106511-80-2Relevant academic research and scientific papers
Development of thieno- and benzopyrimidinone inhibitors of the Hedgehog signaling pathway reveals PDE4-dependent and PDE4-independent mechanisms of action
Hempel, Jonathan E.,Cadar, Adrian G.,Hong, Charles C.
, p. 1947 - 1953 (2016)
From a high content in vivo screen for modulators of developmental patterning in embryonic zebrafish, we previously identified eggmanone (EGM1, 3) as a Hedgehog (Hh) signaling inhibitor functioning downstream of Smoothened. Phenotypic optimization studies for in vitro probe development utilizing a Gli transcription-linked stable luciferase reporter cell line identified EGM1 analogs with improved potency and aqueous solubility. Mechanistic profiling of optimized analogs indicated two distinct scaffold clusters: PDE4 inhibitors able to inhibit downstream of Sufu, and PDE4-independent Hh inhibitors functioning between Smo and Sufu. Each class represents valuable in vitro probes for elucidating the complex mechanisms of Hh regulation.
Synthesis, analgesic, anti-inflammatory and antibacterial activities of some novel 2-methylthio-3-substituted quinazolin-4-(3H)-ones
Alagarsamy, Veerachamy,Rajesh, Ramadoss,Ramaseshu, Meena,Vijaykumar, Sukumaran,Ramseshu, Kona Venkat,Duraianandakumar, Thirumoorthy
, p. 652 - 656 (2004)
A variety of novel 2-methylthio-3-substituted quinazolin-4-(3H)-ones have been synthesized by reacting (2-methylthio-4-oxo-3H-quinazolin-3-yl) dithiocarbamic acid methyl ester with a variety of amines, the starting material dithiocarbamate was synthesized
Synthesis, analgesic and anti-inflammatory activities of some novel 2,3-disubstituted quinazolin-4(3H)-ones.
Alagarsamy, Veerachamy,Muthukumar, Veluchamy,Pavalarani, Nagendran,Vasanthanathan, Poongavanam,Revathi, Rajappan
, p. 557 - 559 (2003)
A series of novel 2-benzylamino-3-substituted quinazolin-4(3H)-ones have been synthesized by treating 3-amino-2-benzylamino quinazolin-4(3H)-one, with different aldehydes and ketones. The starting material 3-amino-2-benzylamino quinazolin-4(3H)-one was sy
Synthesis and antihypertensive activity of novel 3-benzyl-2-substituted-3H-[1,2,4]triazolo[5,1-b]quinazolin-9-ones
Alagarsamy, Veerachamy,Pathak, Urvishbhai S.
, p. 3457 - 3462 (2008/02/07)
A series of 3-benzyl-2-substituted-3H-[1,2,4]triazolo[5,1-b]quinazolin-9-ones have been synthesized by the cyclocondensation of 3-amino-2-benzylamino-3H-quinazolin-4-one with a variety of one-carbon donors. The starting material 3-amino-2-benzylamino-3H-quinazolin-4-one was synthesized from methyl anthranilate by a novel innovative route. The title compounds were evaluated for their in vivo antihypertensive activity using spontaneously hypertensive rats (SHR). While all the test compounds exhibited significant antihypertensive activity, 3-benzyl-2-methyl-3H-[1,2,4]triazolo[5,1-b] quinazolin-9-one exhibited antihypertensive activity more than the reference standard prazocin.
Synthesis and pharmacological investigation of some novel 2,3-disubstituted quinazolin-4(3H)-ones as analgesic and antiinflammatory agents
Alagarsamy,Meena,Vijayakumar,Ramseshu,Revathi
, p. 233 - 236 (2007/10/03)
A series of novel 2-substituted quinazolin-4(3H)-ones have been synthesized by condensing the aromatic primary amine of 2-substituted quinazolines with different aldehydes and ketones. The synthesized compounds were confirmed by their spectral data (IR, N
A New Synthesis of 1,3,4-Thiadiazoloquinazolin-5-ones
Pathak, U. S.,Devani, M. B.,Shishoo, C. J.,Kulkarni, R. R.,Rakholia, V. M.,et al.
, p. 489 - 491 (2007/10/02)
A new synthesis of 3-amino-2-mercaptoquinazolin-4-one (4) and its cyclization to thiadiazoloquinazolines by reaction with one carbon donors is reported.
