Jignesh P. Raval

1,3-Dihydro-2H-indol-2-ones derivatives: design, synthesis, in vitro antibacterial, antifungal and antitubercular study.

1,3-dihydro-2H-indol-2-ones derivatives are reported to exhibit a wide variety of biodynamic activities such as antituberculer, anti HIV, fungicidal, antibacterial, anticonvulsant. These valid observations led us to synthesize some new indole-2-one derivative. Thus, herein we report synthesis of various 5-substituted-3-[{5-(6-methyl-2-oxo/thioxo-4-phenyl-1,2,3,4 tetrahydro pyrimidin-5-yl)-1,3,4-thiadiazol-2-yl}imino]-1,3-dihydro-2H-indol-2-one derivatives 4a-l using one pot multicomponent-Biginelli reaction via CaCl(2) catalyst. Structures and purity of these compounds were confirmed by elemental, IR, ((1)H &(13)C) NMR and Mass spectral analysis. Newly synthesized compounds were also tested for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H(37)Rv, in vitro antibacterial activity against selected human pathogens viz. Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi, Staphylococcus aureus, Staphylococcus pyogenus, Bacillus subtilis and antifungal activity against Candida albicans, Aspergillus niger, Aspergillus clavatus strains.

A strategic approach to the synthesis of functionalized spirooxindole pyrrolidine derivatives: in vitro antibacterial, antifungal, antimalarial and antitubercular studies

A series of spiro[pyrrolidin-2,3′-oxindoles] has been synthesized by exo-selective 1,3-dipolar cycloaddition reaction of a stabilized azomethine ylide, generated in situ by thermal [1,5]-prototropy, across various (E)-3-arylidene-1-phenyl-pyrrolidine-2,5-diones. The stereochemistry of these N-heterocycles has been confirmed using an X-ray diffraction study. To rationalize the observed regio- and stereoselectivity, DFT calculations at the B3LYP/6-31G(d,p) level were employed. It was found that this reaction preferentially affords the kinetic product. The compounds have been screened for their in vitro antibacterial, antifungal, antimalarial and antitubercular activities. Several compounds exhibited good activities comparable to those of established standard drugs.

Spray-dried Cefixime Encapsulated Poly(lactide-co-glycolide) Microparticles: Characterization and Evaluation of In Vitro Release Kinetics with Antibacterial Activity

Our study reports on the development of novel biodegradable microparticles prepared by a spray-drying technique using the poly(lactide-co-glycolide) (PLGA), a biodegradable polymer for the controlled delivery of cefixime. Cefixime is a water-soluble drug having short biological half-life of 3 h. The behavior of PLGA in controlling drug release responses of cefixime microparticles was investigated. The resultant microparticles were characterized by scanning electron microscopy, encapsulation efficiency, particle-size distribution, X-ray diffraction, and in vitro dissolution studies (pH 7.2). To investigate the type of release mechanism that occurs, dissolution data were plotted according to different kinetic models. The in vitro release profiles from microparticles followed first order and Higuchi model release. Antibacterial studies were carried out using a standard agar diffusion method to determine the effectiveness of formulations in inhibiting the growth of microorganisms. It showed that the released drug from the formulations was effectively inhibiting the growth of microorganisms with the minimum inhibitory concentration of < 1 µg/mL. Data revealed the potential of formulations for treatment of infections caused by various microorganisms. Thus, this study demonstrates the high potential of the spray-drying technique to obtain stable cefixime microparticles with good encapsulation efficiency to achieve a delivery profile that would yield the controlled released level of the drug over a long period of time (74 h).

Release Kinetics of Cellulosic Nano particulate Formulation for Oral Administration of an Antiviral Drug: Effect of Process and Formulation variables

Release Kinetics of Cellulosic Nano particulate Formulation forOral Administration of anAntiviral Drug: Effect of Process and Formulation variables Recently, researchers have increasing interest in cellulosic polymers for optimizing the efficiency of existing drugs utilizing better-designed drug delivery systems. In the present research nanoparticles were prepared using cellulose esters to obtain a drug product with a good oral bioavailability and biological half life. Acyclovir (ACY) was formulated by combining the modified solvent evaporation/extraction technique, sonicator and high pressure homogenization approaches. Various formulation parameters such as sonication-time, concentration of cellulose esters and surfactants were studied. Nanoparticles were obtained with enhanced encapsulation efficiency, negatively charged, defined shape, size and with homogeneous size distribution.

Design, synthesis, and in vitro antimicrobial activities of novel azetidinyl-3-quinazolin-4-one hybrids

A series of 2-[(4′-oxo-3′-chloro-2′-phenylazetidin-1′-ylamino)-methyl]-3-[N-isonicotinamide-yl]-quinazolin-4-one hybrids were synthesized starting from anthranilic acid in basic media using chloroacetyl chloride and benzene as solvent. The structure of the synthesized compounds has been evaluated on the basis of their elemental (C, H, and N) and spectral analysis (IR, 1H NMR, and 13C NMR spectrometry). In vitro antimicrobial evaluation of the synthesized compounds revealed that they posses promising antimicrobial activity against some gram-positive and gram-negative bacteria. Furthermore, compounds 7d and 7f exhibited potent antitubercular activity.

A Convenient, Rapid Microwave-Assisted Synthesis of 2-Substituted Phenyl-2,3-Dihydrobenzo[B][1,4]Thiazepine-3-Carboxamide Derivatives and Its Antimicrobial Activity

Abstract Using an environmentally benign procedure under microwave irradiation, a variety of 4-methyl-N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)-2-substituted phenyl-2,3-dihydrobenzo [b][1,4]thiazepine-3-carboxamide compounds were synthesized from 2-arylidene-3-oxo-N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)butanamide. Structures of these compounds were confirmed by IR, NMR (1H & 13C), and mass spectral analyses. Also, a considerable increase in the reaction rate has been observed with better yield in the microwave technique. The newly synthesized compounds were evaluated for antimicrobial activity against a variety of bacterial strains, and some of these compounds have shown significant antibacterial and antifungal activities. 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 Activity. GRAPHICAL ABSTRACT

In vitro antimycobacterial activity of novel N′-(4-(substituted phenyl amino)-6-(pyridin-2-ylamino)-1,3,5-triazin-2-yl)isonicotinohydrazide

A variety of N′-(4-(substituted phenyl amino)-6-(pyridin-2-ylamino)-1,3,5-triazin-2-yl)isonicotinohydrazide, 7a–r were synthesized by using 2-aminopyridine, isonicotic acid hydrazide and cyanuric chloride, and the structures of these compounds were confirmed by IR and NMR (1H and 13C) spectral analyses. Newly synthesized compounds were tested for their in vitro anti-tubercular activity against Mycobacterium tuberculosis H37Rv using the BACTEC 460 radiometric system.

RETRACTED: Synthesis and evaluation of anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation properties of new 2-(4-isobutylphenyl)propanoic acid derivatives

RETRACTED

Soya Based Polyurethane: Dynamic Mechanical Characterization

Novel biobased polyurethanes from soyabean oil-derived polyols, soyabean oil phosphate ester polyol (SOPE), blending of SOPE with monoglyceride of soyabean oil (SOPESG) and blending of SOPE with polyethylene glycol 400 mol. wt (SOPEP14) using aromatic isocynate adduct(TDI-TMP) were prepared and their dynamic mechanical properties were investigated after casting sheets on glass plate. The results showed that the damping ability gets enhanced through the introduction of monoglyceride and PEG-400 in to the base resin system.