56388-02-4

Upstream product

• 506-68-3 bromocyane 
• 99-42-3 methyl (4-hydroxy-3-nitro)benzoate 
• 536-25-4 methyl 3-amino-4-hydroxybenzoate 
• 104619-51-4 di(1H-imidazol-1-yl)methanimine 
• 99-76-3 methyl 4-hydroxylbenzoate 

Downstream Products

• 56350-69-7 1-(2-amino-benzooxazole-5-carbonyl)-4-phenyl-thiosemicarbazide 

Relevant academic research and scientific papers

ANTIBACTERIAL PICOLINAMIDE COMPOUNDS

Here we report the discovery of 2-(4-(3-(trifluoromethoxy)phenoxy)picolinamido) benzo[d]oxazole-5-carboxylate as an antibacterial with potent and selective activity against C. difficile. Its MIC50 andMIC90 values,documented across 101 strains of C. difficile, are 0.12 and 0.25 μg/mL, respectively. The compound is effective against C. difficile both at the logarithmic (vegetative) and stationary phases of growth. It targets cell-wall biosynthesis, as assessed both by macromolecular biosynthesis assays and by scanning-electron microscopy. Animals infected with a lethal dose of C. difficile and treated with compound 1 had better survival compared to treatment with vancomycin, which is the front-line antibiotic used for severe recurrent C. difficile infection.

Design, synthesis, and evaluation of substituted 2-acylamide-1,3-benzo[d]zole analogues as agents against MDR- and XDR-MTB

N-(5-Chlorobenzo[d]oxazol-2-yl)-4-methyl-1,2,3-thiadiazole-5-carboxamideox-amide has been identified as a potent inhibitor of Mtb H37Rv, with a minimum inhibitory concentration (MIC) of 0.42 μM. In this study, a series of substituted 2-acylamide-1,3-zole analogues were designed and synthesized, and their anti-Mtb activities were analyzed. In total, 17 compounds were found to be potent anti-Mtb agents, especially against the MDR- and XDR-MTB strains, with MIC values 10 μM. These analogues can inhibit both drug-sensitive and drug-resistant Mtb. Four representative compounds were selected for further profiling, and the results indicate that compound 18 is acceptably safe and has favorable pharmacokinetic (PK) properties. In addition, this compound displays potent activity against Gram-positive bacteria, with MIC values in the range of 1.48–11.86 μM. The data obtained herein suggest that promising anti-Mtb candidates may be developed via structural modification, and that further research is needed to explore other compounds.

Synthesis and biological activities of some Novel 2-Amino-(5 or 7-Substituted- 2-Oxoindolin-3-Ylidene) Benzoxazole-5-Carbohydrazide derivatives

A series of 2-amino-(5 or 7-substituted-2-oxoindolin-3-ylidene) benzoxazole-5-carbohydrazide derivatives were synthesized by treating 2-aminobenzoxazole-5-carbohydrazide with different substituted isatins. All the synthesized derivatives (VI a-l) were screened for their in vitro anticancer (against HeLa, IMR-32 & MCF-7 cancer cell lines), antioxidant (against DPPH radicals) and antimicrobial activities. The results of these studies showed the dose dependant anticancer, antioxidant and antimicrobial activities of the test compounds and the IC50 values of some compounds were comparable with their standard agent. The test compounds having substitution with different electron withdrawing groups at C-5 position showed more potent anticancer, antioxidant and antibacterial activities than those at C-7 position.

Synthesis of potent and selective inhibitors of Candida albicans N-myristoyltransferase based on the benzothiazole structure

Two parallel synthetic methods using solid-supported reagents were established to examine the rapid optimization of weak hit compound 1. Several compounds showed high potency in the low nanomolar range against N-myristoyltransferase. The structure-activity relationship (SAR) and antifungal activities of a series of novel 2-aminobenzothiazole N-myristoyltransferase inhibitors are presented.