Naik Halehatty R Prakash, Naik Halehatty S Bhojya, Naik Thangali R Ravikumar, Naika H Raja, Gouthamchandra K, Mahmood Riaz, Ahamed B M Khadeer
Department of Studies and Research in Industrial Chemistry, School of Chemical Sciences, Kuvempu University, Shankaraghatta, Bhadravati Taluk 577 451, Shimoga, Karnataka, India.
Eur J Med Chem. 2009 Mar;44(3):981-9. doi: 10.1016/j.ejmech.2008.07.006. Epub 2008 Jul 16.
We have characterized a new class of 2-mercapto/2-selenobenzo[h]quinoline-3-carbaldehyde (3/4). Antibacterial potential of these compounds against a wide range of gram-positive and gram-negative bacteria was studied. The selenium containing compound 4 showed significant inhibition zone on Staphylococcus aureus (22.76+/-0.14), Bacillus subtilis (20.63+/-0.24), and Streptococcus pyogenes (19.54+/-0.20) over sulfur containing compound 3. To validate the ethnotherapeutic claims of the synthetic compounds in skin diseases, wound healing activity was studied, besides antioxidant activity to understand the mechanism of wound healing. The interaction behavior of these compounds with DNA was investigated by absorption spectra (obtained K(b) constant for 3 is 2.7x10(5) and for 4 is 3.8x10(6)), viscosity, and thermal denaturation studies. Finally, the results show that the DNA intercalated 3/4 compounds are strong antioxidants; they show significant wound healing activity and protect oxidative DNA damage from harmful free radical reactions.
我们已对一类新型的2-巯基/2-硒代苯并[h]喹啉-3-甲醛（3/4）进行了表征。研究了这些化合物对多种革兰氏阳性菌和革兰氏阴性菌的抗菌潜力。含硒化合物4对金黄色葡萄球菌（22.76±0.14）、枯草芽孢杆菌（20.63±0.24）和化脓性链球菌（19.54±0.20）的抑菌圈比含硫化合物3显著。为了验证合成化合物在皮肤病方面的民族治疗效果，除了研究抗氧化活性以了解伤口愈合机制外，还研究了伤口愈合活性。通过吸收光谱（化合物3的K(b)常数为2.7×10(5)，化合物4的K(b)常数为3.8×10(6)）、粘度和热变性研究，研究了这些化合物与DNA的相互作用行为。最后，结果表明，插入DNA的3/4化合物是强抗氧化剂；它们具有显著的伤口愈合活性，并能保护DNA免受有害自由基反应的氧化损伤。
