Synthesis of a new series of heterocyclic scaffolds for medicinal purposes.

نویسندگان

  • H S Hilal
  • M S Ali-Shtayeh
  • R Arafat
  • T Al-Tel
  • W Voelter
  • A Barakat
چکیده

A new series of substituted 8-fluro-4H-pyrimido[2,1-b] [1,3]benzothiazole-4-ones () substituted 7-methyl-4H-isoxazolo[2,3-a]pyrimidin-4-ones, and substituted 2-methyl-5,6,7,8-tetrahydro-9H-isoxazolo[2,3-a]pyridopyrimidin-9-ones, compounds I-VII, have been prepared via condensation of beta-keto esters with 2-aminopyridine derivatives, in the presence of polyphosphoric acid. The same technique has also been used to prepare diazepine compounds, VIII-X, by condensation of a gamma-keto ester with 2-aminopyridine derivatives. Details of synthetic procedures are shown. The new compounds have been characterized by elemental analysis, GC-MS, FT-IR and NMR spectrometry. Antibacterial, antifungal and anticancer (cytotoxic) activities, for three of these compounds, have been investigated and are presented.

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

New Benzimidazoles Derivatives: Synthesis, Characterization and Antifungal Activities

One of the most important goals in medicinal chemistry is the development of new heterocyclic compounds with pharmaceutical activity. Thus, a novel series of the derivatives of benzimidazole were synthesized and the structures of all the synthesized compounds have been confirmed by IR, 1 H- and 13C-NMR, Mass Spectroscopy and elemental analysis. The title compounds have been evaluated for antifu...

متن کامل

Synthesis and Biological Evaluation of 2-Phenyl Benzothiazole Derivatives as Cytotoxic Agents

Cancer is a leading cause of death worldwide. Many heterocyclic cores are present in the structures of clinically approved anticancer drugs. Meanwhile, benzothiazoles have been reported as one of the most important heterocyclic scaffolds in previously reported anticancer agents in the literature. Therefore, in this report, a novel series of 2-phenyl benzothiazole derivatives was synthesized, bi...

متن کامل

Synthesis of Some New Heterocyclic Compounds with Potential Biological Activity

A series of new 2-arylimino-3-aryl-5-[5?-(3,4-dichlorophenyl)-2?-furylidene]-4-thiazolidinones (3a-l) have been synthesised by the condensation of 5-(3,4-dichlorophenyl)-2-furaldehyde 1 with 2-arylimino-3-aryl-5H-4-thiazolidinones 2 in glacial acetic acid. The physical and spectral data of the synthesised compounds are determined. The synthesised compounds have been screened for their in vitro ...

متن کامل

Nano-Ceria (CeO2): An Efficient Catalyst for the Multi-Component Synthesis of a Variety of Key Medicinal Heterocyclic Compounds

This review gives an overview of the applications of ceria nanoparticles as inexpensive, efficient, reusable, and environmentally sustainable heterogeneous catalysts for the synthesis of a variety of key medicinal heterocyclic compounds with the emphasis on mechanistic aspects of the reactions. Literature has been surveyed from 2005 to 2018.

متن کامل

Thiadiazoles: the appropriate pharmacological scaffolds with leishmanicidal and antimalarial activities: a review

Leishmaniasis and malaria are serious public health problems in tropical and sub-tropical regions worldwide. Development of drug-resistant strains has disrupted efforts to control the spread of these diseases in the world. The conventional antiparasitic chemotherapy still suffers from side effects and drug resistance. Therefore, the development of novel antimalarial and leishmanicidal drugs rem...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

عنوان ژورنال:
  • European journal of medicinal chemistry

دوره 41 8  شماره 

صفحات  -

تاریخ انتشار 2006