Ratnadeep S. Joshi

Synthesis, analgesic and anti-inflammatory activities of some novel pyrazolines derivatives

In search for a new analgesic and anti-inflammatory agent with improved potency, we designed and synthesized a series of 3,2-(4,5-dihydro-5-(4-morphilinophenyl)-1H-pyarazol-3-yl)phenols 6(a-g) and its N-phenylpyrazol-1-carbothioamide 7(a-g) by Claisan-Schmidt condensation followed by the reaction of hydrazine hydrate. All the synthesized compounds were assayed for their in vivo analgesic and anti-inflammatory activities. All the compounds synthesized showed the potential to demonstrate analgesic and anti-inflammatory activity, of particular interest compounds 6a, 6b, 6g, 7a, 7d and 7g were found comparable to Diclofenac.

Ultrasound assisted green synthesis of bis(indol-3-yl)methanes catalyzed by 1-hexenesulphonic acid sodium salt.

1-Hexenesulphonic acid sodium salt as catalyst for green synthesis of bis(indol-3-yl)methanes was described. The reaction of indole with various aldehydes in water using ultrasound irradiation at ambient temperature for appropriate time using 1-hexenesulphonic acid sodium salt furnish the desired product in good to excellent yield. Utilization of aqueous medium, simple reaction conditions, isolation, and purification makes this manipulation very interesting from an economic and environmental perspective.

Development of practical methodologies for the synthesis of novel 3(4-oxo-4H-chromen-3-yl)acrylic acid hydrazides.

We report a new environmentally-benign, convenient and facile methodology for the synthesis of new series of 3(4-oxo-4H-chromen-3-yl)acrylic acid hydrazides derivatives designed by exploring the molecular hybridization approach between isoniazide and 3(4-oxo-4H-chromen-3-yl)acrylic acids by using EDCl/HOBt under ultrasound irradiation in very short reaction time. Utilization of easy reaction conditions, isolation and purification makes this manipulation very interesting from an economic perspective.

Synthesis, Characterization, and Biological Screening of Some Novel Thiazolidin-4-One and α-Aminophosphonate Derivatives

Abstract Synthesis of some new functionalized thiazolidin-4-ones and α-amino phosphonate derivatives has been reported. The imines were synthesized from the reaction of various substituted anilines with 1-phenyl-3-(pyridine-4-yl)-1H-pyrazole-4-carbaldehyde in ethanol at reflux condition. The corresponding thiazolidin-4-ones and α-aminophosphonates were prepared by reaction of imines with mercaptoacetic acid and triethyl phosphite, respectively. The structures of the newly synthesized compounds were confirmed by IR, 1H NMR, and mass spectral data and were evaluated for their antimicrobial activities. GRAPHICAL ABSTRACT

Synthesis and Antimicrobial Evaluation of New 5-(2-Hydroxyphenyl)-3-(4-(Phenylthio)Phenyl)-1H-Pyrazole-2(5H)-Carbothioamide Analogues of 2-(4-(Phenylthio)Phenyl)-4H-Chromen-4-One

Abstract A series of novel 5-(2-hydroxyphenyl)-3-(4-(phenylthio)phenyl)-1H-pyrazole-2(5H)-carbothioamide derivatives have been synthesized via the ring opening of 2-(4-(phenylthio)phenyl)-4H-chromen-4-one with semicarbazide in ethanol and KOH under ultrasonic irradiation. The synthesized compounds were screened for antibacterial and antifungal activity against bacteria Staphylococcus aureus (MRSA E710) and Escherichia coli (25922) and fungi Candida albicans and Aspergillus fumigates, respectively. Some of the tested compounds showed significant antimicrobial activity. IR, 1H NMR, mass spectral data, and elemental analysis elucidated the structures of all the newly synthesized compounds. Supplemental materials are available for this article. Go to the publishers online edition of Phosphorus, Sulfur, and Silicon and the Related Elements for the following free supplemental resource: Biological Assay. GRAPHICAL ABSTRACT

Ultrasonic Promoted Synthesis and Antibacterial Screening of Some Novel Piperidine Incorporated α-Aminophosphonates

Abstract A simple and high-yielding method was developed for the synthesis of novel α-aminophosphonates from imines, obtained from 4-(piperidine-1-yl)benzaldehyde, by using triethylphosphite in the presence of dilute HCl under ultrasound irradiation. This method, which was developed for the synthesis of α-aminophosphonates, gave excellent yields. 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. GRAPHICAL ABSTRACT

Potassium dihydrogen phosphate: an inexpensive reagent for the solvent-free, one-pot synthesis of α-aminophosphonates

Abstract An efficient procedure is described for the synthesis of α-aminophosphonates in the presence of catalytic amount of potassium dihydrogen phosphate (5 mol%) under solvent-free condition at room temperature. Triethyl phosphite reacts with imines (generated in situ from an aldehyde and an amine) to give corresponding coupled products in excellent yields. The present methodology presents several advantages, such as elevated yield, short reaction time, and easy work-up.