Padmashali, BasavarajChidananda, Ballekere NanjundaswamyGovindappa, BanuprakashBasavaraj, Siddesh M.Chandrashekharappa, SandeepVenugopala, Katharigatta N.2020-10-162020-10-162019-05Padmashali Basavaraj, Chidananda Ballekere Nanjundaswamy, Govindappa Banuprakash, Basavaraj Siddesh M., Chandrashekharappa Sandeep, Venugopala Katharigatta N.. Synthesis and characterization of novel 1,6-dihydropyrimidine derivatives for their pharmacological properties. Journal of Applied Pharmaceutical Science. 2019 May; 2019 May: 117-1242231-3354http://imsear.searo.who.int/handle/123456789/210594The present research work involves the use of commercially available thiophene-2-carbaldehyde as a starting materialto construct novel pyrimidine compounds. Synthesis of pyrimidine derivatives has been done by the trimolecularBiginelli condensation reaction, which involves the use of thiophene-2-carbaldehyde with cyano ethylacetate andthiourea to yield 4-oxo-6-(thiophen-2-yl)-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile (1). The intermediate 1was methylated using methyl iodide and K2CO3 in dimethylformamide (DMF) which afforded dimethylated derivative1-methyl-2-(methylthio)-6-oxo-4-(thiophen-2-yl)-1,6-dihydropyrimidine-5-carbonitrile (2). The intermediatecompound 2 when refluxed with hydrazine hydrate in ethanol as a solvent led to the formation of the parent compound2-hydrazineyl-1-methyl-6-oxo-4-(thiophen-2-yl)-1,6-dihydropyrimidine-5-carbonitrile (3), the parent compound 3was used for the synthesis of carboxamides of N′-(5-cyano-1-methyl-6-oxo-4-(thiophen-2-yl)-1,6-dihydropyrimidin2-yl)substituted benzohydrazide (4a–d) and Schiff bases of (E)-2-(2-substituted benzylidenehydrazineyl)-1-methyl6-oxo-4-(thiophen-2-yl)-1,6-dihydropyrimidine-5-carbonitrile (5a–g). Selected title compounds are screened forantibacterial, analgesic, and antifungal activities.Substituted 1,6-dihydropyrimidinesynthesisantibacterialantifungalanalgesic.Journal ArticleIndiaDepartment of Chemistry, School of Basic Sciences, Rani Channamma University, Belagavi, IndiaDepartment of Chemistry, Sahyadri Science College (Kuvempu University), Shimoga, IndiaDepartment of Chemistry, SJB Institute of Technology, Bangalore, IndiaDepartment of Chemistry, KLE College of Engineering and Technology, Chikodi, Belagavi, IndiaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Kingdom of Saudi ArabiaDepartment of Biotechnology and Food Technology, Faculty of Applied Science, Durban University of Technology, Durban, South Africa.