Synthesis and Testing of 5-Benzyl-2,4-diaminopyrimidines as Potential Inhibitors of Leishmanial and Trypanosomal Dihydrofolate Reductase
نویسندگان
چکیده
منابع مشابه
Novel inhibitors of Leishmanial dihydrofolate reductase.
The program DOCK3.5 was used to search the Cambridge Structural Database for novel inhibitors of Leishmanial dihydrofolate reductase. A number of compounds were obtained and screened against the enzyme and against the intact parasite Leishmania donovani and the related organisms Trypanosoma brucei and Trypanosoma cruzi. The compounds screened showed weak activity in both the enzyme assays and t...
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کاتالیست یک سنتز جدید برای تیواترها توصیف شده است. واکنش الکل ها با آریل، هتروآریل و آلکیل تیو ل ها درحضور 1،3،5- تری آزو- 2،4،6- تری فسفرین-2،2،4،4،6،6 هگزاکلراید ((tapc به عنوان یک کاتالیست موُثر، بازده های خوب تا عالی از تیواترها را حاصل می کند. علاوه براین، واکنش تحت شرایط بدون فلز و بدون حلال پیش می رود، بنابراین یک مکمل جالب برای روش های شناخته شده سنتز تیواترها ارائه می دهد. یک مکانیسم ا...
15 صفحه اولnano-rods zno as an efficient catalyst for the synthesis of chromene phosphonates, direct amidation and formylation of amines
چکیده ندارد.
Synthesis and biological evaluation of 5-arylfuro[2,3-d]pyrimidines as novel dihydrofolate reductase inhibitors.
A series of about fifty novel 5-arylfuro[2,3-d]pyrimidine derivatives were synthesized as potential inhibitors of dihydrofolate reductase (DHFR) arising from different species. Weak enzyme inhibition was observed for most of the compounds, with only a few reaching IC50 values less than 30 microM. With regards to antibacterial and anti-malarial potency, only seven compounds showed a modest in vi...
متن کاملSynthesis of Novel 17-Oxo-17a-Aza-D-Homo-3, 5-Seco-Steroids as Potential 5α-Reductase Inhibitors
Benign prostatic hyperplasia (BPH) is a non-malignant enlargement of the prostate gland. Itis a leading disorder of the elderly male population. Excessive production of dihydrotestosteronehas been implicated in this pathological condition. Steroidal 5α-reductase is a membrane boundNADPH dependent enzyme which is responsible for the conversion of testosterone (T) todihydrotestosterone (DHT). The...
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ژورنال
عنوان ژورنال: Journal of Enzyme Inhibition and Medicinal Chemistry
سال: 2002
ISSN: 1475-6366,1475-6374
DOI: 10.1080/1475636021000059083