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Recent News
11 April 2024
Press Release
Cambridge, UK and Kyiv, Ukraine, 11 April 2024: Metrion Biosciences Limited (“Metrion”), the specialist ion channel and cardiac safety screening contract research organisation (CRO) and drug discovery company, and Enamine Ltd (“Enamine”), the global leader in supplying small molecules and early drug discovery services, announced that Metrion has enhanced its High Throughput Screening (HTS) services with the addition of access to Enamine’s compound libraries.
27 March 2024
Press Release
March, 2024, Kyiv, Ukraine. Enamine Ltd, the global leader in supplying small molecules and early drug discovery services, announces the expansion of its library synthesis capabilities with a focus on Enamine REAL compounds to further support the growing demands of agricultural and pharmaceutical companies, research institutes, and drug discovery centers.
01 March 2024
News
We are excited to announce a strategic collaboration between Enamine, the world's leading provider of chemical building blocks, compound libraries, and biology services, and Genez International, a prominent enterprise with 15 years of experience in cross-border supply management, biopharmaceutical research and development, semiconductor equipment, and high-definition digital imaging systems.
Eur. J. Med. Chem. , 2014, 85 245-254
DOI: 10.1016/j.ejmech.2014.07.103
Havrylyuk D.; Zimenkovsky B.; Karpenko O.; Grellier P.; Lesyk R.
A series of novel 4-thiazolidinone–pyrazoline conjugates have been synthesized and tested for anti-Trypanosoma brucei activity. Screening data allowed us to identify five thiazolidinone–pyrazoline hybrids, which possess promising trypanocidal activity, with IC50 ≤ 1.2 μM. The highest active thiazolidinone–pyrazoline conjugates 3c and 6b (IC50 values of 0.6 μM and 0.7 μM, respectively) were 6-times more potent antitrypanosomal agents than nifurtimox. In addition, these compounds, as well as 6d and 6e had selectivity index higher than 50, and were more selective than nifurtimox. SAR study included substituent variations at the pyrazoline moiety, modifications of N3 position of the thiazolidinone portion, elongation of the linker between the heterocycles, as well as rhodanine–isorhodanine isomerism. It was also shown that methyl or aryl substitution at the thiazolidinone N3-position is crucial for trypanocidal activity.
Havrylyuk D.; Zimenkovsky B.; Karpenko O.; Grellier P.; Lesyk R.
Eur. J. Med. Chem. 2014, 85 245-254
DOI: 10.1016/j.ejmech.2014.07.103