SYNTHESIS AND SCREENING OF BENZOFURAN FUSED C-2,4,6-SUBSTITUTED PYRIMIDINE DERIVATIVES AS A NEW ANTIBACTERIAL AND ANTIFUNGAL AGENT

Abstract

Objective: Benzofuran and their heterocyclic analogs represent an important class of molecules which have a wide range of pharmacological activities. Therefore, in this study synthesis and antimicrobial activity of benzofuran fused C-2,4,6-substituted pyrimidine derivatives was extensively discussed.Methods: Benzofuran fused C-2,4,6-substituted pyrimidine derivatives (4a-k) were built by cyclo condensation, Claisen-Schmidt condensation followed by cyclization via coupling of benzoyl fragments, which include benzofuran, a pyrimidine ring and C-6 substituted phenyl residue with various substituents, connected by linker-S-band. The structures of the synthesized compounds were confirmed by analytical and spectral techniques and evaluated their antimicrobial activity.Results: The results of antibacterial and antifungal activity against various microbes, most of the compounds have shown considerable antimicrobial activity, but compounds 4g and 4e exhibits superior activity compared to standards, this may be due to presence bromo and fluro electron withdrawing substituent on the benzoyl moiety and more lipophilic nature of pyrimidine ring.Conclusion: According to the activity studies, it is observed that the synthesis and antimicrobial activity of benzofuran fused C-2,4,6-substituted pyrimidine derivatives have been shown better antimicrobial activity. The obtained results suggest that these classes of compounds can be considered as new hits for further structural optimization to obtain better antimicrobial drug development program.

Authors and Affiliations

Javarappa Rangaswamy, Nagaraja Naik

Keywords

Related Articles

LARVICIDE AND ANTIFUNGAL ACTIVITIES OF SARSAPARILLA (SMILAX LARVATA) EXTRACTS

Objective: This study aimed to investigate the toxicity, antimicrobial and larvicide activities of Smilax larvata Griseb. (Smilacaceae) extracts.Methods: Toxicity evaluation was performed by testing brine shrimp lethalit...

DEVELOPMENT AND VALIDATION OF A STABILITY INDICATING RP-HPLC METHOD FOR THE DETERMINATION OF VALSARTAN

Objective: A stability indicating RP-HPLC method was developed and validated for the determination of Valsartan using Telmisartan (10 µg/ml) as the internal standard.Methods: In this procedure Phenomenex ODS C-18(250×4...

IN VITRO ANTIOXIDANT ACTIVITIES, TOTAL FLAVONOID, PHENOLIC AND CAROTENOID CONTENT FROM VARIOUS EXTRACTS OF FOUR SPECIES ASTERACEAE HERB

Objectives: The objectives of this research were to study antioxidant activities from various extracts of Asteraceae herbs using two methods of antioxidant assays which were DPPH (2,2-diphenyl-1-picrylhidrazyl) and FRAP...

BIOASSAY-GUIDED EVALUATION OF FICUS SEMICORDATA FOR ANTIDIABETIC ACTIVITY

Objective: The early stage of diabetes mellitus type 2 is associated with postprandial hyperglycemia. The therapeutic approach involved in the treatment of type 2 diabetes mellitus is the use of agents that can decrease...

GENOTOXIC AND MUTAGENIC STUDIES OF THE ANTIEPILEPTIC DRUG LEVETIRACETAM IN PREGNANT RATS AND THEIR FETUSES

Objective: Levetiracetam (LEV) is an anti-epileptic drug, initially approved as an adjunct therapy in adult patients with partial-onset seizures, and used as monotherapy treatment during pregnancy. However, very few, if...

Download PDF file
  • EP ID EP575489
  • DOI 10.22159/ijpps.2017v9i9.17487
  • Views 43
  • Downloads 0

How To Cite

Javarappa Rangaswamy, Nagaraja Naik (2017). SYNTHESIS AND SCREENING OF BENZOFURAN FUSED C-2,4,6-SUBSTITUTED PYRIMIDINE DERIVATIVES AS A NEW ANTIBACTERIAL AND ANTIFUNGAL AGENT. International Journal of Pharmacy and Pharmaceutical Sciences, 9(9), 27-32. https://www.europub.co.uk/articles/-A-575489