A series of (2-(1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl) acetamido) acids) (6 a-m), (7) has been designed to inhibit the action of fungus chitin synthase enzyme (CHS). The synthesis of the designed compounds was carried out in four steps starting from the reaction between 1-methylquinazoline-2,4(1H,3H)-dione and ethyl chloroacetate to yield the ethyl acetate derivative. This ester was hydrolyzed to the corresponding carboxylic acid derivative that was then utilized to couple several amino acids getting the final designed compounds. The synthesized compounds were tested for their inhibition against CHS. Compound 7 showed the highest potency among others with minimum inhibitory concentration (IC₅₀) of 0.166 mmol/L, while polyoxin B (the positive control) had IC₅₀ of 0.17 mmol/L. The synthesized compounds were also evaluated for their in vitro antifungal activity using Aspergillus fumigates, Aspergillus flavus, Crytococcus neoformans and Candida albicans. Unfortunately, the 14 synthesized compounds showed lower in vitro activity compared to the used active controls. However, compound 6m and fluconazole have synergistic effect on Aspergillus flavus; Compounds 7 and fluconazole have synergistic effects on Aspergillus fumigates.

已设计了一系列（2-（1-甲基-2,4-二氧代-1,2-二氢喹唑啉-3（4H）-基）乙酰氨基）酸（6 am），（7）来抑制真菌几丁质合酶（CHS）。从1-甲基喹唑啉-2,4（1 H，3 H）-二酮与氯乙酸乙酯的反应开始，以四个步骤进行设计化合物的合成，从而得到乙酸乙酯衍生物。将该酯水解成相应的羧酸衍生物，然后将其用于偶联几个氨基酸，得到最终设计的化合物。测试合成的化合物对CHS的抑制作用。化合物7在抑制浓度最小的情况下显示出最高的效能（IC ₅₀）为0.166 mmol / L，而多恶菌素B（阳性对照）的IC ₅₀为0.17 mmol / L。还使用熏蒸曲霉，黄曲霉，新孢子菌和白色念珠菌评估了合成的化合物的体外抗真菌活性。不幸的是，与使用的活性对照相比，这14种合成的化合物显示出较低的体外活性。然而，化合物6m和氟康唑对黄曲霉具有协同作用。化合物7和氟康唑对熏蒸曲霉有协同作用。