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Bhat S.,25 North Wolfe Street | Shim J.S.,25 North Wolfe Street | Liu J.O.,25 North Wolfe Street | Liu J.O.,Johns Hopkins University
Bioorganic and Medicinal Chemistry Letters | Year: 2013

Tricyclic thiazoleamine derivatives that were identified as hits in a screen against human umbilical vein endothelial cell proliferation were subjected to a structure-activity relationship study. Two structurally superimposable scaffolds - 4H-thiochromeno[4,3-d]thiazol-2-amine and 5,6-dihydro-4H-benzo[6,7]cyclohepta[1,2-d]thiazol-2-amine derivatives - yielded low-micromolar inhibitors, and two among them 37 and 43 also exhibited antiangiogenic activity in an endothelial tube formation assay. Thus, 37 and 43 can serve as leads to develop a novel class of antiangiogenic agents. © 2013 Elsevier Ltd. All rights reserved. Source

Bhat S.,25 North Wolfe Street | Olaleye O.,25 North Wolfe Street | Olaleye O.,Texas Southern University | Meyer K.J.,25 North Wolfe Street | And 4 more authors.
Bioorganic and Medicinal Chemistry | Year: 2012

Our previous target validation studies established that inhibition of methionine aminopeptidases (MtMetAP, type 1a and 1c) from Mycobacterium tuberculosis (Mtb) is an effective approach to suppress Mtb growth in culture. A novel class of MtMetAP1c inhibitors comprising of N′-hydroxy-N-(4H,5H- naphtho[1,2-d]thiazol-2-yl)methanimidamide (4c) was uncovered through a high-throughput screen (HTS). A systematic structure-activity relationship study (SAR) yielded variants of the hit, 4b, 4h, and 4k, bearing modified A- and B-rings as potent inhibitors of both MtMetAPs. Except methanimidamide 4h that showed a moderate Mtb inhibition, a desirable minimum inhibitory concentration (MIC) was not obtained with the current set of MtMetAP inhibitors. However, the SAR data generated thus far may prove valuable for further tuning of this class of inhibitors as effective anti-tuberculosis agents. © 2012 Elsevier Ltd. All rights reserved. Source

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