7H-Benzo[7,8]chromeno[2,3-d]pyrimidin-9(8H)-amine (6a,b) have been synthesized via hydrazinolysis of the imidates (5a,b). Polysubstituted chromenotriazolopyrimidine (7a-j), (12a,b) and Schiff base (8a,b) derivatives have also been prepared. The new heterocyclic derivatives were affirmed by spectral data. The target compounds have been screened for antibacterial and antifungal activity. Compounds 6a,b and 7a-c, g,h displayed the most favorable antimicrobial activities in resemblance to the reference antimicrobial agents by IZ range over 24 mm. In addition, MIC, MBC and MFC were also tested and screen for most active compound 6a by 6.25 µg/mL showing bactericidal effect. SAR study revealed that the antimicrobial vitality of the target compounds was safely influenced by the lipophilicity substituents and the calculated log P value. The potent compounds were subjected into in vitro enzyme screening (14α-Demethylase and DNA Gyrase) against both interesting targets and showed good inhibitory profile. Molecular modeling analyses were introduced and discussed focusing on the docking of active compounds into two essential targets, and their ADMET properties were studied.

通过酰亚胺化物（5a，b）的肼解反应合成了7 H-苯并[7，8]铬色[2，3 - d ]嘧啶-9（8 H）-胺（6a ，b）。还制备了多取代的铬三氮杂唑并嘧啶（7a-j），（12a，b）和席夫碱（8a，b）衍生物。光谱数据证实了新的杂环衍生物。已经筛选了目标化合物的抗菌和抗真菌活性。化合物6a，b和7a-c，g，h在超过24 mm的IZ范围内显示出与参考抗菌剂相似的最有利的抗菌活性。此外，还对MIC，MBC和MFC进行了测试，并以6.25 µg / mL的速度对大多数活性化合物6a进行了筛选，显示出杀菌作用。SAR研究表明，亲脂性取代基和计算出的log P值会安全地影响目标化合物的抗菌活性。对有效化合物进行体外酶筛选（14α-脱甲基酶和DNA促旋酶）都针对两个有趣的靶标，并显示出良好的抑制作用。介绍并讨论了分子建模分析，重点是将活性化合物对接到两个基本目标中，并研究了它们的ADMET性质。