Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents.

09:49 EDT 1st November 2014 | BioPortfolio

Summary of "Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents."

A series of N'-substituted-2-(5-nitrofuran or 5-nitrothiophen-2-yl)-3H-benzo[d]imidazole-5-carbohydrazide derivatives were synthesized and investigated for their abilities to inhibit β-hematin formation, hemoglobin hydrolysis and in vivo for their antimalarial efficacy in rodent Plasmodium berghei. Selected analogues were screened for their antitubercular activity against sensitive MTB H(37)Rv and multidrug-resistant MDR-MTB strains, and cytotoxic activity against a panel of human tumor cell lines and two nontumourogenic cell lines. Compounds 3a, 5a, f, 6g were the most promising as inhibitors of β-hematin formation, however, their effect as inhibitors of hemoglobin hydrolysis were marginal. The most active compounds to emerge from the in vitro and in vivo murine studies were 3a and 6i, suggesting an antimalarial activity via inhibition of β-hematin formation and are as efficient as chloroquine. The cytotoxic and antitubercular activities of the present compounds were not comparable with those of the standard drugs employed. But, however, compound 5b showed better antitubercular activity compared to rifampin against multidrug-resistant MDR-MTB strains. Compounds 3a, 6i and 5b showed a good safety index.

Affiliation

Laboratorio de Síntesis Orgánica, Universidad Central de Venezuela, Aptdo. 47206, Los Chaguaramos, 1041-A Caracas, Venezuela.

Journal Details

This article was published in the following journal.

Name: Bioorganic & medicinal chemistry
ISSN: 1464-3391
Pages: 2023-9

Links

PubMed Articles [17844 Associated PubMed Articles listed on BioPortfolio]

Synthesis, characterisation and evaluation of N-mannich bases of 2-substituted Benzimidazole derivatives.

Benzimidazoles and its derivatives represent one of the mainly biological active classes of literature.

Biological Evaluation of the Activity of Some Benzimidazole-4,7-dione Derivatives.

The study presented here is a follow up of the authors' interest in the approach to selective and cytotoxic bioreductive anticancer prodrugs. The current work is devoted to explore both the biological...

Synthesis and cytotoxic evaluation of some new 1,3dioxolo4,5-gchromen-8-one derivatives.

Homoisoflavonoids are naturally occurring compounds belong to flavonoid classes possessing various biological properties such as cytotoxicity. In this work, an efficient strategy for the synthesis of ...

Biological approach of anticancer activity of new benzimidazole derivatives.

A series of new benzimidazole derivatives, earlier synthesized, was tested in vitro as new bioreductive prodrugs with the potential anticancer activity. Their effect on the DNA destruction and growth ...

Synthesis and biological evaluation of 3-phenethylazetidine derivatives as triple reuptake inhibitors.

We report the synthesis of 3-phenethylazetidine derivatives 2 and their biological activities against 5-HT, NE and DA transporters as well as microsomal stability, CYP inhibition, and hERG inhibition ...

Clinical Trials [1658 Associated Clinical Trials listed on BioPortfolio]

Evaluation of Home-Based Management of Fever in Urban Ugandan Children

The purpose of this study is to see if providing effective antimalarial treatment at home for parents/guardians to treat their children for malaria will lead to an improved health outcome ...

Clinical Investigation of In-vivo Susceptibility of P.Falciparum to Artesunate in Western Cambodia

There are worrying signs that parasitological responses to the artemisinin drugs for uncomplicated falciparum malaria are slower than elsewhere in the world.If responses to artesunate are ...

Autologous or Donor Cytotoxic T-Lymphocytes in Treating Patients With Relapsed Epstein-Barr Virus-Associated Hodgkin's Lymphoma or Non-Hodgkin's Lymphoma

RATIONALE: Biological therapies use different ways to stimulate the immune system and stop cancer cells from growing. Treating a person's or donor's a cytotoxic T lymphocytes in the labora...

A Study Evaluating the Effects of Lipid Lowering Treatment on Steroid Synthesis

Cholesterol is the precursor of glucocorticoids, mineralocorticoids and sex steroids. Both adrenal and non-adrenal (ovarian + testicular) all steroid hormones are primarily synthesized usi...

BI 6727 Randomised Trial in Ovarian Cancer

This is an international, randomized phase II trial. The aim is to assess the efficacy and the safety of BI 6727 Versus investigator's best choice single agent cytotoxic in recurrent third...

Medical and Biotech [MESH] Definitions

Derivatives of ethylene, a simple organic gas of biological origin with many industrial and biological use.

An acridine derivative formerly widely used as an antimalarial but superseded by chloroquine in recent years. It has also been used as an anthelmintic and in the treatment of giardiasis and malignant effusions. It is used in cell biological experiments as an inhibitor of phospholipase A2.

A field of biological research combining engineering in the formulation, design, and building (synthesis) of novel biological structures, functions, and systems.

A cytotoxic polypeptide quinoxaline antibiotic isolated from Streptomyces echinatus that binds to DNA and inhibits RNA synthesis.

Ergostane derivatives of 28 carbons with oxygens at C1, C22, and C26 positions and the side chain cyclized. They are found in WITHANIA plant genus and have cytotoxic and other effects.

Search BioPortfolio:
Loading
Advertisement

Relevant Topic

Blood
Latest News Clinical Trials Research Drugs Reports Corporate
Blood is a specialized bodily fluid that delivers necessary substances to the body's cells (in animals) – such as nutrients and oxygen – and transports waste products away from those same cells.  In vertebrates, it is composed of blo...

Advertisement