An article Green synthesis, biological evaluation, molecular docking studies and 3D-QSAR analysis of novel phenylalanine linked quinazoline-4(3H)-one-sulphonamide hybrid entities distorting the malarial reductase activity in folate pathway WOS:000476887000008 published article about MICROWAVE-ASSISTED SYNTHESIS; IONIC-LIQUID; DRUG-RESISTANCE; DIHYDROFOLATE-REDUCTASE; SULFONAMIDE; INHIBITORS; ANTICANCER; EFFICIENT; PARASITE; PREDICT in [Patel, Tarosh S.; Dixit, Bharat C.] Sardar Patel Univ, VP&RPTP Sci Coll, Chem Dept, Vallabh Vidyanagar 388120, Gujarat, India; [Bhatt, Jaimin D.] Sardar Patel Univ, VP&RPTP Sci Coll, Ind Chem Dept, Vallabh Vidyanagar 388120, Gujarat, India; [Dixit, Ritu B.] Ashok & Rita Patel Inst Integrated Studies & Res, New Vallabh Vidyanagar 388121, Gujarat, India; [Chudasama, Chaitanya J.] Sardar Patel Univ, Shree Alpesh N Patel PG Inst, Dept Biochem, Anand 388001, Gujarat, India; [Patel, Bhavesh D.] Sardar Patel Univ, VP&RPTP Sci Coll, Microbiol Dept, Vallabh Vidyanagar 388120, Gujarat, India in 2019.0, Cited 65.0. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4. Recommanded Product: 3-Hydroxybenzaldehyde
A modified Grimmel’s method for N-heterocyclization of phenylalanine linked sulphonamide side arm at position-2 was optimized leading to 2,3-disustituted-4-quinazolin-(3H)-ones. Further, [Bmim][BF4]-H2O (IL) was used as green solvent as well as catalyst for the synthesis of twenty two hybrid quinazolinone motifs (4a-4v) by N-heterocyclization reaction using microwave irradiation technique. The in vitro screening of the hybrid entities against the malarial species Plasmodium falciparum yielded five potent molecules 4l, 4n, 4r, 4t & 4u owing comparable antimalarial activity to the reference drugs. In continuation, an in silico study was carried out to obtain a pharmacophoric model and quantitative structure activity relationship. We also built a 3D-QSAR model to procure more information that could be applied to design new molecules with more potent Pf-DHFR inhibitory activity. The designed pharmacophore was recognized to be more potent for the selected molecules, exhibiting five pharmacophoric features. The active scaffolds were further evaluated for enzyme inhibition efficacy against alleged receptor Pf-DHFR computationally and in vitro, proving their candidature as lead dihydrofolate reductase inhibitors as well as the selectivity of the test candidates was ascertained by toxicity study against vero cells. The perception of good oral bioavailability was also proved by study of pharmacokinetic properties.
Recommanded Product: 3-Hydroxybenzaldehyde. About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Patel, TS; Bhatt, JD; Dixit, RB; Chudasama, CJ; Patel, BD; Dixit, BC or concate me.
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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