{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,8]],"date-time":"2026-07-08T17:59:52Z","timestamp":1783533592018,"version":"3.55.0"},"reference-count":23,"publisher":"MDPI AG","issue":"23","license":[{"start":{"date-parts":[[2022,12,6]],"date-time":"2022-12-06T00:00:00Z","timestamp":1670284800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"National Natural Science Foundation of China","award":["82173694"],"award-info":[{"award-number":["82173694"]}]},{"name":"National Natural Science Foundation of China","award":["32141003"],"award-info":[{"award-number":["32141003"]}]},{"name":"National Natural Science Foundation of China","award":["81960623"],"award-info":[{"award-number":["81960623"]}]},{"name":"National Natural Science Foundation of China","award":["2021-I2M-1-039"],"award-info":[{"award-number":["2021-I2M-1-039"]}]},{"name":"National Natural Science Foundation of China","award":["2021-I2M-1-055"],"award-info":[{"award-number":["2021-I2M-1-055"]}]},{"name":"National Natural Science Foundation of China","award":["National Pathogen Resource Center-NPRC-32"],"award-info":[{"award-number":["National Pathogen Resource Center-NPRC-32"]}]},{"name":"National Natural Science Foundation of China","award":["2021-PT350-001"],"award-info":[{"award-number":["2021-PT350-001"]}]},{"name":"CAMS Innovation Fund for Medical Sciences (CIFMS)","award":["82173694"],"award-info":[{"award-number":["82173694"]}]},{"name":"CAMS Innovation Fund for Medical Sciences (CIFMS)","award":["32141003"],"award-info":[{"award-number":["32141003"]}]},{"name":"CAMS Innovation Fund for Medical Sciences (CIFMS)","award":["81960623"],"award-info":[{"award-number":["81960623"]}]},{"name":"CAMS Innovation Fund for Medical Sciences (CIFMS)","award":["2021-I2M-1-039"],"award-info":[{"award-number":["2021-I2M-1-039"]}]},{"name":"CAMS Innovation Fund for Medical Sciences (CIFMS)","award":["2021-I2M-1-055"],"award-info":[{"award-number":["2021-I2M-1-055"]}]},{"name":"CAMS Innovation Fund for Medical Sciences (CIFMS)","award":["National Pathogen Resource Center-NPRC-32"],"award-info":[{"award-number":["National Pathogen Resource Center-NPRC-32"]}]},{"name":"CAMS Innovation Fund for Medical Sciences (CIFMS)","award":["2021-PT350-001"],"award-info":[{"award-number":["2021-PT350-001"]}]},{"name":"National Science and Technology Infrastructure of China","award":["82173694"],"award-info":[{"award-number":["82173694"]}]},{"name":"National Science and Technology Infrastructure of China","award":["32141003"],"award-info":[{"award-number":["32141003"]}]},{"name":"National Science and Technology Infrastructure of China","award":["81960623"],"award-info":[{"award-number":["81960623"]}]},{"name":"National Science and Technology Infrastructure of China","award":["2021-I2M-1-039"],"award-info":[{"award-number":["2021-I2M-1-039"]}]},{"name":"National Science and Technology Infrastructure of China","award":["2021-I2M-1-055"],"award-info":[{"award-number":["2021-I2M-1-055"]}]},{"name":"National Science and Technology Infrastructure of China","award":["National Pathogen Resource Center-NPRC-32"],"award-info":[{"award-number":["National Pathogen Resource Center-NPRC-32"]}]},{"name":"National Science and Technology Infrastructure of China","award":["2021-PT350-001"],"award-info":[{"award-number":["2021-PT350-001"]}]},{"name":"Fundamental Research Funds for The Central Universities","award":["82173694"],"award-info":[{"award-number":["82173694"]}]},{"name":"Fundamental Research Funds for The Central Universities","award":["32141003"],"award-info":[{"award-number":["32141003"]}]},{"name":"Fundamental Research Funds for The Central Universities","award":["81960623"],"award-info":[{"award-number":["81960623"]}]},{"name":"Fundamental Research Funds for The Central Universities","award":["2021-I2M-1-039"],"award-info":[{"award-number":["2021-I2M-1-039"]}]},{"name":"Fundamental Research Funds for The Central Universities","award":["2021-I2M-1-055"],"award-info":[{"award-number":["2021-I2M-1-055"]}]},{"name":"Fundamental Research Funds for The Central Universities","award":["National Pathogen Resource Center-NPRC-32"],"award-info":[{"award-number":["National Pathogen Resource Center-NPRC-32"]}]},{"name":"Fundamental Research Funds for The Central Universities","award":["2021-PT350-001"],"award-info":[{"award-number":["2021-PT350-001"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>As a major public health problem, the prevalence of Acinetobacter baumannii (A. baumannii) infections in hospitals due to the pathogen\u2019s multiple-antibiotic resistance has attracted extensive attention. We previously reported a series of 1,3-diamino-7H-pyrrolo[3,2-f]quinazoline (PQZ) compounds, which were designed by targeting Escherichia coli dihydrofolate reductase (ecDHFR), and exhibited potent antibacterial activities. In the current study, based on our molecular-modeling study, it was proposed that PQZ compounds may function as potent A. baumannii DHFR (abDHFR)-inhibitors as well, which inspired us to consider their anti-A. baumannii abilities. We further found that three PQZ compounds, OYYF-171, -172, and -175, showed significant antibacterial activities against A. baumannii, including multidrug-resistant (MDR) strains, which are significantly stronger than the typical DHFR-inhibitor, trimethoprim (TMP), and superior to, or comparable to, the other tested antibacterial agents belonging to \u03b2-lactam, aminoglycoside, and quinolone. The significant synergistic effect between the representative compound OYYF-171 and the dihydropteroate synthase (DHPS)-inhibitor sulfamethoxazole (SMZ) was observed in both the microdilution-checkerboard assay and time-killing assay, which indicated that using SMZ in combination with PQZ compounds could help to reduce the required dosage and forestall resistance. Our study shows that PQZ is a promising scaffold for the further development of folate-metabolism inhibitors against MDR A. baumannii.<\/jats:p>","DOI":"10.3390\/molecules27238609","type":"journal-article","created":{"date-parts":[[2022,12,7]],"date-time":"2022-12-07T04:38:54Z","timestamp":1670387934000},"page":"8609","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":7,"title":["The Anti-Multidrug-Resistant Acinetobacter baumannii Study on 1,3-diamino-7H-pyrrolo[3,2-f]quinazoline Compounds"],"prefix":"10.3390","volume":"27","author":[{"given":"Han","family":"Wu","sequence":"first","affiliation":[{"name":"School of Pharmacy, Minzu University of China, Beijing 100081, China"},{"name":"Key Laboratory of Ethnomedicine, Minzu University of China, Ministry of Education, Beijing 100081, 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100050, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chunyang","family":"Xie","sequence":"additional","affiliation":[{"name":"Beijing Key Laboratory of Antimicrobial Agents\/Laboratory of Pharmacology, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Weiting","family":"Cao","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Minzu University of China, Beijing 100081, China"},{"name":"Key Laboratory of Ethnomedicine, Minzu University of China, Ministry of Education, Beijing 100081, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ziqi","family":"Zhao","sequence":"additional","affiliation":[{"name":"School of Pharmacy, Minzu University of China, Beijing 100081, China"},{"name":"Key Laboratory of Ethnomedicine, Minzu University of China, Ministry of Education, Beijing 100081, 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