English

A Bahashwan

doi:10.5897/ajpp11.094

Abstract

Pyrimidine derivatives, in general, have received significant interest due to their purported biological activities the anti-inflammatory, analgesic, anti-parkinsonism, and anti-microbial activities for five 2[(N-methyl indolyl)-methyl] pyrimidino derivatives 1-5 is reported. Pharmacological screenings showed that these compounds have good anti-inflammatory, analgesic, anti-parkinsonism, and anti-microbial activities comparable with reference drugs. Compound 2 showed similar activity of diclofenac sodium as analgesic. Compound 1, 2, 4 and flurbiprofen exhibited essentially equipotent anti-inflammatory activities. Compounds 1 and 3 were the most potent anti-parkinsonism agents compared with benztropine. In addition, compounds 1-5 showed antimicrobial activities comparable to streptomycin, erythromycin and fusidic acid as reference drugs. These pharmacological studies provide the activities for new pyrimidino derivatives and are expected to possess notable chemical and pharmacological activities for further pharmacological research.   Key words: Pyrimidino, pharmacological, analgesic, anti-inflammatory, anti-parkinsonism.

Highlights

Pyrimidines and fused pyrimidines, being an integral part of DNA and RNA, play an essential role in several biological processes and have considerable pharmacological importance, the pyrimidine ring can be found in nucleoside antibiotics, anti-bacterial, cardiovascular as well as agrochemical and veterinarian products (Fayed et al, 2009)
Heterocyclic compounds have received considerable attention owing to their variety of biological activities, especially as inhibitors of PDE5 extracted from human platelets (Piaz et al, 2002), HIV-1 reverse transcriptase (Sweeney et al, 2008), human EPK2 (Takayoshi et al, 2006), cyclin-dependent kinas (Brana et al, 2005)
Heterocyclic nitrogen compounds are indispensable structural units for medicinal chemists and used as antibiotics, anthelmintics, antiviral, anti-depressant, and anti-inflammatory (Ramaliagam et al, 2010; Shamroukh et al, 2007; Mansour et al, 2003). In view of these observations we evaluate some new pyrimidine derivatives 1-5 which were previously synthesized according to Ouf et al (2008), for their analgesic, antiinflammatory, anti-parkinsonism, and anti-microbial activities in comparison to some reference drugs (Figure 1)

Summary

Introduction

Pyrimidines and fused pyrimidines, being an integral part of DNA and RNA, play an essential role in several biological processes and have considerable pharmacological importance, the pyrimidine ring can be found in nucleoside antibiotics, anti-bacterial, cardiovascular as well as agrochemical and veterinarian products (Fayed et al, 2009). Heterocyclic nitrogen compounds are indispensable structural units for medicinal chemists and used as antibiotics, anthelmintics, antiviral, anti-depressant, and anti-inflammatory (Ramaliagam et al, 2010; Shamroukh et al, 2007; Mansour et al, 2003). In view of these observations we evaluate some new pyrimidine derivatives 1-5 which were previously synthesized according to Ouf et al (2008), for their analgesic, antiinflammatory, anti-parkinsonism, and anti-microbial activities in comparison to some reference drugs (Figure 1)

Methods

Results

Conclusion