Synthesis and Evaluation of Anticonvulsant Activity of New 2-(4-Oxo-2-Propylquinazolin-4(3H)-yl) Acetohydrazide Derivatives | Chapter 1 | Pharmaceutical Research: Recent Advances and Trends Vol. 5

 

Aim: A new series of 2-(4-oxo-2-propylquinazolin-4(3H)-yl)acetohydrazide derivatives was prepared by reacting quinazolin-4(3H)-one hydrazide with substituted aromatic aldehydes. Quinazoline is a powerful pharmacological drug that possesses a number of biological properties, including antibacterial, antiviral, anticancer, convulsive, anxiety-inducing, anti-inflammatory, and analgesic properties. In this background, we have synthesized a series of quinazoline 4(3H)-one derivative 4a-4f and screened for their anticonvulsant activity.

 

Background: Antiepileptic agents are neither curative nor preventive and are active exclusively as a means of controlling the symptoms of epilepsy. They can directly act on ion channels or indirectly impact the synthesis, metabolism, or function of neurotransmitters or receptors that control channel opening and closing.

 

Methods: In this work, Schiff bases were prepared by treating quinazolin-4(3H)-one hydrazide with aromatic aldehydes. Six compounds 4a-4f were screened for anticonvulsant activity using the Isoniazid (INH)- and Pentylenetetrazole (PTZ)-induced convulsion models in mice.

 

Results: All the compounds were given satisfactory reaction yields that represent the efficiency of the employed synthetic route. In the INH-induced convulsion model, quinazolinones 4a, 4b, 4d, 4e, and 4f significantly delayed the onset of convulsion when compared to an induction control group, while the delay in seizure onset was not significant for 4c. In the PTZ-induced convulsion model, quinazolinones 4a, 4d, 4e, and 4f considerably delayed the onset of convulsion when compared to the induction control group, while the delay in seizure onset was not significant for 4b and 4c.

 

This indicates the anticonvulsant activity of these derivatives which might be due to potentiating GABA activity in the CNS. This anticonvulsant activity was due to the presence of electron-donating groups like OH, NH2, and OCH3 and electron-withdrawing groups like CF3 at the 2nd and 4th positions of the aromatic ring attached to the hydrazide function.

 

Conclusion: Based on the results, it can be concluded that quinazoline-4(3H)-one derivative exhibited anticonvulsant activity. Notably, all tested compounds showed prolonged onset of convulsions and protected maximum animals, suggesting an increased level of GABA by its potentiation or prevention of its depletion.

 

Author(s) Details

Suraj G. Malpani
Shivlingeshwar College of Pharmacy, Almala Dist: Latur-413520, Maharashtra, India.

 

Mayuri Jayprakash Chandrawanshi
Shivlingeshwar College of Pharmacy, Almala Dist: Latur-413520, Maharashtra, India.

 

Please see the book here:- https://doi.org/10.9734/bpi/prrat/v5/172

Examination of Hepatoprotective Activity of Annona squamosa Linn. Leaves against Isoniazid and Rifampin Induced Hepatotoxicity in Rats | Chapter 10 | Contemporary Research and Perspectives in Biological Science Vol. 9

Background: Tuberculosis is a granulomatous, chronic illness causing serious problems in developing countries. The first line of treatments is isoniazid, rifampin, pyrazinamide, ethambutol and streptomycin. The goal of this investigation was to examine if the ethanolic extract of Annona squamosa has any hepatoprotective activity in rats suffering from isoniazid-rifampin-induced hepatotoxicity.

Methodology: The rats were separated into five groups (n=6): group 1, control, group 2 isoniazid treated (100 mg/kg, i.p.) and rifampin (100 mg/kg, i.p..) in sterile water, group 3, control and standard drug silymarin, 2.5 mg/kg, b.w., p.o., groups 4 and 5 are treated with200 and 400 mg/kg, b.w., p.o., of ethanolic extract of AS. All of the treatment procedures were monitored for a total of 21 days after the rats were sacrificed. Biochemical and histological investigations were performed on the blood and liver respectively.

Results: Rats (Group - 2) treated with Rifampin (RIF) & Isoniazid (INH) elevated blood Serum Glutamic Oxaloacetic Transferase (SGOT), Serum Glutamate pyruvic transaminase (SGPT) and Alkaline Phosphatase (ALP) levels in varying degrees.  Administration of ethanolic extracts of Annona squamosa considerably reduced Rifampin and Isoniazid-induced elevations in serum liver marker enzymes SGOT, SGPT and ALP. Furthermore, the standard drug and extract-treated groups had significantly larger total macromolecule and total albumen levels. The extract’s efficacy was compared with silymarin, a standard medication. The histological profile also supported the results of biochemical studies. The ethanolic extract of Annona squamosa has been found to protect rats from oxidative liver injury caused by rifampin and isoniazid.

Conclusion: The ethanolic extract of AS protected rats from isoniazid and rifampin-induced oxidative liver injury and has potential hepato-protective properties. Furthermore, research of this type creates therapeutically feasible strategies to treat patients with drug-induced hepatotoxicity.

 

Author (s) Details

Samba Siva Raju Derangula
Department of Pharmacology, Sri Balaji Medical College, Hospital & Research Institute, Tirupati, Andhra Pradesh, India.

 

N. S. Muthiah
Department of Pharmacology, Sree Balaji Medical College and Hospital, Chrompet, Chennai, India.

 

Madhav P.
Department of Pharmacology, Sri Balaji Medical College, Hospital & Research Institute, Tirupati, Andhra Pradesh, India.

 

E. Sukumar
Saveetha Institute of Medical and Technical Sciences, Chennai, India.

 

Please see the book here:- https://doi.org/10.9734/bpi/crpbs/v9/3436

Hepatoprotective Activity of Pongamia pinnata Leaves on Antitubercular Drugs Induced Hepatotoxicity in Rats | Chapter 9 | Pharmaceutical Research - Recent Advances and Trends Vol. 1

 

Aim: The present study highlights the hepatoprotective effect of ethanolic extract of the leaves of the plant Pongamia pinnata on antitubercular drugs (isoniazid and rifampin) induced hepatotoxicity in rats.

Introduction: The hepatotoxic character of a drug is only discovered after it has gone on sale. The most common reason for taking drugs off the market is Drug Induced Liver Injury (DILI), which calls for labelling changes. Research evidence stated that anti-tubercular medication-induced liver damage is mainly due to oxidative stress which primes to cell injury and apoptosis in humans.

Methods: The experiment used five groups of male Wistar rats, each with six animals. Two control groups were given gum acacia and a mixture of isoniazid and rifampin. The two other groups received 200 and 400 mg/kg body weights of ethanolic extract from the leaves of Pongamia pinnata respectively. The fifth group was given silymarin (50mg/kg, p.o.). The concentrations of serum Alanine aminotransferase (ALT), Aspartate aminotransferase (AST), Alkaline Phosphatase (ALP), tissue Malondialdehyde (MDA) and thiols were estimated in the blood of all animals. One-way ANOVA was used for statistical analysis followed by Tukey's test.

Results: When rats were given the mixture of anti-tubercular drugs and high dosage (400 mg/kg) of ethanolic extract of Pongamia pinnata, the blood enzymes showed lower levels than antitubercular treated groups. The co-administration of a high dose of Pongamia pinnata extract with antitubercular drugs reduced MDA levels and elevated thiol levels considerably (p˂ 0.05). These biochemical marker levels however were not adjusted. Conversely, supplementation with Pongamia pinnata attenuated all the changes prompted by the antitubercular drugs and protected the hepatocytes from oxidative destruction revealing the hepatoprotective, antioxidant, antiapoptotic and membrane stabilising action of Pongamia pinnata leaves against drugs-induced toxicity.

Conclusion: In rats, Pongamia pinnata encompasses a partial protective effect against the hepatotoxicity caused by anti-tubercular drugs at high doses.

 

Author(s) Details:

 

Dr. Samba Siva Raju Derangula
Department of Pharmacology, Sri Balaji Medical College, Hospital & Research Institute, Tirupati, Andhra Pradesh, India.

 

Prof. Dr. N. S. Muthiah
Department of Pharmacology, Sree Balaji Medical College & Hospital, Chrompet, Chennai, Tamil Nadu, India.

 

Prof. Dr. H. S. Somashekar
Department of Pharmacology, St. Peter's Medical College, Hospital & Research Institute, Hosur, Tamil Nadu, India.

 

 

Dr. E. Sukumar
Saveetha Institute of Medical & Technical Sciences, Chennai, Tamil Nadu, India.

 

Please see the book here:  https://doi.org/10.9734/bpi/prrat/v1/61

Screening of Antituberculosis Drugs by Thin Layer Chromatography: Experimental Investigation | Chapter 11 | Novel Aspects on Chemistry and Biochemistry Vol. 1

 Tuberculosis resumes to be a main public health issue in underdeveloped countries. In South Asian countries TB is a very universal and prevalent ailment and most of the treatment programmes are controlled directly through administration agencies and emergency rooms. In this study, a novel thin-layer chromatographic screening approach for the labeling of rifampicin, isoniazid, and pyrazinamide in pharmaceutical dosages was manifested. The solvent scheme used to determine these three drugs was (propanol: hexane: ethyl acetate: liquid) (5:2:1.7:0.2 v/v) and the Rf value of rifampicin, pyrazinamide and isoniazid was 0.68, 0.74 and 0.50, individually. The developed arrangement for retention determinant had intra-epoch and inter-era repeatability with a predictable difference (SD) of about 0.5-1.0%.

Author(s) Details:

Abhilasha Durgbanshi,
Department of Chemistry, Dr. Harisingh Gour Vishwavidyalaya (A Central University), Sagar-470 003, India.

Devasish Bose,
Department of Criminology and Forensic Science, Dr. Harisingh Gour Vishwavidyalaya (A Central University), Sagar-470 003, India.

Please see the link here: https://stm.bookpi.org/NACB-V1/article/view/10440Z

Assessment of Isoniazid and Pyridoxine Hydrochloride in Pure and Pharmaceutical Preparations| Chapter 11 | Progress in Chemical Science Research Vol. 1

For the simultaneous assay of pyridoxine hydrochloride and isoniazid, a new spectrophotometric approach was devised. The approach was based on a proton transfer reaction between pyridoxine hydrochloride B6 and chromeazurol S at pH = 5.7, which produced a red, water soluble compound that absorbed at 510 nm. This technique for detecting isoniazid IND was discovered by bleaching the red-colored product, pyridoxine hydrochloride –chromeazurol S. Numbness and elevated blood levels of liver enzymes are frequent adverse effects of the IND. At concentrations ranging from 5 to 700 g/25ml for pyridoxine hydrochloride (i.e. 0.2-28.0) ppm, the molar absorptivity value was 1.51104 l/mol.cm, while at concentrations ranging from 25 to 1500 g/25ml for isoniazid (i.e. 1-60) ppm, the value of molar absorptivity was 1.36104 l/ This research seeks to develop a spectroscopic technique for determining isoniazid and pyridoxine hydrochloride in pharmaceutical formulations. As a result, this method has been successfully employed to detect pyridoxine hydrochloride and isoniazid in pharmaceutical formulations.

Author(s) Details:

Basima A. A. Saleem,
Department of Chemistry, College of Science, Mosul University, Mosul, Iraq.

Please see the link here: https://stm.bookpi.org/PCSR-V1/article/view/6769

A Key Step in the Direction of TB Elimination from the World: Management of Latent Tuberculosis Infection | Chapter 11 | Emerging Trends in Disease and Health Research Vol. 3

 The organism's infection Because a healthy person's immune system avoids disease, Mycobacterium Tuberculosis (MTB) may not produce clinical disease in the majority of people. However, the bacteria can still be found in the body in a form known as Latent Tuberculosis Infection (LTBI), which can cause disease if the immune system is compromised owing to causes such as diabetes, chronic use of steroids, HIV, and other factors. This article tries to concentrate on the diagnosis and treatment of LTBI. Due to infection rates as high as 40% of the population in places like India, treating all afflicted with LTBI may not be practical. However, in high-risk scenarios, focused therapy of LTBI is a viable alternative. The drug(s) used in LTBI therapy has changed dramatically, as will be discussed in this chapter.

Author(S) Details

S. Amit
National Institute of Tuberculosis and Respiratory Diseases, India.

A. Puneet
National Institute of Tuberculosis and Respiratory Diseases, India.

S. Prabhpreet
National Institute of Tuberculosis and Respiratory Diseases, India.

View Book:- https://stm.bookpi.org/ETDHR-V3/article/view/5886