Antimicrobial, Antioxidant, and Anticancer Activities of Some Novel Isoxazole Ring Containing Chalcone and Dihydropyrazole Derivatives

被引:101
|
作者
Shaik, Afzal [1 ]
Bhandare, Richie R. [2 ]
Palleapati, Kishor [3 ]
Nissankararao, Srinath
Kancharlapalli, Venkata [3 ]
Shaik, Shahanaaz [4 ]
机构
[1] Jawaharlal Nehru Technol Univ, Dept Pharmaceut Chem, Vignan Pharm Coll, Vadlamudi 522213, Andhra Pradesh, India
[2] Ajman Univ, Coll Pharm & Hlth Sci, Dept Pharmaceut Sci, POB 346, Ajman, U Arab Emirates
[3] Acharya Nagarjuna Univ, Dept Pharmacognosy & Pharmaceut Chem, ASN Pharm Coll, Tenali 522201, Andhra Pradesh, India
[4] Acharya Nagarjuna Univ, Dept Pharmaceut Chem, Victoria Coll Pharm, Nallapadu 522001, Andhra Pradesh, India
来源
MOLECULES | 2020年 / 25卷 / 05期
关键词
isoxazole; chalcones; dihydropyrazole; antibacterial activity; antifungal activity; anticancer activity; ANTITUBERCULAR EVALUATION; POTENTIAL ANTICANCER; PYRAZOLINES; IDENTIFICATION; ANTIBACTERIAL; ANTIFUNGAL; AGONISTS; ANALOGS; MOIETY;
D O I
10.3390/molecules25051047
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Our previous work identified isoxazole-based chalcones and their dihydropyrazole derivatives as two important five-membered heterocycles having antitubercular activity. Hence, in the present study, we biologically evaluated 30 compounds, including 15 isoxazole ring-containing chalcones (17-31) and 15 dihydropyrazoles (32-46) derived from these chalcones for their antimicrobial, antioxidant, and anticancer activities. Chalcones exhibited superior antibacterial and antioxidant activities compared to dihydropyrazoles. Among the chalcones, compound 28 showed potent antibacterial (MIC = 1 mu g/mL) and antioxidant activities (IC50 = 5 +/- 1 mu g/mL). Dihydropyrazoles, on the contrary, demonstrated remarkable antifungal and anticancer activities. Compound 46 (IC50 = 2 +/- 1 mu g/mL) showed excellent antifungal activity whereas two other dihydropyrazoles 45 (IC50 = 2 +/- 1 mu g/mL) and 39 (IC50 = 4 +/- 1 mu g/mL) exhibited potential anticancer activity. The compounds were also tested for their toxicity on normal human cell lines (LO2) and were found to be nontoxic. The active compounds that have emerged out of this study are potential lead molecules for the development of novel drugs against infectious diseases, oxidative stress, and cancer.
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页数:11
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