Abstract: Heterocyclic compounds occupy a central position among those molecule that makes life possible. The chemistry of heterocyclic compounds has been an interesting field of study for a long time. Heterocyclic nucleus 1,3,4thiadiazole constitutes constitutes an important class of compounds for new drug development. The synthesis of novel thiadiazole derivatives and investigation of their c...

A modular synthetic approach was developed in which variation of the triplets of building blocks used enabled systematic variation of the macrocyclic scaffolds prepared. The approach was demonstrated in the synthesis of 17 diverse natural product-like macrocyclic scaffolds of varied (12-20-membered) ring size. The biological relevance of the chemical space explored was demonstrated through the ...

5-Phenyl-furan-2-carboxylic acids have emerged as a new, promising class of antimycobacterial agents that the ability to interfere with iron homeostasis. Considering lack structural data on these compounds, we analyzed crystal fluorinated ester derivative 5-(4-nitrophenyl)furan-2-carboxylic acid, one most potent candidates in series. Here, describe preparation methyl 5-(2-fluoro-4-nitrophenyl)f...

The antimalarial agents NAS-91 and NAS-21 were found to express potent antimycobacterial activity, NAS-91 being more active than NAS-21. They partially inhibited mycolic acid biosynthesis and profoundly altered oleic acid production. The development of a cell-free assay for Delta 9-desaturase activity allowed direct demonstration of the inhibition of oleic acid biosynthesis by these compounds.

BACKGROUND Tuberculosis is a world-wide problem affecting humans and animals. There is increasing development of resistance of the pathogens to current antimycobacterial agents. Many authors have investigated activities of extracts and isolated compounds from plants. The traditional uses of plants have frequently been the criterion to select plants investigated. In this contribution, we investi...

We describe two brothers of consanguineous Pakistani parents who lived in Norway and had disseminated infections due to nontuberculous mycobacteria. The first boy developed clinical signs of disseminated BCG infection after vaccination. He was successfully treated with antimycobacterial agents. Two and one-half years later, he developed disseminated Mycobacterium avium complex infection and die...

We have designed and synthesized both the quinoline and naphthalene based molecules influenced by the unique structural make-up of mefloquine and TMC207, respectively. These compounds were evaluated for their anti-mycobacterial activity against drug sensitive Mycobacterium tuberculosis H37Rv in vitro at single-dose concentration (6.25 microg/mL). The compounds 22, 23, 26 and 27 inhibited the gr...