Sadaf J. Gilani

Synthesis and pharmacological evaluation of condensed heterocyclic 6-substituted 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole and 1,3,4-oxadiazole derivatives of isoniazid.

The significance of this study was to prepare various isoniazid derivatives by introducing the isoniazid core into several molecules to explore the possibilities of some altered biological activities. Series of 6-substituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole (3a-g) and 1,3,4-oxadiazole (4a-g and 5) derivatives of isoniazid were synthesized in satisfactory yield and pharmacologically evaluated for their anti-inflammatory, analgesic, ulcerogenic, and lipid peroxidation activities by known experimental models.

Synthesis, anticonvulsant and toxicity screening of newer pyrimidine semicarbazone derivatives

A number of N-(4,6-substituted diphenylpyrimidin-2-yl) semicarbazones (4a-t) were synthesized and tested for their anticonvulsant activity against the two seizure models, maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (scPTZ). All the synthesized compounds possessed the four essential pharmacophoric elements for good anticonvulsant activity. Most of the compounds displayed good anticonvulsant activity with lesser neurotoxicity. To assess the unwanted effects of the compounds on liver, estimation of enzymes and proteins was carried out.

Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: Synthesis and pharmacological evaluation

A number of 5-(4-substituted phenyl)-2-(substituted benzylsulfanyl)-4-(substituted phenyl)-6-methyl-1,4-dihydro-5-pyrimidine carboxamides (1-30) were designed and synthesized keeping in view the structural requirements as suggested in the pharmacophore model for antihypertensive activity. All the synthesized compounds were tested for antihypertensive activity by non-invasive blood pressure (NIBP) measurements (tail-cuff method) in rats. Almost all the tested compounds displayed considerable decrease in the blood pressure as compared to control. Thirteen compounds showed significant antihypertensive activity comparable to the standard drug nifedipine.

Synthesis and in vitro antimicrobial activity of novel N-(6-chlorobenzo[d]thiazol-2-yl) hydrazine carboxamide derivatives of benzothiazole class

In this study, a series of novel 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole (6a–g) and 1,3,4-oxadiazole (7a–g, 8) were synthesized from N-(6-chlorobenzo[d]thiazol-2-yl) hydrazine carboxamide derivatives of benzothiazole class. Antimicrobial properties of the title compound derivatives were investigated against one Gram (+) bacteria (Staphylococcus aureus), three Gram (−) bacteria (Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae) and five fungi (Candida albicans, Aspergillus niger, Aspergillus flavus, Monascus purpureus and Penicillium citrinum) using serial plate dilution method. The investigation of antibacterial and antifungal screening data revealed that all the tested compounds showed moderate to good inhibition at 12.5–100 µg/mL in DMSO. It has been observed that triazolo-thiadiazole derivatives are found to be more active than 1,3,4-oxadiazole derivatives against all pathogenic bacterial and fungal strains.

Hypoglycemic herbs and their polyherbal formulations: a comprehensive review

Diabetes has been described as the common metabolic disorder of carbohydrate, protein and fat metabolism, which is due to absolute or relative lack of insulin and is characterized by hyperglycemia. Two main types of diabetes based on their clinical manifestations are identified as Type I diabetes—known as Juvenile diabetes or insulin sensitive diabetes and Type II diabetes or non-insulin dependent diabetes mellitus (NIDDM). Diabetes has been conventionally treated with orthodox medicines that function as hypoglycemic agents, or insulin production modulators and/or lipoprotein lowering agents. Since the therapy is life long, therapeutic agents devoid of side effects would be appreciated and one of such approach is use of alternative system of medicine comprising herbal products. Phyto-constituents identified from traditional medicinal plants are presenting an exciting opportunity for the development of new types of therapeutics. Due to increase in demand by patients to use natural products with anti-diabetic activity, investigations on hypoglycemic agents derived from medicinal plants have gained popularity in recent years. The novelty of this review article is to focus on the utility of hypoglycemic herbs and their polyherbal formulations.

Synthesis and pharmacological evaluation of N -(6-chlorobenzo[ d ]thiazol-2-yl)hydrazine carboxamide derivatives of benzothiazole

A series of 6-substituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole (6a–g) and 1,3,4-oxadiazole (7a–g, 8) derivatives of benzothiazole were synthesized in satisfactory yield and pharmacologically evaluated for their anti-inflammatory, analgesic, ulcerogenic, and lipid peroxidation activities by known experimental models. All the synthesized compounds were in good agreement with elemental and spectral data. Some of the synthesized compounds have significant anti-inflammatory and analgesic activities. Ulcerogenic and irritative action on the gastrointestinal mucosa, in comparison with standard are low.

Synthesis, Antifungal and Toxicity Screening of Newer Isoniazid Derivatives

A series of Isoninicotinic acid hydrazide (INH) incorporated derivatives of thiazolidin-4-one (2a-h, 3a-h), azetidin-2one (4a-h) and 1,3,4-oxadiazole (5a-h) were synthesized in satisfactory yield and pharmacologically evaluated for their in vitro antifungal activity. All the synthesized compounds were in good agreement with elemental and spectral data. A majority of the tested compounds showed good to moderate antifungal activity against all tested pathogenic fungal strains. To evaluate the toxicity of the compounds on liver, estimation of enzymes was also carried out.

Polymeric hydrogels for contact lens-based ophthalmic drug delivery systems

Abstract The field of ocular drug delivery is one of the most interesting and challenging routes for researchers over the past 10–20 years. It is difficult to obtain the correct therapeutic concentration of a drug at the required site, due to the physiological and anatomical constraints. To achieve effective ophthalmic therapy, an adequate amount of drug must be delivered and maintained within the eye region. A contact lens is a novel dosage form; curved in shape and made up of polymers that are designed to cover the cornea and which cling to the surface of the eye owing to surface tension. The interest in formulation of contact lenses has significantly increased in the last decade, as several new techniques have been developed for designing contact lenses for extended drug delivery. The use of a contact lens helps increase precorneal residence time to a longer duration and exhibit its maximum biological action. Additionally, it can provide a uniform release profile, compared to the pulsatile delivery with eye drops. This can potentially result in improved therapeutic outcomes which significantly improve the compliance. In this chapter, we describe the literature on ocular delivery using contact lenses, their classification and manufacturing process, and recent advances on drug delivery techniques using such lenses.

Nanocarriers for the treatment of tuberculosis

BACKGROUND Nano size based drug delivery systems are an emerging technique with the potential to develop new strategies involving handling of drugs at the nanometer scale. There are many nano-based drug delivery systems that have been extensively reported as drug carriers for the treatment of tuberculosis. METHODS There are numerous nano sized drug delivery systems like lipid nanoparticles, polymeric micelle, carbon nanotubes and polymeric nanoparticles that have been reported for a long time to treat diseases. There are a number of drawbacks in conventional TB dosage forms such as the development of multiple drug resistance, resulting in intolerable toxicity and high drug dose required. So, to overcome the drawbacks of conventional therapy, there is a need for a new drug delivery system with an aim to reduce the side effects of drug treatment. Nano-sized based drug delivery systems have considerable potential for the treatment of tuberculosis. These delivery systems have several advantages like high stability, high loading capacity, the feasibility of incorporation of both hydrophilic and hydrophobic drugs, and feasibility of variable routes of administration, and prolonged drug release from the matrix. These advantages enable enhanced drug solubility, bioavailability, reduced dosing frequency, high targeting, and may resolve the problem of non adherence to prescribed therapy, which is one of the major obstacles in the control of tuberculosis epidemics. CONCLUSION This article gives an exhaustive review of patents and research papers published over the years on the challenges, the current treatment therapy of the disease faces, and potential advantages of nano sized formulations to offer more effective treatment and prevention for tuberculosis.

Optimization and Validation for Simultaneous Estimation of Citicoline and Piracetam in bulk and tablet formulations using RP-HPLC method: Analytical quality by design approach

The present work describes a reversed phase high performance liquid chromatographic method for simultaneous estimation of Citicoline (CIT) and Piracetam (PIR) in bulk as well as tablet dosage forms. The estimation was carried out on a C18 column using mobile mixture of acetonitrile and 10 mM disodium hydrogen phosphate buffer in the ratio of 10: 90 (v/v) as a mobile phase. All analytes were detected by measuring the absorbance at 205 nm with flow rate of 1.0 ml/min. The total run time of the study was 16 min. for complete separation of both drugs. The elution was achieved at the retention times of 3.79 and 13.08 min for Citicoline, and Piracetam, respectively. The method was validated for accuracy, precision, linearity, specificity and sensitivity as per ICH norms. The calibration curves were found linear over the concentration ranges of 4–40μg/mL for Citicoline and 5–50μg/mL for Piracetam. From the validation study it was found that the method is specific, rapid, accurate and precise.