13098-73-2Relevant academic research and scientific papers
Synthesis, Antileishmanial Activity and In Silico Studies of Aminoguanidine Hydrazones (AGH) and Thiosemicarbazones (TSC) Against Leishmania chagasi Amastigotes
Alexandre-Moreira, Magna S.,Aquino, Pedro G. V.,Bourguignon, Jean-Jacques,Bri-Card, Jacques,Freitas, Johnnatan D.,Meneghetti, Mario R.,Nascimento, Igor J. S.,Queiroz, Aline C.,Rodrigues, Klinger A. F.,Rodrigues, Raiza R. L.,Santos, Mariana S.,Schmitt, Martine,de Aquino, Thiago M.,Araújo, Morgana V.,Fran?a, Paulo H. B.,Rodrigues, érica E. E. S.,Santos-Júnior, Paulo F. S.,da Silva-Júnior, Edeildo F.,de Araújo-Júnior, Jo?o X.
, p. 151 - 169 (2022/02/05)
Background: Leishmaniasis is a worldwide health problem, highly endemic in developing countries. Among the four main clinical forms of the disease, visceral leishmaniasis is the most se-vere, fatal in 95% of cases. The undesired side-effects from first-li
An unprecedented intramolecular to intermolecular mechanistic switch in 1,1-diaminoazines leading to differential product formation during the I2-induced tandem oxidative transformation
Kathuria, Deepika,Gupta, Pankaj,Chourasiya, Sumit S.,Sahoo, Subash C.,Beifuss, Uwe,Chakraborti, Asit K.,Bharatam, Prasad V.
, p. 4129 - 4138 (2019/04/30)
The tautomeric preference of guanylhydrazones towards the azine form induces an unprecedented intramolecular to intermolecular mechanistic switch during the I2-catalyzed oxidative transformation leading to 4,5-disubstituted-3-amino-1,2,4-triazoles in contrast to the reaction of semicarbazones and thiosemicarbazones to form 1,3,4-oxa/thiadiazoles. This intramolecular to intermolecular cyclization shift was established through control experiments and was attributed to the high energy demand (～22 kcal mol-1) for the azine tautomer to adopt the s-cis conformation which is essential for the intramolecular reaction. An I2 induced protocol for an efficient and straightforward synthesis of 4,5-disubstituted-3-amino-1,2,4-triazoles has been developed via tandem oxidative transformation of guanylhydrazones (in its preferentially existing azine tautomeric form) with distinct advantages such as wide substrate scope, use of substoichiometric amounts of iodine, no requirement of external oxidizing agents, base free reaction conditions, short reaction time and moderate to good yields. The role of silver salt in improving the yield and shortening of reaction time was also highlighted.
METHOD OF TREATING CANCER WITH A COMBINATION OF BENZYLIDENEGUANIDINE DERIVATIVES AND CHEMOTHERAPEUTIC AGENT.
-
Page/Page column 20-21; 40, (2017/03/08)
The present invention relates to a composition for use in treating a glioma or ameliorating the effects of a glioma, particularly glioblastoma, wherein said composition comprises a first active agent selected from the group consisting of a compound of for
NOVEL THERAPEUTIC USES OF BENZYLIDENEGUANIDINE DERIVATIVES FOR THE TREATMENT OF PROTEOPATHIES
-
Page/Page column 48, (2016/01/25)
The present invention relates to novel uses of a compound of formula (I), or a tautomer and/or a pharmaceutically acceptable salt thereof, in treating a disorder associated with the PPP1R15A pathway and associated with protein misfolding stress and in par
Synthesis and biological activities of 2-amino-1-arylidenamino imidazoles as orally active anticancer agents
Li, Wen-Tai,Hwang, Der-Ren,Song, Jen-Shin,Chen, Ching-Ping,Chuu, Jiunn-Jye,Hu, Chih-Bo,Lin, Heng-Liang,Huang, Chen-Lung,Huang, Chiung-Yi,Tseng, Huan-Yi,Lin, Chu-Chung,Chen, Tung-Wei,Lin, Chi-Hung,Wang, Hsin-Sheng,Shen, Chien-Chang,Chang, Chung-Ming,Chao, Yu-Sheng,Chen, Chiung-Tong
experimental part, p. 2409 - 2417 (2010/09/03)
2-Amino-l-arylidenaminoimidazoles, a novel class of orally (po) active microtubule-destabilizing anticancer agents, were synthesized. The compounds were designed from a hit compound identified in a drug discovery platform by using cancer cell-based high throughput screening assay. Selective synthesized compounds exerted cell cytotoxicity against human cancer cells. The underlying mechanisms for the anticancer activity were demonstrated as interacting with the tubulins and inhibiting microtubule assembly, leading to proliferation inhibition and apoptosis induction in the human tumor cells. Furthermore, two compounds showed in vivo anticancer activities in both po and intravenously (iv) administered routes and prolonged the life spans of murine leukemic P388 cells-inoculated mice. These new po active antimitotic anticancer agents are to be further examined in preclinical studies and developed for clinical uses.
Novel molecular hybrids of cinnamic acids and guanylhydrazones as potential antitubercular agents
Bairwa, Ranjeet,Kakwani, Manoj,Tawari, Nilesh R.,Lalchandani, Jaya,Ray,Rajan,Degani, Mariam S.
supporting information; experimental part, p. 1623 - 1625 (2010/06/16)
In an attempt to identify potential new agents active against tuberculosis, 20 novel phenylacrylamide derivatives incorporating cinnamic acids and guanylhydrazones were synthesized using microwave assisted synthesis. Activity of the synthesized compounds was evaluated using resazurin microtitre plate assay (REMA) against Mycobacterium tuberculosis H37Rv. Based on empirical structure-activity relationship data it was observed that both steric and electronic parameters play major role in the activity of this series of compounds. Compound 7s (2E)-N-((-2-(3,4-dimethoxybenzylidene) hydrazinyl) (imino) methyl)-3-(4-methoxyphenyl) acrylamide showed MIC of 6.49 μM along with good safety profile of >50-fold in VERO cell line. Thus, this compound could act as a potential lead for further antitubercular studies.
