Novel 4-(morpholin-4-yl)-N′-(arylidene)benzohydrazides: Synthesis, antimycobacterial activity and QSAR investigations

Raparti, Vyankatesh T.; Chitre, Trupti S.; Bothara, Kailas; Kumar, Vanaja; Dangre, Sudarshan C.; Khachane, Chetan V.; Gore, Suraj T; Deshmane, Bhavana J.

doi:10.1016/j.ejmech.2009.04.023

Cited by 75 publications

(48 citation statements)

References 23 publications

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“…Morpholine nucleus is an integral part of linezolid, a clinically used drug for the treatment of infections caused by gram-positive bacteria [16]. A number of morpholine containing chemical compounds have also been reported as antimicrobial agents [17][18][19][20][21][22]. Encouraged by these observations and also in continuation of our search for potent antimicrobial agents [23,24] including antimicrobial agents having coumarin moiety [25,26], we decided to prepare some 2-morpholinomethylamino-4-(7-unsubstituted/substitutedcoumarin-3-yl)-6-chlorosubstitutedphenyl pyrimidines, herein after the title compounds (1a-18a), as antimicrobial agents.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Evaluation of Antimicrobial Activity of Some 2-Morpholinomethylamino-4-(7-Unsubstituted/Substituted Coumarin-3-yl)-6-Chlorosubstitutedphenyl Pyrimidines

Abida¹,

Alsalman²

2016

Trop. J. Pharm Res

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Section: Introductionmentioning

confidence: 99%

Synthesis and Evaluation of Antimicrobial Activity of Some 2-Morpholinomethylamino-4-(7-Unsubstituted/Substituted Coumarin-3-yl)-6-Chlorosubstitutedphenyl Pyrimidines

Abida¹,

Alsalman²

2016

Trop. J. Pharm Res

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“…They have become drugs of immense importance and having a variety of biological activities such antitumor (Xia et al, 2007;Vijaya et al, 2007), antianginal (Abadi and Eissa, 2003), antitubercular (Bonde and Gaikwad, 2004;Joshi et al, 2008), antihypertensive (Bhandari et al, 2009;Raparti et al, 2009), MAO enzyme inhibitor (Ke et al, 2008), antibacterial (Joshi et al, 2008. Since the p-hydroxybenzohydrazide, thiadiazole, and thiazolin (Xia et al, 2007;Vijaya et al, 2007) moieties were reported for their anticancer properties, the newly synthesized compounds may show similar pharmacological profile to classical anticancer drugs.…”

Section: Chemistrymentioning

confidence: 99%

Synthesis and antitumor activity of (4-hydroxyphenyl)[5-substituted alkyl/aryl)-2-thioxo-1,3,4-thiadiazol-3-yl]methanone and [(3,4-disubstituted)-1,3-thiazol-2ylidene]-4-hydroxybenzohydrazide

Bhole¹,

Bhusari²

2010

Med Chem Res

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To examine new drug leads with potential anticancer activity, some (4-hydroxyphenyl)[5-substituted alkyl/aryl)-2-thioxo-1,3,4-thiadiazol-3-yl]methanone (4.a-4.c) and [-(3,4-disubstituted)-1,3-thiazol-2ylidene)]-4-hydroxybenzohydrazide (6.a-6.d) were synthesized using appropriate synthetic route. The newly prepared compounds 4.a-4.c and 6.a-6.d demonstrated inhibitory effects on the growth of a wide range of cancer cell lines especially on leukemia (HL-60), non-small lung cancer (HOP-92), renal cancer (ACHN) at the range of GI 50 -4.23 to -7.23.

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“…This moiety has an immense importance for its activity access against many diseases. In recent years, interest has also been focused on thiadiazole derivatives and thiazolidine derivatives of benzohydrazide [18][19][20][21]. …”

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confidence: 99%

Synthesis, Antihypertensive Activity, and 3D‐QSAR Studies of Some New p‐Hydroxybenzohydrazide Derivatives

Bhole¹,

Bhusari²

2010

Archiv der Pharmazie

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p-Hydroxybenzohydrazide 2 on treatment with aromatic/aliphatic aldehyde followed by cyclization with carbon disulphide afforded compounds 4a-4n. Also, compound 2 by treatment of substituted isothiocyanate followed by the treatment of chloroacetic acid yields the corresponding compounds 6a-6i. All the test compounds were assayed for antihypertensive activity by non-invasive blood pressure measurement and invasive blood pressure measurement methods. The test compounds showed significant antihypertensive activity. The intact compounds were subjected to 3D-QSAR studies. The 3D-QSAR analysis was carried out by PHASE program and a statistically reliable model with good predictive power (r(2) = 0.98, q(2) = 0.74) was achieved. The 3D-QSAR plots illustrated insights into the structure-activity relationship of these compounds which may aid in the design of potent p-hydroxybenzohydrazide derivatives as antihypertensive agents.

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Novel 4-(morpholin-4-yl)-N′-(arylidene)benzohydrazides: Synthesis, antimycobacterial activity and QSAR investigations

Cited by 75 publications

References 23 publications

Synthesis and Evaluation of Antimicrobial Activity of Some 2-Morpholinomethylamino-4-(7-Unsubstituted/Substituted Coumarin-3-yl)-6-Chlorosubstitutedphenyl Pyrimidines

Synthesis and Evaluation of Antimicrobial Activity of Some 2-Morpholinomethylamino-4-(7-Unsubstituted/Substituted Coumarin-3-yl)-6-Chlorosubstitutedphenyl Pyrimidines

Synthesis and antitumor activity of (4-hydroxyphenyl)[5-substituted alkyl/aryl)-2-thioxo-1,3,4-thiadiazol-3-yl]methanone and [(3,4-disubstituted)-1,3-thiazol-2ylidene]-4-hydroxybenzohydrazide

Synthesis, Antihypertensive Activity, and 3D‐QSAR Studies of Some New p‐Hydroxybenzohydrazide Derivatives

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