The role of medicinal chemistry in the drug discovery process

Beswick, Paul J.; Naylor, A.M.

doi:10.1016/b978-0-7020-4299-7.00009-3

Cited by 2 publications

(2 citation statements)

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“…However, 8a showed an MIC > 500 μg/ml. Since a lead compound is a new chemical entity, that could potentially be developed into a new drug, by optimizing its beneficial effects and minimizing its side effects, this result led us to speculate that an exploration of structural modifications of Compound 8a (Beswick & Naylor, ) and an evaluation of the antituberculosis activity of the resultant compounds could lead to compounds with more significant activity than 8a . As shown in Figure , proposed compounds were synthesized to evaluate the effect of the structural modification that lead to two lead Compounds 7 and 8a .…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antituberculosis activity of new acylthiosemicarbazides designed by structural modification

Martı́nez

Espitia-Pinzón

Silva-Miranda

et al. 2019

Drug Development Research

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Acylthiosemicarbazides 8a-n were designed by structural modification of lead Compound 7. The syntheses of 8a-n involve a five-step procedure starting from carboxylic acids. Compounds 8a-n were tested against three Mycobacterium tuberculosis strains to measure their inhibitory antituberculosis activities. These activities could be explained according to the presence or absence of the chlorine substituent in the aromatic ring of the amide joined to the thiosemicarbazide core. Thiosemicarbazide derivative 8n is a candidate for the development of novel antitubercular agents.Ongoing studies are focused on exploring the mechanism by which these compounds inhibit M. tuberculosis cell growth. K E Y W O R D Sacylthiosemicarbazides, antituberculosis agents, design, isosteric modification, synthesis

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Section: Introductionmentioning

confidence: 99%

Synthesis and antituberculosis activity of new acylthiosemicarbazides designed by structural modification

Martı́nez

Espitia-Pinzón

Silva-Miranda

et al. 2019

Drug Development Research

View full text Add to dashboard Cite

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“…3 Imidazo[1,2-a]pyridine derivatives are becoming more and more important in medicinal and organic chemistry. They have displayed a broad spectrum of pharmacological and biological activities, such as antitumoral, 4 antiviral, 5 antiinflammatory, 6 antibacterial, 7 antifungal, 8 antiulcer, 9 antiprotozoal 10 and antiretroviral activities. 11 So these pyridine derivatives have found their use as glycosidase inhibitors, 12 inhibitors of gastric acid secretion, 13 cyclin-dependent kinase inhibitors, 14 calcium channel blockers, 15 agents against herpesviruses 16 and so on.…”

Section: Introductionmentioning

confidence: 99%