Alves, MA; de Queiroz, AC; Leite, AB; Martins, FT; Doriguetto, AC; Barreiro, EJ; Alexandre-Moreira, MS; Lima, LM in [Alves, Marina A.; Barreiro, Eliezer J.; Lima, Lidia M.] Univ Fed Rio De Janeiro UFRJ, Lab Avaliacao & Sintese Subst Bioativas LASSBio, Inst Nacl Ciencia & Tecnol Farmacos & Medicamento, CCS, POB 68023, BR-21941902 Rio De Janeiro, RJ, Brazil; [Alves, Marina A.; Barreiro, Eliezer J.; Lima, Lidia M.] Univ Fed Rio de Janeiro, Inst Quim, Programa Posgrad Quim, BR-21941909 Rio de Janeiro, RJ, Brazil; [de Queiroz, Aline C.; Leite, Anderson Brandao; Alexandre-Moreira, Magna S.] Univ Fed Alagoas UFAL, Inst Ciencias Biol & Sande, Lab Farmacol & Imunol, BR-57072900 Maceio, AL, Brazil; [Martins, Felipe T.; Doriguetto, Antonio C.] Univ Fed Goias, Inst Quim, Campus Samambaia,CP 131, BR-74001970 Goiania, Go, Brazil published Carbamoyl-N-aryl-imine-urea: a new framework to obtain a putative leishmanicidal drug-candidate in 2020.0, Cited 33.0. COA of Formula: C7H6O2. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4.
Leishmaniasis is a neglected parasitic disease, and current treatment includes limitations of toxicity, variable efficacy, high costs and inconvenient doses and treatment schedules. Therefore, new leishmanicidal drugs are still an unquestionable medical need. In this paper we described the design conception of a new framework, the carbamoyl-N-aryl-imine-urea, to obtain putative leishmanicidal drug-candidates. Compounds 9a-e and 10a-e were designed and synthesized and their leishmanicidal activity was studied in comparison to pentamidine, miltefosine and meglumine antimoniate. The conformational profile of the new carbamoyl-N-aryl-imine-urea framework was investigated by X-ray diffraction studies, using compound 9a as a model. The plasma stability of this putative peptide mimetic subunit was studied for compound 10e (LASSBio-1736). Among the congeneric series, LASSBio-1736 was identified as a new antileishmanial drug-candidate, displaying plasma stability, cytotoxicity against amastigote forms of L. amazonensis and L. braziliensis, and leishmanicidal activity in a cutaneous leishmaniasis murine model, without preliminary evidence of hepatic or renal toxicity.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles