Synthesis and in vitro antileishmanial efficacy of novel benzothiadiazine‐1,1‐dioxide derivatives
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DOI: 10.1002/ardp.202000280
Abstract: Leishmaniasis is a major vector‐borne parasitic disease that affects thousands of people in tropical and subtropical developing countries. In 2019 alone, it killed 26,000–65,000 individuals. Leishmaniasis is curable, yet its eradication and elimination are hampered… read more here.
Keywords: vitro antileishmanial; antileishmanial efficacy; efficacy novel; synthesis vitro ... See more keywords
Synthesis and in vitro study of antiproliferative benzyloxy dihydropyrimidinones
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DOI: 10.1002/ardp.202000466
Abstract: In this study, we report on antiproliferative benzyloxy dihydropyrimidinones (DHPMs) produced by the Biginelli reaction of benzyloxy benzaldehyde, urea, and diverse 1,3‐diones. The reaction was catalyzed by lanthanum triflate and completed within 1–1.5 h, with 74–97%… read more here.
Keywords: benzyloxy; benzyloxy dihydropyrimidinones; antiproliferative benzyloxy; study ... See more keywords
Isatin thiazoles as antidiabetic: Synthesis, in vitro enzyme inhibitory activities, kinetics, and in silico studies.
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DOI: 10.1002/ardp.202100481
Abstract: Diabetes mellitus is one of the most prevalent diseases nowadays. Several marketed drugs are available for the cure and treatment of diabetes, but there is still a dire need of introducing compatible drug molecules with lesser… read more here.
Keywords: vitro enzyme; synthesis vitro; thiazoles antidiabetic; synthesis ... See more keywords
Design, Synthesis, and in vitro and in vivo Evaluations of (Z)‐3,4,5‐Trimethoxystyrylbenzenesulfonamides/sulfonates as Highly Potent Tubulin Polymerization Inhibitors
Sign Up to like & getrecommendations! Published in 2017 at "ChemMedChem"
DOI: 10.1002/cmdc.201600643
Abstract: Newer therapeutics can be developed in drug discovery by adopting the strategy of scaffold hopping of the privileged scaffolds from known bioactive compounds. This strategy has been widely employed in drug‐discovery processes. Structure‐based docking studies… read more here.
Keywords: tubulin polymerization; synthesis vitro; polymerization; design synthesis ... See more keywords
Synthesis, in vitro Antileishmanial Efficacy and Hit/Lead Identification of Nitrofurantoin‐Triazole Hybrids
Sign Up to like & getrecommendations! Published in 2022 at "Chemmedchem"
DOI: 10.1002/cmdc.202200023
Abstract: Leishmaniasis is a vector‐borne neglected parasitic infection affecting thousands of individuals, mostly among populations in low‐ to moderate‐income developing countries. In the absence of protective vaccines, the management of the disease banks solely on chemotherapy.… read more here.
Keywords: nitrofurantoin triazole; synthesis vitro; efficacy hit; vitro antileishmanial ... See more keywords
Synthesis and in vitro antileishmanial efficacy of benzyl analogues of nifuroxazide
Sign Up to like & getrecommendations! Published in 2020 at "Drug Development Research"
DOI: 10.1002/ddr.21755
Abstract: Leishmaniasis is a vector‐borne parasitic disease that mostly affects populations in tropical and subtropical countries. There is currently no vaccine to protect against and only a handful of drugs are available to treat this disease.… read more here.
Keywords: vitro antileishmanial; synthesis vitro; benzyl analogues; antileishmanial efficacy ... See more keywords
Synthesis and in vitro activities on anti-platelet aggregation of 4-methoxyisophthalamides
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DOI: 10.1007/s00044-018-2207-8
Abstract: A series of 4-methoxyisophthalamides (1d–1w) were designed and synthesized and their chemical structures were confirmed by IR, MS, 1H-NMR, and 13C-NMR. The in vitro on anti-platelet aggregation activities of these compounds were assessed by using… read more here.
Keywords: platelet aggregation; synthesis vitro; anti platelet; vitro activities ... See more keywords
Synthesis, in vitro antifungal evaluation and docking studies of novel derivatives of imidazoles and benzimidazoles
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DOI: 10.1007/s00044-019-02369-7
Abstract: A series of imidazole and benzimidazole derivatives was designed and prepared in good yields via convenient and efficient two steps synthetic route using readily available starting materials. The structures of the synthesized compounds and their… read more here.
Keywords: evaluation docking; studies novel; docking studies; vitro antifungal ... See more keywords
Synthesis and in vitro antimycobacterial and antileishmanial activities of hydroquinone-triazole hybrids
Sign Up to like & getrecommendations! Published in 2020 at "Medicinal Chemistry Research"
DOI: 10.1007/s00044-020-02553-0
Abstract: Infectious diseases such as tuberculosis and leishmaniasis are leading causes of human death. One of the major factors contributing to the poor control of these diseases is primarily the reduced effectiveness of the existing chemotherapies… read more here.
Keywords: vitro antimycobacterial; triazole hybrids; hydroquinone triazole; chemistry ... See more keywords
Design, synthesis, in vitro Evaluation and docking studies on dihydropyrimidine-based urease inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2017.07.003
Abstract: In our previous report, we have identified 3,4-dihydropyrimidine scaffold as promising class of urease inhibitor in a structure based virtual screen (SBVS) experiment. In present study, we attempted to optimize the scaffold by varying C-5… read more here.
Keywords: design synthesis; evaluation docking; urease inhibitors; docking studies ... See more keywords
5,6-Dihydropyrimidine-1(2H)-carbothioamides: Synthesis, in vitro GABA-AT screening, anticonvulsant activity and molecular modelling study.
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DOI: 10.1016/j.bioorg.2017.12.031
Abstract: Even after considerable advances in the field of epilepsy treatment, convulsions are inefficiently controlled by standard drug therapy. Herein, a series of pyrimidine-carbothioamide derivatives 4(a-t) was designed as anticonvulsant agents by doing some important structural… read more here.
Keywords: carbothioamides synthesis; study; synthesis vitro; vitro gaba ... See more keywords