Antimicrobial Evaluation of New Synthesized Aza Heterocycles

M. B. Elamin, S. M. Ali, E. Abdallah
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Abstract

The Pd-precatalyst was found to exhibit high catalytic activity for C-C bond formation in Suzuki-Miyaura cross-coupling reactions of differentheteroaryl (5-bromo-2-bromoacetyl) thiophene,4- (5-bromothiophen-2-yl)-methyl-1,3-thiazole,isoquinolinium bromide salt) with either aryl or heteroarylboronic acids. All reactions in this study were conducted in water under thermal heating as well as microwave irradiation conditions. The antimicrobial activities of synthesized compounds were evaluated against eight different strains of microorganisms (four fungal strains, two Gram-positive bacteria and two Gram-negative bacteria) using a cup plate diffusion method. The results showed that, most of the 20 tested compounds exhibited varying degrees of antimicrobial activities. However, 6 compounds recorded high antifungal activity (≤ 20 mm zone of inhibition), 3 were antibacterial (against Gram-positive) and 4 showed high broad-spectrum antibacterial efficacy (against Gram-positive and Gram-negative). These bioactive compounds are recommended for further pharmacological and toxicological investigations for possible formulation as wide spectrum antibacterial and antifungal agents. take longer time (30-40 min). The 20 cross- couple products were screened for their antimicrobial potential. The results reproduced 6 new antifungal, 3 new antibacterial (against Gram-positive) and 4 wide spectrum antibacterial agents (against gram-positive and gram-negative). These interesting findings could be the base for further future investigations in order to synthesize novel antimicrobial drugs.
新合成的含氮杂环的抗菌评价
pd预催化剂对不同的杂芳基(5-溴-2-溴乙酰基)噻吩、4-(5-溴-2-基)甲基-1,3-噻唑、异喹啉溴盐与芳基或杂芳基硼酸的Suzuki-Miyaura交叉偶联反应中C-C键的形成具有较高的催化活性。本研究中的所有反应均在水中进行,加热和微波辐照条件下进行。采用杯板扩散法对8种不同的微生物(4株真菌、2株革兰氏阳性菌和2株革兰氏阴性菌)进行抑菌活性评价。结果表明,20种化合物中大部分具有不同程度的抑菌活性。其中6个化合物具有较高的抑菌活性(≤20 mm抑制区),3个化合物具有抗菌活性(对革兰氏阳性),4个化合物具有较高的广谱抗菌活性(对革兰氏阳性和革兰氏阴性)。这些生物活性化合物被推荐用于进一步的药理学和毒理学研究,以作为可能的广谱抗菌和抗真菌剂。时间较长(30-40分钟)。对20个交叉偶联产物进行了抗菌潜力筛选。结果发现6种新型抗真菌药物,3种新型抗菌药物(抗革兰氏阳性),4种广谱抗菌药物(抗革兰氏阳性和革兰氏阴性)。这些有趣的发现为今后进一步研究合成新型抗菌药物奠定了基础。
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