Structural Determinants of Indole-2-carboxamides: Identification of Lead Acetamides with Pan Antimycobacterial Activity.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00352
Abstract: Tuberculosis (TB), caused by Mycobacterium tuberculosis (M.tb), is one of the leading causes of death in developing countries. Non-tuberculous mycobacteria (NTM) infections are rising and prey upon patients with structural lung diseases such as chronic… read more here.
Keywords: carboxamides identification; lead acetamides; indole carboxamides; determinants indole ... See more keywords
Amide-Amine Replacement in Indole-2-carboxamides Yields Potent Mycobactericidal Agents with Improved Water Solubility.
Sign Up to like & getrecommendations! Published in 2021 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.0c00588
Abstract: Indolecarboxamides are potent but poorly soluble mycobactericidal agents. Here we found that modifying the incipient scaffold by amide-amine substitution and replacing the indole ring with benzothiophene or benzoselenophene led to striking (10-20-fold) improvements in solubility.… read more here.
Keywords: indole carboxamides; carboxamides yields; amine replacement; amide amine ... See more keywords
Synthesis and Evaluation of Pyridyloxypyridyl Indole Carboxamides as Potential PET Imaging Agents for 5-HT2C Receptors.
Sign Up to like & getrecommendations! Published in 2018 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.7b00443
Abstract: Nine pyridyloxypyridyl indole carboxamides were synthesized and displayed high affinities for 5-HT2C receptors and high selectivity over 5-HT2A and 5-HT2B. Among them, 6-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]1H-indole-3-carboxamide (8) exhibits the highest 5-HT2C binding affinity (Ki = 1.3 nM) and… read more here.
Keywords: ht2c receptors; indole carboxamides; evaluation pyridyloxypyridyl; carboxamides potential ... See more keywords
Design, synthesis, apoptotic, and antiproliferative effects of 5-chloro-3- (2-methoxyvinyl)-indole-2-carboxamides and pyrido[3,4-b]indol-1-ones as potent EGFRWT/EGFRT790M inhibitors
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2023.2218602
Abstract: Abstract A new series of indole-2-carboxamides 5a-g, 6a-f and pyrido[3,4-b]indol-1-ones 7a and 7b have been developed as new antiproliferative agents that target both wild and mutant type EGFR. The antiproliferative effect of the new compounds… read more here.
Keywords: design synthesis; egfrwt egfrt790m; indole carboxamides; carboxamides pyrido ... See more keywords