Synthesis and Biological Evaluation of some Novel 2-Mercaptobenzothiazoles Carrying

ABSTRACT Several 2-mercaptobenzothiazole derivatives containing 1,3,4-oxadiazoles, 1,2,4-triazoles and 1,3,4-thiadiazoles at the second position were synthesized. Some of these synthesized compounds were evaluated for their in vivo analgesic, anti-inflammatory, acute toxicity and ulcerogenic actions. Some of the tested compounds showed significant analgesic and anti-inflammatory activities. Two of the compounds showed significant gastrointestinal protection compared to the standard drug diclofenac sodium. The compounds were also tested for their in vitro antimicrobial activity with most displaying selective activity against the Gram-negative bacteria Pseudomonas aeruginosa. In the present investigation the tested compounds did not possess antifungal activity

Herbex-kid Inhibits Immediate Hypersensitivity Reactions in Mice and Rats

Herbex-kid (HK), a polyherbal formulation was evaluated in various experimental allergic models of Type I hypersensitivity reactions. Compound 48/80 (C 48/80) has been shown to induce rat mesentery mast cell degranulation and HK (1.07, 10.75 and 107.5 mg ml−1) inhibited the mast cell degranulation in a dose dependent manner. HK (1.07, 10.75 and 107.5 mg kg−1; p.o.) showed dose-dependent protection against C 48/80 induced systemic anaphylaxis in male Balb/C mice. In active anaphylaxis model, male Wistar rats orally administered with 10.75 and 107.5 mg kg−1 of HK showed significant (P < 0.01) protection against mast cell degranulation, while in passive anaphylaxis model, only at 107.5 mg kg−1 showed significant (P < 0.01) reduction in mast cell degranulation. HK at all dose levels was able to significantly decrease the time spent in nasal rubbing in Wistar rats sensitized to ovalbumin, while only at 107.5 mg kg−1 it showed significant (P < 0.01) reduction in number of sneezes. In C 48/80-induced skin itch model, all dose levels of HK significantly (P < 0.001) decreased the time spent in itching and the number of itches. HK did not produce any significant inhibition in histamine induced contraction in guinea pig ileum. From the above findings we conclude that the HK possesses antiallergic activity mediated by reducing of the release mediators from mast cells and also by 5-HT antagonism without the involvement of histamine (H1) receptors

Biological Activities of 2-Mercaptobenzothiazole Derivatives: A Review

2-Mercaptobenzothiazoles are an important class of bioactive and industrially important organic compounds. These compounds are reported for their antimicrobial and antifungal activities, and are subsequently highlighted as a potent mechanism-based inhibitor of several enzymes like acyl coenzyme A cholesterol acyltransferase, monoamine oxidase, heat shock protein 90, cathepsin D, and c-Jun N-terminal kinases. These derivatives are also known to possess antitubercular, anti-inflammatory, antitumor, amoebic, antiparkinsonian, anthelmintic, antihypertensive, antihyperlipidemic, antiulcer, chemoprotective, and selective CCR3 receptor antagonist activity. This present review article focuses on the pharmacological profile of 2-mercaptobenzothiazoles with their potentialactivities

Synthesis and biological evaluation of some novel 2-mercaptobenzothiazoles carrying 2-pyrazoline

113-119This study presents synthesis of several 2-mercaptobenzothiazole derivatives 6a-s bearing 2-pyrazoline at the second position. Compounds 6h, 6i, 6j and 6n exhibited significant antimicrobial activity (inhibition zone 30-35 mm) against Pseudomonas aeruginosa. Compounds 6i, 6j and 6n showed significant analgesic and anti-inflammatory activities. Compounds 6i and 6n showed significant gastrointestinal protection compared to the standard drug diclofenac sodium

Simple and Validated Method for Estimation of Amlodipine by LC-MS (ESI) Using Healthy Indian Human Volunteers: and Evaluation of Pharmacokinetic Parameters

International audienceA simple and validated liquid chromatographic-mass spectrometric method (LC-MS) for amlodipine in human plasma was quantifi ed using LC-MS (ESI). Chromatography was performed on a C 18 analytical column, the mobile phase used was Acetonitrile-10mM Ammonium acetate in the ratio of 90:10%v/v and the retention times were 0.829 and 1.281 min for azithromycin (Internal standard) and amlodipine respectively. The ionization was optimized using ESI (+) and enhanced selectivity was achieved. The method is validated as per FDA guidelines. The analyte was shown to be stable over the timescale of the whole procedure. The pharmacokinetic parameters such as peak plasma concentration (C max), Time to peak Concentration (t max), Area under the plasma concentration-time curve (AUC 0-t & AUC 0-∞), elimination rate constant (K eli), Elimination half-life (t ½) were calculated. Log transferred values were compared by Analysis of Variance (ANOVA) followed by classical 90% confi dence interval for C max AUC 0-t .and AUC 0-∞ and was found to be within the range. These results indicated that the Test and Reference formulation is bioequivalent

Formulation of Sodium Alginate Nanospheres Containing Amphotericin B for the Treatment of Systemic Candidiasis

Purpose: The aim of this work was to formulate sodium alginate nanospheres of amphotericin B by controlled gellification method and to evaluate the role of the nanospheres as a "passive carrier" in targeted antifungal therapy. Methods: Sodium alginate nanospheres of amphotericin B were prepared by controlled gellification method, and the particle size analysis was carried out by scanning electron microscopy. The carrier capacity of sodium alginate was evaluated in terms of drug to polymer ratio. In vitro release study was carried out on all drug loaded nanospheres by the dialysis method. Release kinetics of drug from different drug loaded nanospheres was also determined. The in vivo antifungal efficacy of nanospheres bound drug vis-à-vis the free drug was evaluated in candidiasis- induced mice models. Results: Preparation of nanospheres through controlled gellification method yielded particles with a size range of 419.6 ± 0.28 nm. Studies on drug to polymer ratio showed a linear relationship between concentration of drug and drug loading capacity. In vitro release kinetic study revealed that the release of drug from the nanospheres followed Fickian diffusion. In vivo studies showed that the nanospherebound drug produced a higher antifungal efficacy than the free drug. Conclusion: The formulated sodium alginate nanospheres containing amphotericin B was found to have better antifungal activity when compared to the free drug and also yielded sustained in vitro release

Development and Application of a Validated LiquidChromatography-Mass Spectrometry Method fortheDetermination of Dexchlorpheniramine Maleate in Human Plasma: Determination of dexchlorpheniramine

Aconvenient liquid chromatographic-single Quadrupole mass spectrometric(LC-MS) method was developed and validated for dexchlorpheniramine maleate (INNname: chlorphenamine) determination in human plasma. The need for just a singleliquid-liquid extraction with ethyl acetate and being highly sensitive were theadvantages of this method. The linearity was also excellent over the range of 1 to150 ng.ml-1of dexchlorpheniramine maleate concentration. The method wasstatistically validated for its selectivity, linearity, precision and robustness. This methodwas successfully applied to the analysis of chlorpheniramine maleate in clinicalstudies