Supaluk PrachayasittikulPhattrapoom LimnusontRatchanok PingaewSomsak RuchirawatVirapong PrachayasittikulSrinakharinwirot UniversityMahidol UniversityChulabhorn Research Institute2018-09-132018-09-132009-12-01EXCLI Journal. Vol.8, (2009), 35-40161121562-s2.0-70349926076https://repository.li.mahidol.ac.th/handle/20.500.14594/26957An array of interesting activities for bioactive 3-substituted thiopyridines have previously been reported. Herein, a series of α-and β-(1-adamantylthio) analogs of 3-picoline and phenylpyridines were prepared and investigated for antimicrobial (agar dilution method against 21 strains of microorganisms) and antimalarial (against P. falciparum) activities. It was found that β-thiopyridines, 5-(1-adamantylthio)-3-picoline (7) and 3-(1-adamantylthio)-4-phenylpyridine (8) are novel antimicrobials and antimalarials. Significantly, analogs 7 and 8 are very potent antimicrobials with MIC range of 2-32 μg/mL where 8 being the most potent. The β-sulfides 7 and 8 selectively inhibited the growth of tested gram-positive bacteria, but inactive against gram-negative bacilli including the members of Enterobacteriaceae. This study identified new antimicrobials that represent promising lead compounds suitable for further preclinical and clinical development.Mahidol UniversityAgricultural and Biological SciencesBiochemistry, Genetics and Molecular BiologyPharmacology, Toxicology and PharmaceuticsArticleSCOPUS