Department of Chemistry, NED University of Engineering and Technology, Karachi, Pakistan.
Department of Chemistry, NED University of Engineering and Technology, Karachi, Pakistan/ H.E.J. Research Institute of Chemistry, ICCBS, University of Karachi, Karachi, Pakistan/.
Pak J Pharm Sci. 2022 Mar;35(2(Special)):665-669.
Seven derivatives of 1-phenyl ethyl group containing 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazine-thiones (THTT) were prepared and examined for their antibacterial and antifungal properties by using Microplate Alamar Blue Assay (MABA) and agar tube dilution protocol respectively. In vitro antifungal potential was investigated against five human pathogens and compared with the standard drugs amphotericin B and miconazole. In vitro antibacterial activity was investigated against four pathogens and compared with the ofloxacin. All compounds exhibited very promising antifungal activities against all tested pathogens. Structure activity relationship showed the importance of the presence of 1-phenyl ethyl substituent at N-3 of THTT nucleus for antifungal effects. However, these compounds showed significant antibacterial activity only against S. aureus. The compound 6c of the series was found most active compound that displayed promising antifungal potential against all tested pathogens [Growth Inhibition (GI) = 100%], and also showed promising antibacterial potential against S. aureus (GI% = 83.49) which is very much closer to the standard ofloxacin (GI% = 88.05). The study may be useful in the development of improved antimicrobial agents.
七种含有 1-苯乙基基团的 3,5-二取代四氢-2H-1,3,5-噻二嗪-4-硫酮（THTT）衍生物被制备出来，并通过微量棋盘法（MABA）和琼脂管稀释法分别对其抗菌和抗真菌性能进行了研究。体外抗真菌活性研究了对五种人类病原体的作用，并与标准药物两性霉素 B 和咪康唑进行了比较。体外抗菌活性研究了对四种病原体的作用，并与氧氟沙星进行了比较。所有化合物都表现出对所有测试病原体非常有前途的抗真菌活性。构效关系表明，THTT 核上 N-3 位存在 1-苯乙基取代基对于抗真菌作用非常重要。然而，这些化合物仅对金黄色葡萄球菌表现出显著的抗菌活性。该系列化合物 6c 被发现是最有效的化合物，对所有测试的病原体都表现出有希望的抗真菌潜力[生长抑制（GI）=100%]，对金黄色葡萄球菌也表现出有希望的抗菌潜力（GI%=83.49），这非常接近标准的氧氟沙星（GI%=88.05）。这项研究可能有助于开发改进的抗菌剂。
