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A series of novel b-lactams was synthesized from different imines and a special ketene derived from Nendo-5-norbornene-2,3-dicarboxyloylglycine 1 via the [2 ? 2] ketene imine cycloaddition. Then, b-lactams 3a-h were treated with 1-azido-4-nitrobenzene 4 to afford blactam-triazole hybrids 5a-h. Of the twenty-three b-lactams tested against chloroquine-resistant P. falciparum K14 strain, 3a and 3d showed IC 50 \ 20 lM, while 3j, 3m, 5a-5f exhibited IC 50 \ 50. These newly synthesized blactams were also tested against S. aureus, E. coli, P. aeruginosa, C. albicans and C. glabrata and showed no activity below 125 lg/mL.

Non‐nucleoside reverse transcriptase inhibitors (NNRTIs) have always been an important part of the anti‐HIV‐1 combination therapy known as combination antiretroviral therapy (cART) since 1996. The use of NNRTIs for about 22 years has led to some mutations in the residues that compose the reverse transcriptase active site, resulting in the emergence of drug‐resistant viruses. Thus, the search for new potent NNRTIs with an improved safety profile and activity against drug‐resistant HIV strains is indispensable, and many hit and lead NNRTIs have been discovered in the last decade. This review provides an overview of the development in this field from 2013 to August 2018.

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The asymmetric unit of the title compound, C11H11NO4, contains two mol­ecules, A and B, with different conformations: in mol­ecule A, the norborne and carb­oxy­lic acid groups lie to the same side of the heterocycle, whereas in a mol­ecule B, they lie on opposite sides. In the crystal, the A mol­ecules form R 2 2(8) carb­oxy­lic acid inversion dimers, linked by pairs of O—H⋯O hydrogen bonds. The B mol­ecules link to one of the ketone O atoms of the A mol­ecule by an O—H⋯O inter­action, resulting in tetra­mers (two A and two B mol­ecules). The tetra­mers are linked by weak C—H⋯O inter­actions, generating a three-dimensional network.

Recently, anti-cancer targeting drugs are directed against specific molecules and signaling pathways. These targeting agents have reasonable specificity, efficacy and less side effects. Tyrosine kinases, which play an essential role in growth factor signaling regulation, are significant targets in this type of therapy. Synthesized numerous tyrosine-kinase inhibitors (TKIs), such as substituted indolin-2-ones, are effective as anti-tumor and anti-leukemia agents. In this study, a series of novel substituted indolin-2-ones were studied as kinase inhibitor analogs through quantitative structure–activity relationship (QSAR) analysis. Two chemometrics methods, such as multiple linear regression (MLR) and partial least squares combined with genetic algorithm for variable selection (GA-PLS), were employed to establish relationships between structural characteristics and kinase inhibitory activity of used oxindole analogs. The GA-PLS was developed as the best predictor and validated QSAR model. The data set compounds were also studied by molecular docking to investigate their binding mechanism in the active site of tyrosine kinase enzyme. According to the information obtained from QSAR models and molecular docking analysis, 40 new potent lead compounds with novel structural features were introduced. Molecular docking, drug-likeness rules, ADMET analysis, bioavailability, toxicity prediction and target identification were carried out on the newly designed oxindoles to elucidate fundamental structural properties that affect their inhibitory activity.

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