. Go to the publishers online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file.

Cellulose sulfuric acid as a bio-supported and recyclable solid acid catalyst for the one-pot synthesis of 2,4,5-triarylimidazoles under microwave irradiation

Abstract A simple, rapid, and highly efficient method has been attempted for the three-component condensation of benzil/benzoin, aldehydes, and ammonium acetate under microwave irradiation in the presence of a catalytic amount of bio-supported cellulose sulfuric acid under solvent-free conditions to afford the 2,4,5-triarylimidazole derivatives. The catalyst is easily prepared, inexpensive, separated simply by filtration, gives excellent yield of products with shorter reaction times, and is recyclable several times.